Nalorphine-like properties of some 2,3-dimethyl-3-arylpiperidines.
A number of N-substituted 2,3-dimethyl-3-arylpiperidines having an m- or p-arylhydroxyl were prepared and evaluated for analgesic agonist and antagonist properties. The diastereomeric N-allyl and N-cyclopropylmethyl derivatives behaved as pure potent antagoinists. Substitution of the arylhydroxyl from the meta to the para position resulted in a net fall of the antagoinist activity.
D000698:Analgesia; D000818:Animals; D005283:Fentanyl / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000882:Haplorhini; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D009269:Nalorphine / Q000494:pharmacology*; D009292:Narcotic Antagonists / Q000138:chemical synthesis*; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D012018:Reflex / Q000187:drug effects; D012119:Respiration / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D009292:Narcotic Antagonists; D010880:Piperidines; D009269:Nalorphine; D005283:Fentanyl