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

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Science  20 Apr 1979:
Vol. 204, Issue 4390, pp. 316-318
DOI: 10.1126/science.86208


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.