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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A129844-5mg | 5mg | In stock | $53.90 | |
A129844-25mg | 25mg | In stock | $243.90 | |
A129844-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $874.90 |
CB 1 receptor antagonist / inverse agonist
Synonyms | AM251 | AM-251 | KBio2_002813 | AM 251; AM-251 | AC-32778 | BDBM21279 | KBio3_000489 | N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide | 1h-pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-me |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | AM-251 is a 123I radioisotope and potent CB1 receptor antagonist derivative of the CB1 cannabinoid receptor inverse agonist SR141716A, presenting a radioprobe for in vivo binding studies at the CB1 receptor with a higher affinity (Ki = 7.49 nM) for CB1 th |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | AGONIST, ANTAGONIST |
Mechanism of action | Antagonist of CB 1 receptor;Agonist of GPR18;Agonist of GPR55 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
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IUPAC Name | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide |
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INCHI | InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) |
InChi Key | BUZAJRPLUGXRAB-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I |
Isomeric SMILES | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I |
WGK Germany | 3 |
PubChem CID | 2125 |
Molecular Weight | 555.24 |
PubChem CID | 2125 |
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Wikipedia | AM251 |
CAS Registry No. | 183232-66-8 |
ChEMBL Ligand | CHEMBL285932 |
GPCRdb Ligand | AM251 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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C1911057 | Certificate of Analysis | Nov 16, 2022 | A129844 |
Solubility | Soluble in DMSO (~10 mg/ml), ethanol (~10 mg/ml), DMF (~10 mg/ml), and 1:3 DMSO:PBS (pH 7.2) (~14 mg/ml). Insoluble in water |
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Sensitivity | Heat Sensitive |
Melt Point(°C) | 196-198°C |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
WGK Germany | 3 |
1. Pryce G, Baker D. (2017) Antidote to cannabinoid intoxication: the CB1 receptor inverse agonist, AM251, reverses hypothermic effects of the CB1 receptor agonist, CB-13, in mice.. Br J Pharmacol, 174 (21): (3790-3794). [PMID:28800377] |
2. Zhang D et al.. (2018) Activation of the cannabinoid receptor 1 by ACEA suppresses senescence in human primary chondrocytes through sirt1 activation.. Exp Biol Med (Maywood), 243 (5): (437-443). [PMID:29444596] |
3. Valera AM et al.. (2012) Adaptation of granule cell to Purkinje cell synapses to high-frequency transmission.. J Neurosci, 32 (9): (3267-80). [PMID:22378898] |
4. Tanaka M et al.. (2021) Adenosine A2B receptor down-regulates metabotropic glutamate receptor 5 in astrocytes during postnatal development.. Glia, 69 (11): (2546-2558). [PMID:34339538] |
5. Min R & Nevian T. (2012) Astrocyte signaling controls spike timing-dependent depression at neocortical synapses.. Nat Neurosci, 15 (5): (746-53). [PMID:22446881] |
6. Younts TJ et al.. (2013) CA1 pyramidal cell theta-burst firing triggers endocannabinoid-mediated long-term depression at both somatic and dendritic inhibitory synapses.. J Neurosci, 33 (34): (13743-57). [PMID:23966696] |
7. Ledgerwood CJ et al.. (2011) Cannabidiol inhibits synaptic transmission in rat hippocampal cultures and slices via multiple receptor pathways.. Br J Pharmacol, 162 (286-94). [PMID:20825410] |
8. Newsom RJ et al.. (2012) Cannabinoid receptor type 1 antagonism significantly modulates basal and loud noise induced neural and hypothalamic-pituitary-adrenal axis responses in male Sprague-Dawley rats.. Neuroscience, 204 (64-73). [PMID:22138156] |
9. Anil SM et al.. (2021) Cannabis compounds exhibit anti-inflammatory activity in vitro in COVID-19-related inflammation in lung epithelial cells and pro-inflammatory activity in macrophages.. Sci Rep, 11 (1462). [PMID:33446817] |
