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Recombinant Adenosine A1 Receptor Antibody - Primary antibody, specific to ADORA1, IgG

    Application:
  • IF/ICC
  • WB
Features and benefits
  • Host species: Rabbit
  • Species reactivity(Reacts with): Human,Mouse,Rat
  • Isotype: Rabbit IgG
  • Conjugation: Unconjugated
Item Number
Ab087488
Grouped product items
SKUSizeAvailabilityPrice Qty
Ab087488-10μl
10μl
In stock
$79.90
Ab087488-50μl
50μl
In stock
$239.90
Ab087488-100μl
100μl
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$379.90
Ab087488-1ml
1ml
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,599.90
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Recombinant; Rabbit anti Human Adenosine A1 Receptor Antibody; WB, ICC, IF; Unconjugated

View related series
Click to view target information: ADORA1
Accession#:P30542 Adenosine A1 Receptor ADORA1 Gene ID:134

Basic Description

Product NameRecombinant Adenosine A1 Receptor Antibody - Primary antibody, specific to ADORA1, IgG
SynonymsA1AR antibody | A1R antibody | AA1R antibody | AA1R_HUMAN antibody | Adenosine receptor A1 antibody | ADORA 1antibody | ADORA 1 antibody | ADORA1 antibody | RDC 7 antibody | RDC7 antibody | Ri antibody | Adenosine A1 R | adenosine A1 receptor | Adenosine
Specifications & PurityExactAb™, Validated, Recombinant, 1.0 mg/mL
Host speciesRabbit
SpecificityADORA1
ImmunogenA synthetic peptide derived from human Adenosine A1 Receptor (AA 148-158)
Positive ControlWB: K562, HeLa, HEK293, A549, Raji, MCF7, NIH/3T3 and C6 cell lysates. ICC: MCF7 cells.
ConjugationUnconjugated
GradeExactAb™, Recombinant, Validated
Product Description

Rabbit anti Human Adenosine A1 Receptor Antibody, Recombinant, could be used for WB, ICC, IF and so on.
Application：
WB: 1/500-1/1000
IF/ICC: 1/50-1/200
Protein Function：
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.

Product Properties

IsotypeIgG
SDS-PAGE150 kDa
Purification MethodAntigen affinity purification
FormLiquid
Concentration1.0 mg/mL
Storage TempStore at -20°C,Avoid repeated freezing and thawing
Shipped InIce chest + Ice pads
Stability And StorageStore at 4°C short term (1-2 weeks). Store at -20°C long term (24 months). Upon delivery aliquot. Avoid freeze/thaw cycle.

Images

Recombinant Adenosine A1 Receptor Antibody (Ab087488) - Western Blot
All lanes: Recombinant Adenosine A1 Receptor Antibody (Ab087488) at 1/1000 dilution
Samples: Lysates at 20 µg per lane
Secondary: Goat Anti-Rabbit IgG H&L (HRP) (Ab170144) at 1/20000 dilution

Predicted band size: 37 kDa
Observed band size: 34 kDa
Exposure time: 30.0 s

Recombinant Adenosine A1 Receptor Antibody (Ab087488) - IF/ICC
Immunocytochemistry analysis of Adenosine A1 Receptor (green) in MCF7 using Recombinant Adenosine A1 Receptor Antibody (Ab087488), and cells were counterstained with DAPI (blue).

Associated Targets(Human)

ADORA1 Tclin Adenosine receptor A1 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ADORA1 Tclin Adenosine A1 receptor (17603 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine receptors; A1 & A3 (1051 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine receptors; A1 & A2 (188 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine receptors; A1 & A2b (259 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine receptors; A1 & A2a (250 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine receptor (26 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine receptor A1/Alpha-2A adrenergic receptor (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Application

ApplicationDilution info
WB1/500-1/1000

">

1/500-1/1000

IF/ICC1/50 - 1/200

">

1/50 - 1/200

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

2 results found

Lot NumberCertificate TypeDateItem
ZJ24F0102371Certificate of AnalysisJan 08, 2024 Ab087488
ZJ24F0102370Certificate of AnalysisJan 08, 2024 Ab087488

Related Documents

 SDS

 Specification Sheet

FAQs and Articles

FAQ
Immunofluorescence Staining Protocol (Methanol permeabilization)
Categories: Protocols
Tags:
Frozen section Immunofluorescence staining Tissue section Methanol permeability IF

