Chloroxymorphamine, an opioid receptor site-directed alkylating agent having narcotic agonist activity

Thomas P. Caruso, A. E. Takemori, Dennis L. Larson, Philip S Portoghese

Research output: Contribution to journalArticlepeer-review

42 Scopus citations

Abstract

Chloroxymorphamine, the 6β-N,N-bis(2-chloroethyl) derivative of oxymorphone, is a potent nonequilibrium narcotic agonist in the longitudinal muscle preparation of guinea pig ileum. The corresponding naltrexone analog, chlornaltrexamine, is a potent nonequilibrium antagonist of morphine. These receptor site-directed alkylating agents possess considerable potential as pharmacologic and biochemical probes of opioid receptors.

Original languageEnglish (US)
Pages (from-to)316-318
Number of pages3
JournalScience
Volume204
Issue number4390
DOIs
StatePublished - Jan 1 1979

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