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Science 20 April 1979:
Vol. 204. no. 4390, pp. 316 - 318
DOI: 10.1126/science.86208
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Articles

Science, Vol 204, Issue 4390, 316-318
Copyright © 1979 by American Association for the Advancement of Science

articles

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

TP Caruso, AE Takemori, DL Larson, and PS Portoghese

Chloroxymorphamine, the 6beta-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 sitedirected alkylating agents possess considerable potenial as pharmacologic and biochemical probes of apoid receptors.


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Irreversible ligands with high selectivity toward delta and mu opiate receptors.
K. Rice, A. Jacobson, T. Burke Jr, B. Bajwa, R. Streaty, and W. Klee (1983)
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Opiate analgesia: evidence for mediation by a subpopulation of opiate receptors.
G. Pasternak, Childers SR, and S. Snyder (1980)
Science 208, 514-516
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