References

1. Suzuki F, Shimada J, Shiozaki S, Ichikawa S, Ishii A, Nakamura J, Nonaka H, Kobayashi H, Fuse E..  (1993)  Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance..  J Med Chem,  36  (17): (2508-2518).  [PMID:8355252] [10.1021/jm00069a009]
2. Baraldi PG, Cacciari B, Spalluto G, Bergonzoni M, Dionisotti S, Ongini E, Varani K, Borea PA..  (1998)  Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists..  J Med Chem,  41  (12): (2126-2133).  [PMID:9622554] [10.1021/jm9708689]
3. Baraldi PG, Cacciari B, Romagnoli R, Spalluto G, Monopoli A, Ongini E, Varani K, Borea PA..  (2002)  7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility..  J Med Chem,  45  (1): (115-126).  [PMID:11754583] [10.1021/jm010924c]
4. Libert F, Van Sande J, Lefort A, Czernilofsky A, Dumont JE, Vassart G, Ensinger HA, Mendla KD.  (1992)  Cloning and functional characterization of a human A1 adenosine receptor..  Biochem Biophys Res Commun,  187  (2): (919-26).  [PMID:1530647] [10.1021/op500134e]
5. Townsend-Nicholson A, Shine J.  (1992)  Molecular cloning and characterisation of a human brain A1 adenosine receptor cDNA..  Brain Res Mol Brain Res,  16  (3-4): (365-70).  [PMID:1339301] [10.1021/op500134e]
6. Ren H, Stiles GL.  (1994)  Characterization of the human A1 adenosine receptor gene. Evidence for alternative splicing..  J Biol Chem,  269  (4): (3104-10).  [PMID:8300646] [10.1021/op500134e]
7. Peterman C, Sanoski CA.  (2005)  Tecadenoson: a novel, selective A1 adenosine receptor agonist..  Cardiol Rev,  13  (6): (315-21).  [PMID:16230891] [10.1021/op500134e]
8. Yamamoto S, Nakanishi O, Matsui T, Shinohara N, Kinoshita H, Lambert C, Ishikawa T.  (2003)  Intrathecal adenosine A1 receptor agonist attenuates hyperalgesia without inhibiting spinal glutamate release in the rat..  Cell Mol Neurobiol,  23  (2): (175-85).  [PMID:12735630] [10.1021/op500134e]
9. Obiefuna PC, Batra VK, Nadeem A, Borron P, Wilson CN, Mustafa SJ.  (2005)  A novel A1 adenosine receptor antagonist, L-97-1 [3-[2-(4-aminophenyl)-ethyl]-8-benzyl-7-{2-ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-1-propyl-3,7-dihydro-purine-2,6-dione], reduces allergic responses to house dust mite in an allergic rabbit model of asthma..  J Pharmacol Exp Ther,  315  (1): (329-36).  [PMID:16020631] [10.1021/op500134e]
10. Maemoto T, Tada M, Mihara T, Ueyama N, Matsuoka H, Harada K, Yamaji T, Shirakawa K, Kuroda S, Akahane A et al..  (2004)  Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors..  J Pharmacol Sci,  96  (1): (42-52).  [PMID:15351792] [10.1021/op500134e]
11. Bruns RF, Fergus JH.  (1990)  Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes..  Mol Pharmacol,  38  (6): (939-49).  [PMID:2174510] [10.1021/op500134e]
12. Froestl W, Mickel SJ, von Sprecher G, Diel PJ, Hall RG, Maier L, Strub D, Melillo V, Baumann PA, Bernasconi R et al..  (1995)  Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists..  J Med Chem,  38  (17): (3313-31).  [PMID:7650685] [10.1021/op500134e]
13. Kalk P, Eggert B, Relle K, Godes M, Heiden S, Sharkovska Y, Fischer Y, Ziegler D, Bielenberg GW, Hocher B.  (2007)  The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure..  Br J Pharmacol,  151  (7): (1025-32).  [PMID:17558436] [10.1021/op500134e]
14. Yan L, Burbiel JC, Maass A, Müller CE.  (2003)  Adenosine receptor agonists: from basic medicinal chemistry to clinical development..  Expert Opin Emerg Drugs,  8  (2): (537-76).  [PMID:14662005] [10.1021/op500134e]
15. Jacobson KA, Gao ZG.  (2006)  Adenosine receptors as therapeutic targets..  Nat Rev Drug Discov,  5  (3): (247-64).  [PMID:16518376] [10.1021/op500134e]
16. Kuno A, Critz SD, Cui L, Solodushko V, Yang XM, Krahn T, Albrecht B, Philipp S, Cohen MV, Downey JM.  (2007)  Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion..  J Mol Cell Cardiol,  43  (3): (262-71).  [PMID:17632123] [10.1021/op500134e]
17. Hayallah AM, Sandoval-Ramírez J, Reith U, Schobert U, Preiss B, Schumacher B, Daly JW, Müller CE.  (2002)  1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists..  J Med Chem,  45  (7): (1500-10).  [PMID:11906291] [10.1021/op500134e]
18. Saki M, Tsumuki H, Nonaka H, Shimada J, Ichimura M.  (2002)  KF26777 (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride), a new potent and selective adenosine A3 receptor antagonist..  Eur J Pharmacol,  444  (3): (133-41).  [PMID:12063073] [10.1021/op500134e]
19. Elzein E, Zablocki J.  (2008)  A1 adenosine receptor agonists and their potential therapeutic applications..  Expert Opin Investig Drugs,  17  (12): (1901-10).  [PMID:19012505] [10.1021/op500134e]
20. Klotz KN, Falgner N, Kachler S, Lambertucci C, Vittori S, Volpini R, Cristalli G.  (2007)  [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor..  Eur J Pharmacol,  556  (1-3): (14-8).  [PMID:17126322] [10.1021/op500134e]
21. Fredholm BB, IJzerman AP, Jacobson KA, Linden J, Müller CE.  (2011)  International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update..  Pharmacol Rev,  63  (1): (1-34).  [PMID:21303899] [10.1021/op500134e]
22. Galley G, Stalder H, Goergler A, Hoener MC, Norcross RD.  (2012)  Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012..  Bioorg Med Chem Lett,  22  (16): (5244-8).  [PMID:22795332] [10.1021/op500134e]
23. Baqi Y, Atzler K, Köse M, Glänzel M, Müller CE.  (2009)  High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors..  J Med Chem,  52  (12): (3784-93).  [PMID:19463000] [10.1021/op500134e]
24. Shinkre BA, Kumar TS, Gao ZG, Deflorian F, Jacobson KA, Trenkle WC.  (2010)  Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists..  Bioorg Med Chem Lett,  20  (19): (5690-4).  [PMID:20801028] [10.1021/op500134e]
25. Lovell KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ et al..  (2013)  N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats..  Bioorg Med Chem Lett,  23  (13): (3713-8).  [PMID:23727046] [10.1021/op500134e]
26. Cappelli A, Manini M, Valenti S, Castriconi F, Giuliani G, Anzini M, Brogi S, Butini S, Gemma S, Campiani G et al..  (2013)  Synthesis and structure-activity relationship studies in serotonin 5-HT1A receptor agonists based on fused pyrrolidone scaffolds..  Eur J Med Chem,  63  (13): (85-94).  [PMID:23466604] [10.1021/op500134e]
27. Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR et al..  (2008)  cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia..  J Med Chem,  51  (22): (7094-8).  [PMID:18983139] [10.1021/op500134e]
28. Congreve M, Andrews SP, Doré AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A et al..  (2012)  Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design..  J Med Chem,  55  (5): (1898-903).  [PMID:22220592] [10.1021/op500134e]
29. van Westen GJ, van den Hoven OO, van der Pijl R, Mulder-Krieger T, de Vries H, Wegner JK, Ijzerman AP, van Vlijmen HW, Bender A.  (2012)  Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data..  J Med Chem,  55  (16): (7010-20).  [PMID:22827545] [10.1021/op500134e]
30. Carlsson J, Yoo L, Gao ZG, Irwin JJ, Shoichet BK, Jacobson KA.  (2010)  Structure-based discovery of A2A adenosine receptor ligands..  J Med Chem,  53  (9): (3748-55).  [PMID:20405927] [10.1021/op500134e]
31. Kim Y, de Castro S, Gao ZG, Ijzerman AP, Jacobson KA.  (2009)  Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor..  J Med Chem,  52  (7): (2098-108).  [PMID:19284749] [10.1021/op500134e]
32. Coombs TC, Tanega C, Shen M, Wang JL, Auld DS, Gerritz SW, Schoenen FJ, Thomas CJ, Aubé J.  (2013)  Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315..  Bioorg Med Chem Lett,  23  (12): (3654-61).  [PMID:23642479] [10.1021/op500134e]
33. Koch P, Akkari R, Brunschweiger A, Borrmann T, Schlenk M, Küppers P, Köse M, Radjainia H, Hockemeyer J, Drabczyńska A et al..  (2013)  1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases..  Bioorg Med Chem,  21  (23): (7435-52).  [PMID:24139167] [10.1021/op500134e]
34. Tosh DK, Deflorian F, Phan K, Gao ZG, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.  (2012)  Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions..  J Med Chem,  55  (10): (4847-60).  [PMID:22559880] [10.1021/op500134e]
35. Jacobson KA.  (2013)  Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates..  J Med Chem,  56  (10): (3749-67).  [PMID:23597047] [10.1021/op500134e]
36. Migliore M, Habrant D, Sasso O, Albani C, Bertozzi SM, Armirotti A, Piomelli D, Scarpelli R.  (2016)  Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies..  Eur J Med Chem,  109  (13): (216-37).  [PMID:26774927] [10.1021/op500134e]
37. Ma ML, Li M, Gou JJ, Ruan TY, Jin HS, Zhang LH, Wu LC, Li XY, Hu YH, Wen K et al..  (2014)  Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor..  Bioorg Med Chem,  22  (21): (6117-23).  [PMID:25262941] [10.1021/op500134e]
38. Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jörg M, Scammells PJ, May LT, Sexton PM, Christopoulos A.  (2017)  Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity..  Cell,  168  (5): (867-877.e13).  [PMID:28235198] [10.1021/op500134e]
39. Albrecht W, Unger A, Bauer SM, Laufer SA.  (2017)  Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases..  J Med Chem,  60  (13): (5290-5305).  [PMID:28613871] [10.1021/op500134e]
40. Weiss SM, Benwell K, Cliffe IA, Gillespie RJ, Knight AR, Lerpiniere J, Misra A, Pratt RM, Revell D, Upton R et al..  (2003)  Discovery of nonxanthine adenosine A2A receptor antagonists for the treatment of Parkinson's disease..  Neurology,  61  (11 Suppl 6): (S101-6).  [PMID:14663021] [10.1021/op500134e]
41. Gillespie RJ, Adams DR, Bebbington D, Benwell K, Cliffe IA, Dawson CE, Dourish CT, Fletcher A, Gaur S, Giles PR et al..  (2008)  Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives..  Bioorg Med Chem Lett,  18  (9): (2916-9).  [PMID:18406614] [10.1021/op500134e]
42. Tosh DK, Rao H, Bitant A, Salmaso V, Mannes P, Lieberman DI, Vaughan KL, Mattison JA, Rothwell AC, Auchampach JA et al..  (2019)  Design and in Vivo Characterization of A1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series..  J Med Chem,  62  (3): (1502-1522).  [PMID:30605331] [10.1021/op500134e]
43. Dungo R, Deeks ED.  (2013)  Istradefylline: first global approval..  Drugs,  73  (8): (875-82).  [PMID:23700273] [10.1021/op500134e]
44. Drabczyńska A, Müller CE, Schiedel A, Schumacher B, Karolak-Wojciechowska J, Fruziński A, Zobnina W, Yuzlenko O, Kieć-Kononowicz K.  (2007)  Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands..  Bioorg Med Chem,  15  (22): (6956-74).  [PMID:17827019] [10.1021/op500134e]
45. Albrecht-Küpper BE, Leineweber K, Nell PG.  (2012)  Partial adenosine A1 receptor agonists for cardiovascular therapies..  Purinergic Signal,  8  (Suppl 1): (91-9).  [PMID:22081230] [10.1021/op500134e]
46. Meibom D, Albrecht-Küpper B, Diedrichs N, Hübsch W, Kast R, Krämer T, Krenz U, Lerchen HG, Mittendorf J, Nell PG et al..  (2017)  Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases..  ChemMedChem,  12  (10): (728-737).  [PMID:28488817] [10.1021/op500134e]
47. Härter M, Kalthof B, Delbeck M, Lustig K, Gerisch M, Schulz S, Kast R, Meibom D, Lindner N.  (2019)  Novel non-xanthine antagonist of the A2B adenosine receptor: From HTS hit to lead structure..  Eur J Med Chem,  163  (13): (763-778).  [PMID:30576906] [10.1021/op500134e]
48. Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD et al..  (2019)  3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma..  J Med Chem,  62  (15): (6876-6893).  [PMID:31282155] [10.1021/op500134e]
49. Susanna Tchilibon,Bhalchandra V Joshi,Soo-Kyung Kim,Heng T Duong,Zhan-Guo Gao,Kenneth A Jacobson.  (2005-03-18)  (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists..  Journal of medicinal chemistry,  48  ((6)): (1745-1758).  [PMID:15771421]
50. Gemma N Ferguson, Celine Valant, James Horne, Heidi Figler, Bernard L Flynn, Joel Linden, David K Chalmers, Patrick M Sexton, Arthur Christopoulos, Peter J Scammells,.  (2008-09-06)  2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists..  Journal of medicinal chemistry,  51  ((19)): ( 6165-6172 ).  [PMID:18771255]
51. Laura H Heitman, Rajeshwar Narlawar, Henk de Vries, Milou N Willemsen, Dieter Wolfram, Johannes Brussee, Adriaan P Ijzerman,.  (2009-03-20)  Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor..  Journal of medicinal chemistry,  52  ((7)): ( 2036-2042 ).  [PMID:19296599]
