797060-24-3Relevant academic research and scientific papers
Synthesis and biological evaluation of some 6-arylamidomorphines as analogues of morphine-6-glucuronide
MacDougall, James M.,Zhang, Xiao-Dong,Polgar, Willma E.,Khroyan, Taline V.,Toll, Lawrence,Cashman, John R.
, p. 5983 - 5990 (2007/10/03)
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.
