| New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. | |
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MedLine Citation:
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PMID: 7392039 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Schiff bases of gamma-aminobutyric acid (gammaAbu) and gamma-aminobutyramide (gammaAbuNH2) were prepared and tested for anticonvulsant and gammaAbu mimetic activity. 4-[[(4-Chlorophenyl)(5-fluoro-2-hydroxyphenyl)methylene]amino]butanoic acid monosodium salt (4) and 4-[[(4-chlorophenyl)(5-fluoro-2-hydroxyphenyl)methylene]amino]butanamide (5) blocked bicuculline-induced lethality and convulsions and displaced [3H]gammaAbu from its membrane binding sites. In the rat dorsal root sensory ganglion, compound 4 exhibited gammaAbu agonist properties. Compounds 4 and 5 are thus anticonvulsants and directly acting gammaAbu mimetics. |
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Authors:
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J P Kaplan; B M Raizon; M Desarmenien; P Feltz; P M Headley; P Worms; K G Lloyd; G Bartholini |
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Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 23 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 1980 Jun |
Date Detail:
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Created Date: 1980-09-26 Completed Date: 1980-09-26 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 702-4 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* Bicuculline / antagonists & inhibitors Brain / metabolism Cerebellum / metabolism Dose-Response Relationship, Drug Ganglia, Spinal / drug effects Humans Lethal Dose 50 Male Mice Rats Schiff Bases / chemical synthesis, pharmacology gamma-Aminobutyric Acid / analogs & derivatives*, chemical synthesis, metabolism, pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Anticonvulsants; 0/Schiff Bases; 485-49-4/Bicuculline; 56-12-2/gamma-Aminobutyric Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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