52. Ilia Korboukh,Emily A Hull-Ryde,Joseph E Rittiner,Amarjit S Randhawa,Jennifer Coleman,Brendan J Fitzpatrick,Vincent Setola,William P Janzen,Stephen V Frye,Mark J Zylka,Jian Jin.  (2012-06-29)  Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice..  Journal of medicinal chemistry,  55  ((14)): (6467-6477).  [PMID:22738238]
53. Takayuki Fukaya,Takeo Ishiyama,Satoko Baba,Shuji Masumoto.  (2013-09-21)  Identification of a novel benzoxazolone derivative as a selective, orally active 18 kDa translocator protein (TSPO) ligand..  Journal of medicinal chemistry,  56  ((20)): (8191-8195).  [PMID:24050790]
54. Okamura T, Kurogi Y, Hashimoto K, Sato S, Nishikawa H, Kiryu K, Nagao Y..  (2004)  Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma..  Bioorg Med Chem Lett,  14  (14): (3775-3779).  [PMID:15203160] [10.1016/j.bmcl.2004.04.099]
55. Vu CB, Peng B, Kumaravel G, Smits G, Jin X, Phadke D, Engber T, Huang C, Reilly J, Tam S, Grant D, Hetu G, Chen L, Zhang J, Petter RC..  (2004)  Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists..  J Med Chem,  47  (17): (4291-4299).  [PMID:15294001] [10.1021/jm0498405]
56. Ulven T, Receveur JM, Grimstrup M, Rist Ø, Frimurer TM, Gerlach LO, Mathiesen JM, Kostenis E, Uller L, Högberg T..  (2006)  Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits..  J Med Chem,  49  (23): (6638-6641).  [PMID:17154491] [10.1021/jm060657g]
57. Vu CB, Kiesman WF, Conlon PR, Lin KC, Tam M, Petter RC, Smits G, Lutterodt F, Jin X, Chen L, Zhang J..  (2006)  Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists..  J Med Chem,  49  (24): (7132-7139).  [PMID:17125265] [10.1021/jm060539t]
58. Vendrell M, Angulo E, Casadó V, Lluis C, Franco R, Albericio F, Royo M..  (2007)  Novel ergopeptides as dual ligands for adenosine and dopamine receptors..  J Med Chem,  50  (13): (3062-3069).  [PMID:17539620] [10.1021/jm060947x]
59. Neustadt BR, Hao J, Lindo N, Greenlee WJ, Stamford AW, Tulshian D, Ongini E, Hunter J, Monopoli A, Bertorelli R, Foster C, Arik L, Lachowicz J, Ng K, Feng KI..  (2007)  Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines..  Bioorg Med Chem Lett,  17  (5): (1376-1380).  [PMID:17236762] [10.1016/j.bmcl.2006.11.083]
60. Arnold NJ, Arnold R, Beer D, Bhalay G, Collingwood SP, Craig S, Devereux N, Dodds M, Dunstan AR, Fairhurst RA, Farr D, Fullerton JD, Glen A, Gomez S, Haberthuer S, Hatto JD, Howes C, Jones D, Keller TH, Leuenberger B, Moser HE, Muller I, Naef R, Nicklin PA, Sandham DA, Turner KL, Tweed MF, Watson SJ, Zurini M..  (2007)  Potent and selective xanthine-based inhibitors of phosphodiesterase 5..  Bioorg Med Chem Lett,  17  (8): (2376-2379).  [PMID:17337182] [10.1016/j.bmcl.2006.11.019]
61. Zhang X, Rueter JK, Chen Y, Moorjani M, Lanier MC, Lin E, Gross RS, Tellew JE, Williams JP, Lechner SM, Markison S, Joswig T, Malany S, Santos M, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH..  (2008)  Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists..  Bioorg Med Chem Lett,  18  (6): (1778-1783).  [PMID:18329269] [10.1016/j.bmcl.2008.02.032]
62. Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Giles PR, Jordan AM, Knight AR, Lawrence A, Lerpiniere J, Misra A, Pratt RM, Todd RS, Upton R, Weiss SM, Williamson DS..  (2008)  Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives..  Bioorg Med Chem Lett,  18  (9): (2920-2923).  [PMID:18407496] [10.1016/j.bmcl.2008.03.076]
63. Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Jordan AM, Knight AR, Lerpiniere J, Misra A, Pratt RM, Roffey J, Stratton GC, Upton R, Weiss SM, Williamson DS..  (2008)  Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines..  Bioorg Med Chem Lett,  18  (9): (2924-2929).  [PMID:18411049] [10.1016/j.bmcl.2008.03.072]
64. Grice CA, Tays KL, Savall BM, Wei J, Butler CR, Axe FU, Bembenek SD, Fourie AM, Dunford PJ, Lundeen K, Coles F, Xue X, Riley JP, Williams KN, Karlsson L, Edwards JP..  (2008)  Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity..  J Med Chem,  51  (14): (4150-4169).  [PMID:18588282] [10.1021/jm701575k]
65. Melman A, Wang B, Joshi BV, Gao ZG, Castro Sd, Heller CL, Kim SK, Jeong LS, Jacobson KA..  (2008)  Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system..  Bioorg Med Chem,  16  (18): (8546-8556).  [PMID:18752961] [10.1016/j.bmc.2008.08.007]
66. Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P..  (2008)  Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors..  J Med Chem,  51  (21): (6642-6645).  [PMID:18834107] [10.1021/jm800986w]
67. Zhang X, Tellew JE, Luo Z, Moorjani M, Lin E, Lanier MC, Chen Y, Williams JP, Saunders J, Lechner SM, Markison S, Joswig T, Petroski R, Piercey J, Kargo W, Malany S, Santos M, Gross RS, Wen J, Jalali K, O'Brien Z, Stotz CE, Crespo MI, Díaz JL, Slee DH..  (2008)  Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease..  J Med Chem,  51  (22): (7099-7110).  [PMID:18947224] [10.1021/jm800851u]
68. Gilligan PJ, Clarke T, He L, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy JF, Ward K, Zeller K, Wong H, Bai S, Saye J, Grossman S, Zaczek R, Arneric SP, Hartig P, Robertson D, Trainor G..  (2009)  Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists..  J Med Chem,  52  (9): (3084-3092).  [PMID:19361209] [10.1021/jm900025h]
69. Gillespie RJ, Bamford SJ, Gaur S, Jordan AM, Lerpiniere J, Mansell HL, Stratton GC..  (2009)  Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides..  Bioorg Med Chem Lett,  19  (10): (2664-2667).  [PMID:19362836] [10.1016/j.bmcl.2009.03.142]
70. Pal S, Choi WJ, Choe SA, Heller CL, Gao ZG, Chinn M, Jacobson KA, Hou X, Lee SK, Kim HO, Jeong LS..  (2009)  Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists..  Bioorg Med Chem,  17  (10): (3733-3738).  [PMID:19375920] [10.1016/j.bmc.2009.03.034]
71. Tosh DK, Chinn M, Ivanov AA, Klutz AM, Gao ZG, Jacobson KA..  (2009)  Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system..  J Med Chem,  52  (23): (7580-7592).  [PMID:19499950] [10.1021/jm900426g]
