KSC-12-192 is a drug that is used in scientific research to study the κ-opioid receptor, where it acts as a biased agonist.
KSC-12-192 preferentially activates G-protein coupling over β-arrestin 2 recruitment in vitro, an intrinsic activity shared with many other KOR ligands developed to separate KOR-mediated analgesia from accompanying dysphoria.
Compared with most of the known KOR G-protein biased agonists, KSC-12-192 and its parent compound ML138 do not exhibit stereoisomerism.
Out of a range of tested compounds with the same substituted triazole scaffold (see table), KSC-12-192 had the highest reported in vitro potency as a human KOR agonist (EC50 = 31nM).
Scaffold Identifiers X R1 R2 R3 KSC-12-192 O H CH3 CF3 ML138 KSC-5-240 O H Cl Cl KSC-12-193 S H CH3 CF3 KSC-5-247G S H Cl Cl KSC-12-238-B5 O CH3 CH3 CF3 KSC-12-238-B4 O CH3 Cl Cl
See also Ketazocine RB-64 ICI-199,441 Spiradoline
References