JNJ-63533054

JNJ-63533054 is a **potent, selective, and brain-penetrant small molecule agonist of the G protein-coupled receptor 139 (GPR139)**. It demonstrates high selectivity (EC50 ≈ 16 nM) for GPR139 over a broad panel of other GPCRs, ion channels, and transporters, including its closest homologue, GPR142[1][3][5][7][9][10]. JNJ-63533054 is orally bioavailable and crosses the blood-brain barrier, making it valuable for central nervous system studies[7][9][10]. Pharmacologically, it has been shown to modulate behavioral responses relevant to psychiatric and substance use disorders, such as reducing morphine intake and diminishing morphine analgesia in animal models by activating GPR139[2]. It has also been tested in models of anxiety, despair, and anhedonia, with modest effects[1].

Other names

3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide