Chloroxymorphamine, and opioid receptor site-directed alkylating agent having narcotic agonist activity.
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.
D000477:Alkylating Agents; D000818:Animals; D002699:Chlorambucil / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D006168:Guinea Pigs; D004091:Hydromorphone / Q000031:analogs & derivatives*; D066298:In Vitro Techniques; D009020:Morphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology; D009271:Naltrexone / Q000031:analogs & derivatives / Q000494:pharmacology; D009588:Nitrogen Mustard Compounds / Q000494:pharmacology*; D009638:Norepinephrine / Q000494:pharmacology; D010111:Oxymorphone / Q000031:analogs & derivatives* / Q000494:pharmacology; D010643:Phenoxybenzamine / Q000494:pharmacology; D011957:Receptors, Opioid / Q000187:drug effects*
D000477:Alkylating Agents; D009588:Nitrogen Mustard Compounds; D011957:Receptors, Opioid; D010643:Phenoxybenzamine; D002699:Chlorambucil; D009270:Naloxone; D009271:Naltrexone; C019299:chloroxymorphamine; D009020:Morphine; D010111:Oxymorphone; D004091:Hydromorphone; D009638:Norepinephrine