Synthesis and biological activity of analogs of .beta.-chlornaltrexamine and .beta.-funaltrexamine at opioid receptors
- 1 October 1986
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 29 (10) , 1861-1864
- https://doi.org/10.1021/jm00160a011
Abstract
.beta.-Chlornaltrexamine and .beta.-funaltrexamine analogues 4-7 with different length "arms" to which an electrophilic moiety is attached were synthesized in an effort to obtain affinity labels that would selectively and irreversibly block specific opioid receptor types and subtypes. One of the compounds, 4, was a potent, irreversible blocker of opioid receptors in the guinea pig ileum and mouse vas deferens preparations. The results of this study suggest that nucleophiles that are remote from the recognition locus are capable of alkylation by reactive electrophiles.This publication has 6 references indexed in Scilit:
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