| Literature DB >> 15498674 |
James M Macdougall1, Xiao-Dong Zhang, Willma E Polgar, Taline V Khroyan, Lawrence Toll, John R Cashman.
Abstract
A series of 6-beta-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 mu opioid receptor with high affinity (0.2-0.6 nM). Functional assays showed that compounds 10a-h acted as full mu opioid receptor agonists. The ED(50) of compound 10e.HCl as an analgesic was 12.6 mg/kg in the tail flick latency test in the rat.Entities:
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Year: 2004 PMID： 15498674 DOI： 10.1016/j.bmc.2004.08.019
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641