[Summarizing description of the pharmacology of budipine, a new 4,4-diphenylpiperidine derivative used in Parkinson therapy (author's transl)].
Budipine is a new 1-tertiary-butyl-diphenylpiperidine derivative with primarily central action. In animal experiments involving different pathological models, a pharmacological profile is found suggesting that budipine has therapeutic potential as antiparkinson drug. Besides a mild centrally stimulatory effect in the unprovoked animal, strong antagonistic effects are observed on tremorine- or N-carbamoyl-2-(2,6-dichlorophenyl)-acetamidine-hydrochloride (LON-954) induced tremor, and on cataleptic states elicited by haloperidol, reserpine, tetrabenazine and perphenazine. Attempts are made to elucidate tha mechanism of action in comparison with conventional clinical anti-parkinson drugs. The anticholinergic activity of budipine is too weak to explain its effectiveness. Direct dopamine receptor stimulation was excluded, but not the release of dopamine or reuptake inhibition. No clear influence was detectable on noradrenergic neurons either peripherally or centrally. An influence of serotoninergic mechanisms by way of reuptake inhibition and release, however, appears feasible. Peripheral effects are minimal. The possible advantages of budipine in the treatment of Parkinson's disease are discussed in comparison to the drugs used in therapy today.
D000818:Animals; D000978:Antiparkinson Agents / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001679:Biogenic Amines / Q000378:metabolism; D002490:Central Nervous System / Q000187:drug effects; D004569:Electroencephalography; D051379:Mice; D010525:Peripheral Nerves / Q000187:drug effects; D010880:Piperidines / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D014202:Tremor / Q000188:drug therapy
D000978:Antiparkinson Agents; D001679:Biogenic Amines; D010880:Piperidines; C026710:budipine
Zusammenfassende Darstellung der Pharmakologie von Budipin, einem neuen 4,4-Diphenylpiperidin-Derivat für die parkinson-Therapie.