Synthesis,opioid receptor binding,and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans |
| |
Authors: | Ananthan Subramaniam Kezar Hollis S Saini Surendra K Khare Naveen K Davis Peg Dersch Christina M Porreca Frank Rothman Richard B |
| |
Affiliation: | Organic Chemistry Department, Southern Research Institute, Birmingham, AL 35255, USA. ananthan@sri.org |
| |
Abstract: | A series of naltrexone-derived pyridomorphinans possessing various substituents at the 5'-position on the pyridine ring were synthesized and evaluated for opioid receptor binding in rodent brain membranes and functional activity in smooth muscle preparations. While the introduction of aromatic 1-pyrrolyl group (6h) improved the delta affinity and delta antagonist potency of the parent compound (3), the introduction of guanidine group (6i) transformed it to a kappa selective ligand in opioid receptor binding and [35S]GTP-gamma-S functional assays. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|