GPR139

GPR139 (a.k.a. or GPRg1 or GPCR12), is an orphan receptor first identified as a rhodopsin family GPCR with exclusive expression in the central nervous system. Its closest homolog, GPR142, however, is expressed primarily in the pancreas and other peripheral tissues[1]. GPR139 is coupled with Gq signaling and appears to be constitutively active when recombinantly expressed in mammalian cells[2].


[1] C. Liu et al. 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. 2015 Nov;88(5):911-25.
[2] CA Dvorak et al. Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8.

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Axon ID Name Description From price
2569 JNJ 63533054 Potent, brain-penetrant, selective agonist of GPR139 €90.00
2609 NCRW0005-F05 GPR139 antagonist; useful tool to study GPR139 pharmacology €125.00

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