72. Gillespie RJ, Bamford SJ, Clay A, Gaur S, Haymes T, Jackson PS, Jordan AM, Klenke B, Leonardi S, Liu J, Mansell HL, Ng S, Saadi M, Simmonite H, Stratton GC, Todd RS, Williamson DS, Yule IA..  (2009)  Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides..  Bioorg Med Chem,  17  (18): (6590-6605).  [PMID:19695884] [10.1016/j.bmc.2009.07.078]
73. Choi WJ, Lee HW, Kim HO, Chinn M, Gao ZG, Patel A, Jacobson KA, Moon HR, Jung YH, Jeong LS..  (2009)  Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists..  Bioorg Med Chem,  17  (23): (8003-8011).  [PMID:19879151] [10.1016/j.bmc.2009.10.011]
74. Fritch PC, McNaughton-Smith G, Amato GS, Burns JF, Eargle CW, Roeloffs R, Harrison W, Jones L, Wickenden AD..  (2010)  Novel KCNQ2/Q3 agonists as potential therapeutics for epilepsy and neuropathic pain..  J Med Chem,  53  (2): (887-896).  [PMID:20020710] [10.1021/jm901497b]
75. Sams AG, Mikkelsen GK, Larsen M, Torup L, Brennum LT, Schrøder TJ, Bang-Andersen B..  (2010)  Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists..  Bioorg Med Chem Lett,  20  (17): (5241-5244).  [PMID:20659802] [10.1016/j.bmcl.2010.06.138]
76. Lee HW, Kim HO, Choi WJ, Choi S, Lee JH, Park SG, Yoo L, Jacobson KA, Jeong LS..  (2010)  Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors..  Bioorg Med Chem,  18  (19): (7015-7021).  [PMID:20826090] [10.1016/j.bmc.2010.08.018]
77. Hou X, Kim HO, Alexander V, Kim K, Choi S, Park SG, Lee JH, Yoo LS, Gao ZG, Jacobson KA, Jeong LS..  (2010)  Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine..  ACS Med Chem Lett,  1  (9): (516-520).  [PMID:21286238] [10.1021/ml1001823]
78. Kumar TS, Mishra S, Deflorian F, Yoo LS, Phan K, Kecskés M, Szabo A, Shinkre B, Gao ZG, Trenkle W, Jacobson KA..  (2011)  Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold..  Bioorg Med Chem Lett,  21  (9): (2740-2745).  [PMID:21185184] [10.1016/j.bmcl.2010.11.082]
79. Federico S, Paoletta S, Cheong SL, Pastorin G, Cacciari B, Stragliotto S, Klotz KN, Siegel J, Gao ZG, Jacobson KA, Moro S, Spalluto G..  (2011)  Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility..  J Med Chem,  54  (3): (877-889).  [PMID:21214204] [10.1021/jm101349u]
80. Baraldi PG, Saponaro G, Aghazadeh Tabrizi M, Baraldi S, Romagnoli R, Moorman AR, Varani K, Borea PA, Preti D..  (2012)  Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists..  Bioorg Med Chem,  20  (2): (1046-1059).  [PMID:22204739] [10.1016/j.bmc.2011.11.037]
81. Hou X, Majik MS, Kim K, Pyee Y, Lee Y, Alexander V, Chung HJ, Lee HW, Chandra G, Lee JH, Park SG, Choi WJ, Kim HO, Phan K, Gao ZG, Jacobson KA, Choi S, Lee SK, Jeong LS..  (2012)  Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands..  J Med Chem,  55  (1): (342-356).  [PMID:22142423] [10.1021/jm201229j]
82. Deflorian F, Kumar TS, Phan K, Gao ZG, Xu F, Wu H, Katritch V, Stevens RC, Jacobson KA..  (2012)  Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A₂A adenosine receptor..  J Med Chem,  55  (1): (538-552).  [PMID:22104008] [10.1021/jm201461q]
83. Tosh DK, Phan K, Deflorian F, Wei Q, Gao ZG, Jacobson KA..  (2011)  Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element..  ACS Med Chem Lett,  2  (8): (626-631).  [PMID:21858244] [10.1021/ml200114q]
84. Sun X, Qiu J, Strong SA, Green LS, Wasley JW, Blonder JP, Colagiovanni DB, Stout AM, Mutka SC, Richards JP, Rosenthal GJ..  (2012)  Structure-activity relationship of pyrrole based S-nitrosoglutathione reductase inhibitors: carboxamide modification..  Bioorg Med Chem Lett,  22  (6): (2338-2342).  [PMID:22342142] [10.1016/j.bmcl.2012.01.047]
85. Vernall AJ, Stoddart LA, Briddon SJ, Hill SJ, Kellam B..  (2012)  Highly potent and selective fluorescent antagonists of the human adenosine A₃ receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold..  J Med Chem,  55  (4): (1771-1782).  [PMID:22277057] [10.1021/jm201722y]
86. El-Tayeb A, Michael S, Abdelrahman A, Behrenswerth A, Gollos S, Nieber K, Müller CE..  (2011)  Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists..  ACS Med Chem Lett,  2  (12): (890-895).  [PMID:24900277] [10.1021/ml200189u]
87. Melancon BJ, Hopkins CR, Wood MR, Emmitte KA, Niswender CM, Christopoulos A, Conn PJ, Lindsley CW..  (2012)  Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery..  J Med Chem,  55  (4): (1445-1464).  [PMID:22148748] [10.1021/jm201139r]
88. Tosh DK, Paoletta S, Phan K, Gao ZG, Jacobson KA..  (2012)  Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions..  ACS Med Chem Lett,  3  (7): (596-601).  [PMID:23145215] [10.1021/ml300107e]
89. Carlsson J, Tosh DK, Phan K, Gao ZG, Jacobson KA..  (2012)  Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists..  ACS Med Chem Lett,  3  (9): (715-720).  [PMID:23342198] [10.1021/ml300097g]
90. Chen T, Benmohamed R, Kim J, Smith K, Amante D, Morimoto RI, Kirsch DR, Ferrante RJ, Silverman RB..  (2012)  ADME-guided design and synthesis of aryloxanyl pyrazolone derivatives to block mutant superoxide dismutase 1 (SOD1) cytotoxicity and protein aggregation: potential application for the treatment of amyotrophic lateral sclerosis..  J Med Chem,  55  (1): (515-527).  [PMID:22191331] [10.1021/jm2014277]
91. Tosh DK, Paoletta S, Deflorian F, Phan K, Moss SM, Gao ZG, Jiang X, Jacobson KA..  (2012)  Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity..  J Med Chem,  55  (18): (8075-8090).  [PMID:22921089] [10.1021/jm300965a]
92. Annedi SC, Maddaford SP, Ramnauth J, Renton P, Rybak T, Silverman S, Rakhit S, Mladenova G, Dove P, Andrews JS, Zhang D, Porreca F..  (2012)  Discovery of a potent, orally bioavailable and highly selective human neuronal nitric oxide synthase (nNOS) inhibitor, N-(1-(piperidin-4-yl)indolin-5-yl)thiophene-2-carboximidamide as a pre-clinical development candidate for the treatment of migraine..  Eur J Med Chem,  55  (94-107).  [PMID:22840695] [10.1016/j.ejmech.2012.07.006]
93. Squarcialupi L, Colotta V, Catarzi D, Varano F, Filacchioni G, Varani K, Corciulo C, Vincenzi F, Borea PA, Ghelardini C, Di Cesare Mannelli L, Ciancetta A, Moro S..  (2013)  2-Arylpyrazolo[4,3-d]pyrimidin-7-amino derivatives as new potent and selective human A3 adenosine receptor antagonists. Molecular modeling studies and pharmacological evaluation..  J Med Chem,  56  (6): (2256-2269).  [PMID:23427825] [10.1021/jm400068e]
