Probes for narcotic receptor mediated phenomena: conceputalization, synthesis, and pharmacological evaluation of ring-expanded phenylmorphans

Monday, October 24, 2011 — Poster Session I
Noon – 2:00 p.m.	Natcher Conference Center	NIDA	BIOCHEM/CHEM-12

Authors

• FY Li
• RB Rothman
• JR Deschamps
• AE Jacobson
• RC Rice

Abstract

A set of topologically distinct ligands have proven to be very useful to understand the ligand-opioid receptor interaction complex and the ligand-opioid receptor interaction. In our laboratory, an isomeric series of structurally rigid and topologically distinct oxide-bridged phenylmorphans was synthesized and evaluated for their affinity to opioid receptors. Several interesting compounds were identified. To further examine the ligand-receptor complex from the viewpoint of the ligand’s structure, we changed the size of the ring to examine structurally similar ligands with somewhat greater flexibility that might allow these ligands to adjust their conformation. This molecular modification might enhance, or change, the ligand’s interaction with opioid receptors.

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