| Design and structure-activity relationship analysis of ligands of gamma-hydroxybutyric acid receptors. | |
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MedLine Citation:
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PMID: 10869864 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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With the use of [3H]gamma-hydroxybutyric acid, binding experiments allowed the screening of new compounds as ligands of gamma-hydroxybutyric acid receptors. Starting from the acid-alcohol gamma-hydroxybutyric acid structure, structure-activity relation analysis and lead optimization highlighted gamma-hydroxybutyric acid derivatives with significantly increased affinities, when compared with the affinity of gamma-hydroxybutyric acid. Further pharmacological studies with the use of gamma-hydroxybutyric acid derivatives allowed the characterization of the first competitive antagonist acting at gamma-hydroxybutyric acid receptors (NCS 382). |
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Authors:
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J J Bourguignon; M Schmitt; B Didier |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Alcohol (Fayetteville, N.Y.) Volume: 20 ISSN: 0741-8329 ISO Abbreviation: Alcohol Publication Date: 2000 Apr |
Date Detail:
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Created Date: 2000-08-11 Completed Date: 2000-08-11 Revised Date: 2005-11-16 |
Medline Journal Info:
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Nlm Unique ID: 8502311 Medline TA: Alcohol Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 227-36 Citation Subset: IM |
Affiliation:
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Laboratoire de Pharmacochimie de la Communication Cellulaire, ERS 655 du CNRS, Faculté de Pharmacie, 74 route du Rhin, B.P. 21, 67401, Illkirch, France. jjb@pharma.u-strasbg.fr |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Benzocycloheptenes
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chemistry,
metabolism,
pharmacology Drug Design* Humans Hydroxybutyrates / antagonists & inhibitors, chemistry, metabolism Ligands* Molecular Conformation Molecular Structure Receptors, Cell Surface / chemistry, drug effects*, metabolism* Structure-Activity Relationship Tritium |
| Chemical | |
Reg. No./Substance:
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0/4-hydroxybutyric acid receptor; 0/Benzocycloheptenes; 0/Hydroxybutyrates; 0/Ligands; 0/Receptors, Cell Surface; 10028-17-8/Tritium; 131733-92-1/NCS 382; 591-81-1/4-hydroxybutyric acid |
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