94. Karlström S, Nordvall G, Sohn D, Hettman A, Turek D, Åhlin K, Kers A, Claesson M, Slivo C, Lo-Alfredsson Y, Petersson C, Bessidskaia G, Svensson PH, Rein T, Jerning E, Malmberg Å, Ahlgen C, Ray C, Vares L, Ivanov V, Johansson R..  (2013)  Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1)..  J Med Chem,  56  (8): (3177-3190).  [PMID:23516963] [10.1021/jm3012273]
95. Jörg M, Shonberg J, Mak FS, Miller ND, Yuriev E, Scammells PJ, Capuano B..  (2013)  Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space..  Bioorg Med Chem Lett,  23  (11): (3427-3433).  [PMID:23602401] [10.1016/j.bmcl.2013.03.070]
96. Stössel A, Schlenk M, Hinz S, Küppers P, Heer J, Gütschow M, Müller CE..  (2013)  Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones..  J Med Chem,  56  (11): (4580-4596).  [PMID:23631427] [10.1021/jm400336x]
97. Wang Y, Liu JJ, Dransfield PJ, Zhu L, Wang Z, Du X, Jiao X, Su Y, Li AR, Brown SP, Kasparian A, Vimolratana M, Yu M, Pattaropong V, Houze JB, Swaminath G, Tran T, Nguyen K, Guo Q, Zhang J, Zhuang R, Li F, Miao L, Bartberger MD, Correll TL, Chow D, Wong S, Luo J, Lin DC, Medina JC..  (2013)  Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles..  ACS Med Chem Lett,  4  (6): (551-555).  [PMID:24900707] [10.1021/ml300427u]
98. Germain AR, Carmody LC, Nag PP, Morgan B, Verplank L, Fernandez C, Donckele E, Feng Y, Perez JR, Dandapani S, Palmer M, Lander ES, Gupta PB, Schreiber SL, Munoz B..  (2013)  Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells..  Bioorg Med Chem Lett,  23  (6): (1834-1838).  [PMID:23403082] [10.1016/j.bmcl.2013.01.025]
99. Inamdar GS, Pandya AN, Thakar HM, Sudarsanam V, Kachler S, Sabbadin D, Moro S, Klotz KN, Vasu KK..  (2013)  New insight into adenosine receptors selectivity derived from a novel series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamides and furamides..  Eur J Med Chem,  63  (924-934).  [PMID:23685887] [10.1016/j.ejmech.2013.03.020]
100. Piersanti G, Bartoccini F, Lucarini S, Cabri W, Stasi MA, Riccioni T, Borsini F, Tarzia G, Minetti P..  (2013)  Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease..  J Med Chem,  56  (13): (5456-5463).  [PMID:23789814] [10.1021/jm400491x]
101. Paoletta S, Tosh DK, Finley A, Gizewski ET, Moss SM, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA..  (2013)  Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain..  J Med Chem,  56  (14): (5949-5963).  [PMID:23789857] [10.1021/jm4007966]
102. Nayak A, Chandra G, Hwang I, Kim K, Hou X, Kim HO, Sahu PK, Roy KK, Yoo J, Lee Y, Cui M, Choi S, Moss SM, Phan K, Gao ZG, Ha H, Jacobson KA, Jeong LS..  (2014)  Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists..  J Med Chem,  57  (4): (1344-1354).  [PMID:24456490] [10.1021/jm4015313]
103. Schroeder CE, Yao T, Sotsky J, Smith RA, Roy S, Chu YK, Guo H, Tower NA, Noah JW, McKellip S, Sosa M, Rasmussen L, Smith LH, White EL, Aubé J, Jonsson CB, Chung D, Golden JE..  (2014)  Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-amidinophenylbenzamides as potent inhibitors of venezuelan equine encephalitis virus..  J Med Chem,  57  (20): (8608-8621).  [PMID:25244572] [10.1021/jm501203v]
104. Takai K, Inoue Y, Konishi Y, Suwa A, Uruno Y, Matsuda H, Nakako T, Sakai M, Nishikawa H, Hashimoto G, Enomoto T, Kitamura A, Uematsu Y, Kiyoshi A, Sumiyoshi T..  (2014)  Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists..  Bioorg Med Chem Lett,  24  (14): (3189-3193).  [PMID:24856064] [10.1016/j.bmcl.2014.04.085]
105. Toti KS, Moss SM, Paoletta S, Gao ZG, Jacobson KA, Van Calenbergh S..  (2014)  Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators..  Bioorg Med Chem,  22  (15): (4257-4268).  [PMID:24931275] [10.1016/j.bmc.2014.05.036]
106. Tosh DK, Paoletta S, Chen Z, Moss SM, Gao ZG, Salvemini D, Jacobson KA..  (2014)  Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor..  Bioorg Med Chem Lett,  24  (15): (3302-3306).  [PMID:24969016] [10.1016/j.bmcl.2014.06.006]
107. Mikkelsen GK, Langgård M, Schrøder TJ, Kreilgaard M, Jørgensen EB, Brandt G, Griffon Y, Boffey R, Bang-Andersen B..  (2015)  Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility..  Bioorg Med Chem Lett,  25  (6): (1212-1216).  [PMID:25701253] [10.1016/j.bmcl.2015.01.062]
108. Petrelli R, Torquati I, Kachler S, Luongo L, Maione S, Franchetti P, Grifantini M, Novellino E, Lavecchia A, Klotz KN, Cappellacci L..  (2015)  5'-C-Ethyl-tetrazolyl-N(6)-substituted adenosine and 2-chloro-adenosine derivatives as highly potent dual acting A1 adenosine receptor agonists and A3 adenosine receptor antagonists..  J Med Chem,  58  (5): (2560-2566).  [PMID:25699637] [10.1021/acs.jmedchem.5b00074]
109. Preti D, Baraldi PG, Saponaro G, Romagnoli R, Aghazadeh Tabrizi M, Baraldi S, Cosconati S, Bruno A, Novellino E, Vincenzi F, Ravani A, Borea PA, Varani K..  (2015)  Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor..  J Med Chem,  58  (7): (3253-3267).  [PMID:25780876] [10.1021/acs.jmedchem.5b00215]
110. Lopez-Tapia F, Walker KA, Brotherton-Pleiss C, Caroon J, Nitzan D, Lowrie L, Gleason S, Zhao SH, Berger J, Cockayne D, Phippard D, Suttmann R, Fitch WL, Bourdet D, Rege P, Huang X, Broadbent S, Dvorak C, Zhu J, Wagner P, Padilla F, Loe B, Jahangir A, Alker A..  (2015)  Novel Series of Dihydropyridinone P2X7 Receptor Antagonists..  J Med Chem,  58  (21): (8413-8426).  [PMID:26460788] [10.1021/acs.jmedchem.5b00365]
111. Tosh DK, Paoletta S, Chen Z, Crane S, Lloyd J, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA..  (2015)  Structure-Based Design, Synthesis by Click Chemistry and in Vivo Activity of Highly Selective A3 Adenosine Receptor Agonists..  Medchemcomm,  6  (4): (555-563).  [PMID:26236460] [10.1039/c4md00571f]
112. Donegan RK, Lieberman RL..  (2016)  Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions..  J Med Chem,  59  (3): (788-809).  [PMID:26356532] [10.1021/acs.jmedchem.5b00828]
