JNJ-63533054 | GPR139 agonist, suppresses morphine intake
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $70.00 | ||
| 25 mg | $260.00 |
JNJ-63533054 (1802326-66-4) is a potent and selective brain-penetrant GPR139 agonist (EC50=16 nM) an orphan G-protein-coupled receptor expressed in the CNS.1 Tritium-labeled JNJ-63533054 binds to cell membranes expressing GPR139 and can be displaced by putative endogenous ligands.2 Decreases compulsive-like alcohol drinking and hyperalgesia in alcohol-dependent rodents.3 Suppresses morphine intake in a mouse self-administration model.4
References/Citations:
1) Dvorak et al. (2015), Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor; ACS Med. Chem. Lett., 6 1015
2) Liu 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., 88 911
3) Kononoff et al. (2018), Systemic and Intra-Habenular Activation of the Orphan G Protein-Coupled Receptor GPR139 Decreases Compulsive-Like Alcohol Drinking and Hyperalgesia in Alcohol-Dependent Rats; eNeuro, 5 ENEURO 0153-18 2018
4) Wang et al. (2019), Genetic behavioral screen identifies an orphan anti-opioid system; Science, 365 1267
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
JNJ-63533054 (1802326-66-4) is a potent and selective brain-penetrant GPR139 agonist (EC50=16 nM) an orphan G-protein-coupled receptor expressed in the CNS.1 Tritium-labeled JNJ-63533054 binds to cell membranes expressing GPR139 and can be displaced by putative endogenous ligands.2 Decreases compulsive-like alcohol drinking and hyperalgesia in alcohol-dependent rodents.3 Suppresses morphine intake in a mouse self-administration model.4
References/Citations:
1) Dvorak et al. (2015), Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor; ACS Med. Chem. Lett., 6 1015
2) Liu 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., 88 911
3) Kononoff et al. (2018), Systemic and Intra-Habenular Activation of the Orphan G Protein-Coupled Receptor GPR139 Decreases Compulsive-Like Alcohol Drinking and Hyperalgesia in Alcohol-Dependent Rats; eNeuro, 5 ENEURO 0153-18 2018
4) Wang et al. (2019), Genetic behavioral screen identifies an orphan anti-opioid system; Science, 365 1267
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