Novel opioid cyclic tetrapeptides: Trp isomers of CJ‐15,208 exhibit distinct opioid receptor agonism and short‐acting κ opioid receptor antagonism

Abstract

The L-Trp and the D-Trp isomers of CJ-15,208 demonstrate stereospecific opioid activity in vivo. The relatively brief κ opioid receptor antagonism, coupled with the prevention of stress-induced reinstatement of extinguished cocaine-seeking behaviour, suggests the D-Trp isomer could be used therapeutically to maintain abstinence from psychostimulant abuse.