113. Huard K, Gosset JR, Montgomery JI, Gilbert A, Hayward MM, Magee TV, Cabral S, Uccello DP, Bahnck K, Brown J, Purkal J, Gorgoglione M, Lanba A, Futatsugi K, Herr M, Genung NE, Aspnes G, Polivkova J, Garcia-Irizarry CN, Li Q, Canterbury D, Niosi M, Vera NB, Li Z, Khunte B, Siderewicz J, Rolph T, Erion DM..  (2016)  Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family..  J Med Chem,  59  (3): (1165-1175).  [PMID:26734723] [10.1021/acs.jmedchem.5b01752]
114. Waszkielewicz AM, Gunia-Krzyżak A, Powroźnik B, Słoczyńska K, Pękala E, Walczak M, Bednarski M, Żesławska E, Nitek W, Marona H..  (2016)  Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents..  Bioorg Med Chem,  24  (8): (1793-1810).  [PMID:26988801] [10.1016/j.bmc.2016.03.006]
115. Tosh DK, Ciancetta A, Warnick E, O'Connor R, Chen Z, Gizewski E, Crane S, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA..  (2016)  Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists..  J Med Chem,  59  (7): (3249-3263).  [PMID:26890707] [10.1021/acs.jmedchem.5b01998]
116. Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood E, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, Zhang H, Heise CE, Oh A, Ong CC, La H, Chakravarty P, Chan C, Jakubiak D, Epler J, Ramaswamy S, Vega R, Cain G, Diaz D, Zhong Y..  (2016)  Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window..  J Med Chem,  59  (11): (5520-5541).  [PMID:27167326] [10.1021/acs.jmedchem.6b00638]
117. Tosh DK, Ciancetta A, Warnick E, Crane S, Gao ZG, Jacobson KA..  (2016)  Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists..  J Med Chem,  59  (24): (11006-11026).  [PMID:27933810] [10.1021/acs.jmedchem.6b01183]
118. Gràcia J, Buil MA, Castro J, Eichhorn P, Ferrer M, Gavaldà A, Hernández B, Segarra V, Lehner MD, Moreno I, Pagès L, Roberts RS, Serrat J, Sevilla S, Taltavull J, Andrés M, Cabedo J, Vilella D, Calama E, Carcasona C, Miralpeix M..  (2016)  Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships..  J Med Chem,  59  (23): (10479-10497).  [PMID:27933955] [10.1021/acs.jmedchem.6b00829]
119. Blanco MJ, Benesh DR, Knobelsdorf JA, Khilevich A, Cortez GS, Mokube F, Aicher TD, Groendyke TM, Marmsater FP, Tang TP, Johnson KW, Clemens-Smith A, Muhlhauser MA, Swanson S, Catlow J, Emkey R, Johnson MP, Schkeryantz JM..  (2017)  Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache..  Bioorg Med Chem Lett,  27  (2): (323-328).  [PMID:27908761] [10.1016/j.bmcl.2016.11.049]
120. Basu S, Barawkar DA, Thorat S, Shejul YD, Patel M, Naykodi M, Jain V, Salve Y, Prasad V, Chaudhary S, Ghosh I, Bhat G, Quraishi A, Patil H, Ansari S, Menon S, Unadkat V, Thakare R, Seervi MS, Meru AV, De S, Bhamidipati RK, Rouduri SR, Palle VP, Chug A, Mookhtiar KA..  (2017)  Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation..  J Med Chem,  60  (2): (681-694).  [PMID:28055204] [10.1021/acs.jmedchem.6b01584]
121. Yu J, Zhao LX, Park J, Lee HW, Sahu PK, Cui M, Moss SM, Hammes E, Warnick E, Gao ZG, Noh M, Choi S, Ahn HC, Choi J, Jacobson KA, Jeong LS..  (2017)  N6-Substituted 5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation..  J Med Chem,  60  (8): (3422-3437).  [PMID:28380296] [10.1021/acs.jmedchem.7b00241]
122. Falsini M, Squarcialupi L, Catarzi D, Varano F, Betti M, Dal Ben D, Marucci G, Buccioni M, Volpini R, De Vita T, Cavalli A, Colotta V..  (2017)  The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A2A Receptor Subtype..  J Med Chem,  60  (13): (5772-5790).  [PMID:28590753] [10.1021/acs.jmedchem.7b00457]
123. Yu J, Ahn S, Kim HJ, Lee M, Ahn S, Kim J, Jin SH, Lee E, Kim G, Cheong JH, Jacobson KA, Jeong LS, Noh M..  (2017)  Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential..  J Med Chem,  60  (17): (7459-7475).  [PMID:28799755] [10.1021/acs.jmedchem.7b00805]
124. Basu S, Barawkar DA, Ramdas V, Patel M, Waman Y, Panmand A, Kumar S, Thorat S, Naykodi M, Goswami A, Reddy BS, Prasad V, Chaturvedi S, Quraishi A, Menon S, Paliwal S, Kulkarni A, Karande V, Ghosh I, Mustafa S, De S, Jain V, Banerjee ER, Rouduri SR, Palle VP, Chugh A, Mookhtiar KA..  (2017)  Design and synthesis of novel xanthine derivatives as potent and selective A2B adenosine receptor antagonists for the treatment of chronic inflammatory airway diseases..  Eur J Med Chem,  134  (218-229).  [PMID:28415011] [10.1016/j.ejmech.2017.04.014]
125. Williamson DS, Smith GP, Acheson-Dossang P, Bedford ST, Chell V, Chen IJ, Daechsel JCA, Daniels Z, David L, Dokurno P, Hentzer M, Herzig MC, Hubbard RE, Moore JD, Murray JB, Newland S, Ray SC, Shaw T, Surgenor AE, Terry L, Thirstrup K, Wang Y, Christensen KV..  (2017)  Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1)..  J Med Chem,  60  (21): (8945-8962).  [PMID:29023112] [10.1021/acs.jmedchem.7b01186]
126. Aurelio L, Baltos JA, Ford L, Nguyen ATN, Jörg M, Devine SM, Valant C, White PJ, Christopoulos A, May LT, Scammells PJ..  (2018)  A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists..  J Med Chem,  61  (5): (2087-2103).  [PMID:29446948] [10.1021/acs.jmedchem.8b00047]
127. Petrelli R, Scortichini M, Kachler S, Boccella S, Cerchia C, Torquati I, Del Bello F, Salvemini D, Novellino E, Luongo L, Maione S, Jacobson KA, Lavecchia A, Klotz KN, Cappellacci L..  (2017)  Exploring the Role of N6-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice ∇..  J Med Chem,  60  (10): (4327-4341).  [PMID:28447789] [10.1021/acs.jmedchem.7b00291]
128. Patel S, Meilandt WJ, Erickson RI, Chen J, Deshmukh G, Estrada AA, Fuji RN, Gibbons P, Gustafson A, Harris SF, Imperio J, Liu W, Liu X, Liu Y, Lyssikatos JP, Ma C, Yin J, Lewcock JW, Siu M..  (2017)  Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease..  J Med Chem,  60  (19): (8083-8102).  [PMID:28929759] [10.1021/acs.jmedchem.7b00843]
129. Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T..  (2018)  Identification and biological evaluation of thiazole-based inverse agonists of RORγt..  Bioorg Med Chem Lett,  28  (9): (1446-1455).  [PMID:29631962] [10.1016/j.bmcl.2018.03.093]
130. Jaiteh M, Zeifman A, Saarinen M, Svenningsson P, Bréa J, Loza MI, Carlsson J..  (2018)  Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease..  J Med Chem,  61  (12): (5269-5278).  [PMID:29792714] [10.1021/acs.jmedchem.8b00204]
131. Paz OS, de Jesus Pinheiro M, do Espirito Santo RF, Villarreal CF, Castilho MS..  (2017)  Nanomolar anti-sickling compounds identified by ligand-based pharmacophore approach..  Eur J Med Chem,  136  (487-496).  [PMID:28528302] [10.1016/j.ejmech.2017.05.035]
