Comparative study of 1-cyclohexyl-4-(1,2-diphenylethyl)-piperazine and its enantiomorphs on analgesic and othe pharmacological activities in experimental animals.
The analgesic activity of (+/-)-1-cycylohexyl-4-(1,2-diphenylethyl)-piperazine (MT-45) was comparable to that of morphine. The activity of the S(+)-isomer was 1.14 to 1.97 times in mice and 1.00 and 1.23 times in rats as potent as MT-45, and 18.3 to 61.6 times as potent as the R(--)isomer, which was approximately comparable to that of Spa. The hyperglycemic and miotic activities of MT-45 and its S(+)-isomer in rabbits were negligible or very low, though they showed potent morphine-like activites. On the other hand, the R(--)-isomer showed no or very weak effects on those, while Spa showed definite effects. These results suggest that the modes of action of MT-45 and its enantiomorphs are partly different from those of morphine and Spa, and it may be concluded that MT-45 belongs to a new series of compounds having a potent analgesic activity.
D000700:Analgesics; D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D001831:Body Temperature / Q000187:drug effects; D004558:Electric Stimulation; D005769:Gastrointestinal Motility / Q000187:drug effects; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008968:Molecular Conformation; D009020:Morphine / Q000494:pharmacology; D009904:Optical Rotation; D010146:Pain / Q000503:physiopathology; D010627:Phenethylamines / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology* / Q000633:toxicity; D011680:Pupil / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D013237:Stereoisomerism
D000700:Analgesics; D001786:Blood Glucose; D010627:Phenethylamines; D010879:Piperazines; C012631:(+,-)-1-cyclohexyl-4-(1,2-diphenylethyl)piperazine; D009020:Morphine