Related Experiment Videos
Synthesis, opioid receptor binding, and functional activity of 5'-substituted
Subramaniam Ananthan1, Hollis S Kezar, Surendra K Saini
1Organic Chemistry Department, Southern Research Institute, Birmingham, AL 35255, USA. ananthan@sri.org
Bioorganic & Medicinal Chemistry Letters
|February 5, 2003
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.