CERC-501, also known as JNJ-67953964, LY-2456302 and Aticaprant, is a potent, selective, short-acting antagonist of the kappa-opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the µ-opioid receptor (MOR) and delta-opioid receptor (DOR). Aticaprant is under development for the treatment of major depressive disorder and substance use disorders including alcoholism, nicotine addiction, and illicit drug dependence. Aticaprant has been found to dose-dependently block fentanyl-induced miosis at 25 mg and 60 mg in humans (with minimal to no blockade at doses of 4 to 10 mg), indicating that the drug significantly occupies and antagonizes the MOR at a dose of at least 25 mg but not of 10 mg or less.
Puffer:
Powder
CAS Nummer:
[1174130-61-0]
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