Potent and selective GPR139 agonist (EC50= 16 nM). Selective for GPR139 over a panel of GPCRs, ion channels and transporters, including GPR142. Brain and cell penetrant.
1.Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, Li Q, Joseph V, Sutton SW, Eckert W et al.. (2015) GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.. Mol Pharmacol, 88 (5):(911-25). [PMID:26349500]
2.Dvorak CA, Coate H, Nepomuceno D, Wennerholm M, Kuei C, Lord B, Woody D, Bonaventure P, Liu C, Lovenberg T et al.. (2015) Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.. ACS Med Chem Lett, 6 (9):(1015-8). [PMID:26396690]
3.Shoblock JR, Welty N, Fraser I, Wyatt R, Lord B, Lovenberg T, Liu C, Bonaventure P. (2019) In vivo Characterization of a Selective, Orally Available, and Brain Penetrant Small Molecule GPR139 Agonist.. Front Pharmacol, 10 (3):(273). [PMID:30949055]
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J2116199