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The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonists
The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonists
- Source :
- European journal of pharmacology. 264(2)
- Publication Year :
- 1994
-
Abstract
- N-Methyl-D-aspartate- (NMDA-) evoked [3H]acetylcholine release in rabbit caudate nucleus slices was inhibited by the antiparkinsonian drugs budipine (1-tert-butyl-4,4-diphenylpiperidine) and biperiden (1-bicyclo[2.2.1.]hept-5-en-2-yl-1-phenyl-3-piperidino propanol) yielding functional Ki values of 4.6 and 8.8 microM. In contrast to the competitive antagonist 2-amino-5-phosphonopentaonate, budipine and biperidene significantly reduced both the apparent KD and the Emax value of NMDA. Moreover, they displaced [3H]MK-801 specifically bound to membranes of the same tissue, although with low affinity (IC50: 38 and 92 microM). It is concluded that budipine and biperiden are use-dependent (uncompetitive) antagonists at the NMDA receptor, binding to the receptor-linked ion channel, but probably not to the MK-801 binding site. NMDA antagonism may contribute to the antiparkinsonian effects of budipine.
- Subjects :
- Caudate nucleus
Budipine
Pharmacology
In Vitro Techniques
Binding, Competitive
Receptors, N-Methyl-D-Aspartate
Biperiden
Antiparkinson Agents
Piperidines
medicine
Animals
Chemistry
Antagonist
Acetylcholine
Mechanism of action
Competitive antagonist
NMDA receptor
Rabbits
medicine.symptom
Caudate Nucleus
Dizocilpine Maleate
Software
medicine.drug
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 264
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- European journal of pharmacology
- Accession number :
- edsair.doi.dedup.....13500684a43f5c53c7ec2650db1b2f42