Differing stereospecificities distinguish opiate receptor subtypes

Stephen R. Zukin

Research output: Contribution to journalArticlepeer-review

Abstract

Paired stereoisomers of compounds active at the proposed μ,κ and σ classes of opiate receptors display differing stereoselectivity patterns at the receptor subtypes. The (-) isomers of cyclazocine and SKF-10047 are far more potent than the (+) isomers as displacers of [3H]dihydromorphine from receptors. However, the (-) isomers are only moderately more potent than the (+) isomers at displacing [3H]ethylketocyclazocine from κ receptors in an assay controlled for radioligand binding to μ receptors, and the (+) and (-) isomers are similar in potency for displacement of [3H]phencyclidine (PCP) from σ receptors. At the σ/PCP receptor, (+) ketamine proved four times as potent as (-) ketamine, while the dioxalan derivative dexoxadrol is far more potent than its nearly inactive enantiomer levoxadrol. The results for the σ/PCP receptor are in agreement with those of behavioral studies. Stereospecificity patterns may provide support for the concept of the opiate receptor subclasses as biochemically distinct entities.

Original languageEnglish (US)
Pages (from-to)1307-1310
Number of pages4
JournalLife Sciences
Volume31
Issue number12-13
DOIs
StatePublished - 1982
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology

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