Opioid agonist and antagonist effects of configurational stereoisomers of 3-(dimethylamino)-2,2-dimethyl-7-hydroxy-1-tetralol.
The opioid agonist and antagonist effects of two configurational aminotetralin stereoisomers, namely, the cis-(MRSAL) and trans-(RMG) diastereo isomers of 3-(dimethylamino)-2,2-dimethyl-7-hydroxy-1-tetralol were studied using the guinea pig ileum longitudinal muscle preparation. MRSAL demonstrated opioid antagonist activity but failed to show agonist effects. In contrast, RMG showed agonist activity which was partially reversed by NX and MRSAL. RMG also exhibited weak antagonist activity towards DHM, NM and DADLE. These results showed that MRSAL was an opioid antagonist while RMG possessed weak mixed opioid agonist-antagonist activities.
D000818:Animals; D004558:Electric Stimulation; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009281:Naphthalenes / Q000494:pharmacology*; D009292:Narcotic Antagonists / Q000494:pharmacology*; D009294:Narcotics / Q000494:pharmacology*; D013237:Stereoisomerism; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*; D044024:Tetralones
D009281:Naphthalenes; D009292:Narcotic Antagonists; D009294:Narcotics; D013764:Tetrahydronaphthalenes; D044024:Tetralones; C050312:3-dimethylamino-2,2-dimethyl-7-hydroxy-1-tetralol