1-Pyridyl-3,4-dihydro-beta-carbolines: synthesis and central action.
1-Pyridyl-3,4-dihydro-beta-carbolines (2a-2f) were synthesized by two methods. The central action of these compounds was investigated in mice and rats using behavioral tests. The most active 6-methoxy-1-(3-pyridyl)-3,4-dihydro-beta-carboline (2e) possesses potential antidepressant properties, as it reversed the effects of reserpine (sedation, hypothermia and ptosis), potentiated the stimulation induced by levodopa given jointly with pargyline, and reduced the immobility time in the despair test. Moreover, compound 2e inhibited the spontaneous locomotor activity, evoked tremor and produced an analgesic effect.
D006916:5-Hydroxytryptophan / Q000037:antagonists & inhibitors; D000700:Analgesics / Q000138:chemical synthesis; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D002492:Central Nervous System Depressants / Q000138:chemical synthesis*; D006591:Hexobarbital / Q000494:pharmacology; D007980:Levodopa / Q000494:pharmacology; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D012110:Reserpine / Q000037:antagonists & inhibitors; D014363:Tryptamines / Q000037:antagonists & inhibitors
D000700:Analgesics; D000927:Anticonvulsants; D002243:Carbolines; D002492:Central Nervous System Depressants; D014363:Tryptamines; C030820:tryptamine; D007980:Levodopa; D012110:Reserpine; D006591:Hexobarbital; D006916:5-Hydroxytryptophan