Animal and molecular pharmacology of mixed agonist-antagonist analgesic drugs.
1 The pharmacology of analgesic drugs with mixed agonist-antagonist action is reviewed in the light of the theory of drug action at single and multiple receptors. 2 Evidence for a heterogeneous population of opiate receptors in mammalian brain and in isolated tissue preparations is discussed. 3 The unusual pharmacological and pharmacokinetic profiles of the oripavine derivative buprenorphine are discussed in relation to the action of the drug at a molecular level.
D000818:Animals; D001921:Brain / Q000502:physiology; D002047:Buprenorphine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D008297:Male; D051379:Mice; D009292:Narcotic Antagonists / Q000494:pharmacology*; D009294:Narcotics / Q000494:pharmacology*; D051381:Rats; D011957:Receptors, Opioid / Q000502:physiology*; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000187:drug effects
D009292:Narcotic Antagonists; D009294:Narcotics; D011957:Receptors, Opioid; D002047:Buprenorphine