Literature DB >> 7199925

[Summarizing description of the pharmacology of budipine, a new 4,4-diphenylpiperidine derivative used in Parkinson therapy (author's transl)].

H G Menge, U Brand.   

Abstract

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.

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Year:  1982        PMID: 7199925

Source DB:  PubMed          Journal:  Arzneimittelforschung        ISSN: 0004-4172


  4 in total

1.  Drug binding to aromatic residues in the HERG channel pore cavity as possible explanation for acquired Long QT syndrome by antiparkinsonian drug budipine.

Authors:  Eberhard P Scholz; Edgar Zitron; Claudia Kiesecker; Sonja Lueck; Sven Kathöfer; Dierk Thomas; Slawomir Weretka; Simon Peth; Volker A W Kreye; Wolfgang Schoels; Hugo A Katus; Johann Kiehn; Christoph A Karle
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2003-10-14       Impact factor: 3.000

2.  The interaction of 1-alkyl-4,4-diphenylpiperidines with the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine receptor binding site.

Authors:  H Russ; U Pindur; H Przuntek
Journal:  J Neural Transm       Date:  1986       Impact factor: 3.575

3.  Adjuvant treatment of Parksinson's disease with budipine: a double-blind trial versus placebo.

Authors:  K Jellinger; H Bliesath
Journal:  J Neurol       Date:  1987-06       Impact factor: 4.849

4.  Intracerebroventricular administration of 1-methyl-4-phenylpyridinium ion in mice: effects of simultaneously administered nomifensine, deprenyl, and 1-t-butyl-4,4-diphenylpiperidine.

Authors:  W Mihatsch; H Russ; H Przuntek
Journal:  J Neural Transm       Date:  1988       Impact factor: 3.575

  4 in total

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