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

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

doi:10.1126/science.86208

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

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

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-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 language	English (US)
Pages (from-to)	316-318
Number of pages	3
Journal	Science
Volume	204
Issue number	4390
DOIs	https://doi.org/10.1126/science.86208
State	Published - Jan 1 1979

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

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.",

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AU - Caruso, Thomas P.

AU - Takemori, A. E.

AU - Larson, Dennis L.

AU - Portoghese, Philip S

PY - 1979/1/1

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N2 - 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.

AB - 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.

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

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