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. 1979 Apr 20;204(4390):316-8.
doi: 10.1126/science.86208.

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

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

T P Caruso et al. Science. .

Abstract

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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