| An N-protected gamma-aminobutyric acid dipeptide with anticonvulsant action. | |
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MedLine Citation:
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PMID: 6547164 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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N-Pivaloyl-leucyl-gamma-aminobutyric acid (PLG) is a synthetic dipeptide with a partition coefficient of 1.67 in an ethyl acetate/water system that partially inhibits the synaptosomal uptake and activates the release of [U-14C]gamma-aminobutyric acid [( U-14C]GABA). The displacement of GABA from crude synaptic membranes by PLG occurs with an IC50 of 10(-5) M. The compound has the capacity to cross the blood-brain barrier and increase central GABA levels. Its ED50 on cardiazol -induced convulsions is 60-65 mg/kg. PLG is resistant to hydrolysis by chymotrypsin and partially inhibits the proteolytic activity of trypsin. |
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Authors:
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L Galzigna; M Bianchi; A Bertazzon; A Barthez; G Quadro; M A Coletti-Previero |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of neurochemistry Volume: 42 ISSN: 0022-3042 ISO Abbreviation: J. Neurochem. Publication Date: 1984 Jun |
Date Detail:
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Created Date: 1984-07-13 Completed Date: 1984-07-13 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 2985190R Medline TA: J Neurochem Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1762-6 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anticonvulsants / chemical synthesis* Blood-Brain Barrier Brain / metabolism Dipeptides / chemical synthesis* Kinetics Rats Rats, Inbred Strains Seizures Synaptosomes / drug effects, metabolism* gamma-Aminobutyric Acid / metabolism* |
| Chemical | |
Reg. No./Substance:
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0/Anticonvulsants; 0/Dipeptides; 56-12-2/gamma-Aminobutyric Acid; 91147-50-1/N-pivaloylleucyl-gamma-aminobutyric acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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