Differential neurotoxicity of etorphine-like opiates: Lack of correlation with their ability to activate opiate receptors

Xiu Hai Ren, Jian Zhao, Lu Pu, Kun Ling, De Ling Yin, Gang Pei

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

The present study was undertaken to compare the neurotoxic effects of three etorphine-like opiates (etorphine, dihydroetorphine, and another derivative of oripavine) and heroin with their ability to activate opiate receptors in human neuroblastoma cell line SK-N-SH as well as in two other neuronal cell lines. Neurotoxicity was measured by using [3H]-thymidine incorporation analysis, cell viability measurement and Cytosensor microphysiometry. It was found that, in spite of the very similar molecular structures of these opiates, they displayed significant differences in cytotoxicity, with etorphine and another derivative of oripavine possessing high potency but dihydroetorphine and heroin little effect. However, neurotoxic potency of the opiates was not directly correlated to their ability to activate opioid receptors, as determined by [35S]-guanylyl-5'- O-(γ-tho)-triphosphate binding assay. These findings provide clear evidence of differential neurotoxicity of etorphine-like opiates, and suggest that the neurotoxicity is not closely related to the molecular configuration required as opioid receptor agonist but is probably associated with the present of a double bond in the structure.

Original languageEnglish (US)
Pages (from-to)735-743
Number of pages9
JournalToxicon
Volume36
Issue number5
DOIs
StatePublished - May 15 1998

ASJC Scopus subject areas

  • Toxicology

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