Journal article

STRUCTURAL DETERMINANTS OF OMICRON-RECEPTOR AFFINITY

BL LARGENT, H WIKSTROM, AL GUNDLACH, SH SNYDER

MOLECULAR PHARMACOLOGY | WILLIAMS & WILKINS | Published : 1987

Abstract

The structural determinants of sigma receptor affinity have been evaluated by examining a wide range of compounds related to opioids, neuroleptics, and phenylpiperidine dopaminergic structures for affinity at sigma receptor-binding sites labeled with (+)-[3H]3-PPP. Among opioid compounds, requirements for sigma receptor affinity differ strikingly from the determinants of affinity for conventional opiate receptors. Sigma sites display reverse stereoselectivity to classical opiate receptors. Multi-ringed opiate-related compounds such as morphine and naloxone have negligible affinity for sigma sites, with the highest sigma receptor affinity apparent for benzomorphans which lack the C ring of op..

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University of Melbourne Researchers