10. Anis O et al.. (2021) Cannabis-Derived Compounds Cannabichromene and ?9-Tetrahydrocannabinol Interact and Exhibit Cytotoxic Activity against Urothelial Cell Carcinoma Correlated with Inhibition of Cell Migration and Cytoskeleton Organization.. Molecules, 26 (2): [PMID:33477303] |
11. Landucci E et al.. (2011) CB1 receptors and post-ischemic brain damage: studies on the toxic and neuroprotective effects of cannabinoids in rat organotypic hippocampal slices.. Neuropharmacology, 60 (4): (674-82). [PMID:21130785] |
12. Nissen W et al.. (2010) Cell type-specific long-term plasticity at glutamatergic synapses onto hippocampal interneurons expressing either parvalbumin or CB1 cannabinoid receptor.. J Neurosci, 30 (4): (1337-47). [PMID:20107060] |
13. Zhao Y et al.. (2009) Distinct functional and anatomical architecture of the endocannabinoid system in the auditory brainstem.. J Neurophysiol, 101 (5): (2434-46). [PMID:19279154] |
14. Chiu CQ et al.. (2010) Dopaminergic modulation of endocannabinoid-mediated plasticity at GABAergic synapses in the prefrontal cortex.. J Neurosci, 30 (21): (7236-48). [PMID:20505090] |
15. Hashimotodani Y et al.. (2017) LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance.. Neuron, 95 (4): (928-943.e3). [PMID:28817805] |
16. Zhao Y et al.. (2011) Mechanisms underlying input-specific expression of endocannabinoid-mediated synaptic plasticity in the dorsal cochlear nucleus.. Hear Res, 279 (1-2): (67-73). [PMID:21426926] |
17. Kortleven C et al.. (2012) Neurotensin inhibits glutamate-mediated synaptic inputs onto ventral tegmental area dopamine neurons through the release of the endocannabinoid 2-AG.. Neuropharmacology, 63 (6): (983-91). [PMID:22884466] |
18. Zhao Y & Tzounopoulos T. (2011) Physiological activation of cholinergic inputs controls associative synaptic plasticity via modulation of endocannabinoid signaling.. J Neurosci, 31 (9): (3158-68). [PMID:21368027] |
19. Shalev N et al.. (2022) Phytocannabinoid Compositions from Cannabis Act Synergistically with PARP1 Inhibitor against Ovarian Cancer Cells In Vitro and Affect the Wnt Signaling Pathway.. Molecules, 27 (21): [PMID:36364346] |
20. Sorge RE et al.. (2014) Olfactory exposure to males, including men, causes stress and related analgesia in rodents.. Nat Methods, 11 (6): (629-32). [PMID:24776635] |
21. Ferreira SG et al.. (2015) Presynaptic adenosine A2A receptors dampen cannabinoid CB1 receptor-mediated inhibition of corticostriatal glutamatergic transmission.. Br J Pharmacol, 172 (4): (1074-86). [PMID:25296982] |
22. Dorgans K et al.. (2019) Short-term plasticity at cerebellar granule cell to molecular layer interneuron synapses expands information processing.. Elife, 8 [PMID:31081751] |
23. Peeri H et al.. (2021) Specific Compositions of Cannabis sativa Compounds Have Cytotoxic Activity and Inhibit Motility and Colony Formation of Human Glioblastoma Cells In Vitro.. Cancers (Basel), 13 (7): [PMID:33916466] |
24. Dahlén A et al.. (2021) THC-induced behavioral stereotypy in zebrafish as a model of psychosis-like behavior.. Sci Rep, 11 (15693). [PMID:34344922] |
25. Perez-Rosello T et al.. (2013) Synaptic Zn2+ inhibits neurotransmitter release by promoting endocannabinoid synthesis.. J Neurosci, 33 (22): (9259-72). [PMID:23719795] |
26. Abalo R et al.. (2010) The cannabinoid antagonist SR144528 enhances the acute effect of WIN 55,212-2 on gastrointestinal motility in the rat.. Neurogastroenterol Motil, 22 (6): (694-e206). [PMID:20132133] |
27. Colangeli R et al.. (2017) The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.. Sci Rep, 7 (11152). [PMID:28894217] |
28. Chávez AE et al.. (2010) TRPV1 activation by endogenous anandamide triggers postsynaptic long-term depression in dentate gyrus.. Nat Neurosci, 13 (12): (1511-8). [PMID:21076423] |
29. Weyrer C et al.. (2019) The Role of CaV2.1 Channel Facilitation in Synaptic Facilitation.. Cell Rep, 26 (9): (2289-2297.e3). [PMID:30811980] |