Chloroxymorphamine, an Opioid Receptor Site-Directed Alkylating Agent Having Narcotic Agonist Activity

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.