Pharmacological studies on 3-[gamma-(p-fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazino ]1,2-a] quinoline hydrochloride (compound 69/183). Part III: Assessment of tranquillising activity.
The tranquillising activity of 3-[gamma-(p-fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazino [1, 2-a]quinoline hydrochloride (centpyraquin), a new adrenergic neurone blocking antihypertensive agent, has been evaluated in various laboratory animals. The compound has a calming effect in mice, rats, cats and monkeys. In low doses it reduces the spontaneous motor activity followed in progressively higher doses by hypothermia, ptosis and catalepsy and a taming effect in monkeys and cats. It potentiates pentobarbitone-, hexobarbitone- and ethanol-induced sleep and antagonises amphetamine induced toxicity in mice. It, however, fails to antagonise morphine induced mania and hyperactivity in cats. It blocks conditioned avoidance response in rats at a much lower dose (ED50 = 2.73 mg/kg) than the unconditioned response (ED50 = 10,9 mg/kg). In cats centpyraquin increases the voltage and slows the frequency of cortical EEG discharges. Centpyraquin has the profile of activity of a neuroleptic on the central nervous system.
D000661:Amphetamine / Q000037:antagonists & inhibitors; D000818:Animals; D014150:Antipsychotic Agents; D001362:Avoidance Learning / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D002090:Butyrophenones; D004569:Electroencephalography; D005260:Female; D000882:Haplorhini; D008297:Male; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009043:Motor Activity / Q000187:drug effects; D011804:Quinolines / Q000494:pharmacology*; D051381:Rats; D012890:Sleep / Q000187:drug effects; D013997:Time Factors
D014150:Antipsychotic Agents; D002090:Butyrophenones; D011804:Quinolines; D009020:Morphine; D000661:Amphetamine