Synthesis and biological evaluation of some 6-arylamidomorphines as analogues of morphine-6-glucuronide Original Research Article

A series of 6-β-arylamidomorphines was synthesized and biologically evaluated. Various aryl substituents were introduced into the arylamidomorphines to examine substituent structure–activity relationships. Competition binding assays showed that compounds 10a–h bound to the μ opioid receptor with high affinity (0.2–0.6 nM). Functional assays showed that compounds 10a–h acted as full μ opioid receptor agonists. The ED50 of compound 10e·HCl as an analgesic was 12.6 mg/kg in the tail flick latency test in the rat.