132. Lambertucci C, Marucci G, Dal Ben D, Buccioni M, Spinaci A, Kachler S, Klotz KN, Volpini R..  (2018)  New potent and selective A1 adenosine receptor antagonists as potential tools for the treatment of gastrointestinal diseases..  Eur J Med Chem,  151  (199-213).  [PMID:29614417] [10.1016/j.ejmech.2018.03.067]
133. Basu S, Barawkar DA, Ramdas V, Naykodi M, Shejul YD, Patel M, Thorat S, Panmand A, Kashinath K, Bonagiri R, Prasad V, Bhat G, Quraishi A, Chaudhary S, Magdum A, Meru AV, Ghosh I, Bhamidipati RK, Raje AA, Madgula VLM, De S, Rouduri SR, Palle VP, Chugh A, Hariharan N, Mookhtiar KA..  (2017)  Discovery of Potent and Selective A2A Antagonists with Efficacy in Animal Models of Parkinson's Disease and Depression..  ACS Med Chem Lett,  8  (8): (835-840).  [PMID:28835798] [10.1021/acsmedchemlett.7b00175]
134. Duroux R, Ciancetta A, Mannes P, Yu J, Boyapati S, Gizewski E, Yous S, Ciruela F, Auchampach JA, Gao ZG, Jacobson KA..  (2017)  Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners..  Medchemcomm,  8  (8): (1659-1667).  [PMID:29250307] [10.1039/C7MD00247E]
135. Vanda D, Zajdel P, Soural M..  (2019)  Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases..  Eur J Med Chem,  181  (111569-111569).  [PMID:31404862] [10.1016/j.ejmech.2019.111569]
136. Brunschweiger A, Koch P, Schlenk M, Rafehi M, Radjainia H, Küppers P, Hinz S, Pineda F, Wiese M, Hockemeyer J, Heer J, Denonne F, Müller CE..  (2016)  8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors..  Bioorg Med Chem,  24  (21): (5462-5480).  [PMID:27658798] [10.1016/j.bmc.2016.09.003]
137. Załuski M, Schabikowski J, Schlenk M, Olejarz-Maciej A, Kubas B, Karcz T, Kuder K, Latacz G, Zygmunt M, Synak D, Hinz S, Müller CE, Kieć-Kononowicz K..  (2019)  Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies..  Bioorg Med Chem,  27  (7): (1195-1210).  [PMID:30808606] [10.1016/j.bmc.2019.02.004]
138. Pieterse L, van der Walt MM, Terre'Blanche G..  (2020)  C2-substituted quinazolinone derivatives exhibit A1 and/or A2A adenosine receptor affinities in the low micromolar range..  Bioorg Med Chem Lett,  30  (16): (127274-127274).  [PMID:32631506] [10.1016/j.bmcl.2020.127274]
139. Iwaki Y,Yashiro K,Kokubo M,Mori T,Wieting JM,McGowan KM,Bridges TM,Engers DW,Denton JS,Kurata H,Lindsley CW.  (2019)  Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249..  Bioorg Med Chem Lett,  29  (13.0): (1601-1604).  [PMID:31072652] [10.1016/j.bmcl.2019.04.048]
140. Abdelrahman A,Yerande SG,Namasivayam V,Klapschinski TA,Alnouri MW,El-Tayeb A,Müller CE.  (2020)  Substituted 4-phenylthiazoles: Development of potent and selective A, A and dual A/A adenosine receptor antagonists..  Eur J Med Chem,  186  (111879-111879).  [PMID:31780082] [10.1016/j.ejmech.2019.111879]
141. Urabe H,Miyakoshi N,Ohtake N,Nozoe A,Ochi M,Fukasawa M,Kinoshita K,Yamaguchi JI,Marumo T,Hikichi H,Chaki S,Hashihayata T.  (2020)  Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability..  Eur J Med Chem,  203  (112521-112521).  [PMID:32698110] [10.1016/j.ejmech.2020.112521]
142. Sahin Z,Biltekin SN,Yurttas L,Berk B,Özhan Y,Sipahi H,Gao ZG,Jacobson KA,Demirayak Ş.  (2021)  Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition..  Eur J Med Chem,  212  (113125-113125).  [PMID:33422981] [10.1016/j.ejmech.2020.113125]
143. Reddy GL, Sarma R, Liu S, Huang W, Lei J, Fu J, Hu W..  (2021)  Design, synthesis and biological evaluation of novel scaffold benzo[4,5]imidazo [1,2-a]pyrazin-1-amine: Towards adenosine A2A receptor (A2A AR) antagonist..  Eur J Med Chem,  210  (113040-113040).  [PMID:33316692] [10.1016/j.ejmech.2020.113040]
144. Jacobson, Kenneth A KA and 7 more authors..  (2005)  A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists..  Chemistry & biology,      [PMID:15734651]
145. Ellenbogen, Kenneth A KA and 10 more authors..  (2005)  Trial to evaluate the management of paroxysmal supraventricular tachycardia during an electrophysiology study with tecadenoson..  Circulation,    (21):   [PMID:15956124]
146. Gregory, S G SG and 178 more authors..  (2006)  The DNA sequence and biological annotation of human chromosome 1..  Nature,    (18):   [PMID:16710414]
147. Sjöblom, Tobias T and 28 more authors..  (2006)  The consensus coding sequences of human breast and colorectal cancers..  Science (New York, N.Y.),    (13):   [PMID:16959974]
148. Mustafa, S S, Venkatesh, P P, Pasha, K K, Mullangi, R R and Srinivas, N R NR..  (2006)  Altered intravenous pharmacokinetics of topotecan in rats with acute renal failure (ARF) induced by uranyl nitrate: do adenosine A1 antagonists (selective/non-selective) normalize the altered topotecan kinetics in ARF?.  Xenobiotica; the fate of foreign compounds in biological systems,      [PMID:17162470]
149. Gonca, Ersöz E and Darıcı, Faruk F..  (2015)  The effect of cannabidiol on ischemia/reperfusion-induced ventricular arrhythmias: the role of adenosine A1 receptors..  Journal of cardiovascular pharmacology and therapeutics,      [PMID:24853683]
150. Martins, Daniel F DF and 7 more authors..  (2015)  Caffeine prevents antihyperalgesic effect of gabapentin in an animal model of CRPS-I: evidence for the involvement of spinal adenosine A1 receptor..  Journal of the peripheral nervous system : JPNS,      [PMID:26456872]
151. Jaberi, Elham E and 13 more authors..  (2016)  Mutation in ADORA1 identified as likely cause of early-onset parkinsonism and cognitive dysfunction..  Movement disorders : official journal of the Movement Disorder Society,      [PMID:27134041]
152. Rodríguez, David and 7 more authors..  (2016)  Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists..  ACS chemical biology,    (21):   [PMID:27439119]
153. Qi, Wei W and 39 more authors..  (2017)  An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED..  Nature chemical biology,      [PMID:28135235]
154. Barakat, Ahmed A..  (2019)  Revisiting Tramadol: A Multi-Modal Agent for Pain Management..  CNS drugs,      [PMID:31004280]

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