| Modifying quinolone antibiotics yields new anxiolytics. | |
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MedLine Citation:
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PMID: 14647497 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Patients taking fluoroquinolone antibiotics such as norfloxacin exhibit a low incidence of convulsions and anxiety. These side effects probably result from antagonism of the neurotransmitter gamma-aminobutyric acid (GABA) at the brain GABA(A) receptor complex (GRC). Modification of norfloxacin yields molecules such as compound 4 that potentiate GABA action with alpha(2) subunit selectivity. Compound 4 is anxiolytic but does not cause sedation, and may represent a new class of ligands that have anxiolytic activity without sedative liability. |
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Authors:
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Timothy B C Johnstone; Derk J Hogenkamp; Leanne Coyne; Jiping Su; Robert F Halliwell; Minhtam B Tran; Ryan F Yoshimura; Wen-Yen Li; Jeff Wang; Kelvin W Gee |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S. Date: 2003-11-30 |
Journal Detail:
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Title: Nature medicine Volume: 10 ISSN: 1078-8956 ISO Abbreviation: Nat. Med. Publication Date: 2004 Jan |
Date Detail:
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Created Date: 2004-01-02 Completed Date: 2004-04-09 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 9502015 Medline TA: Nat Med Country: United States |
Other Details:
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Languages: eng Pagination: 31-2 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, College of Medicine, University of California, Irvine, California 92697, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Anti-Anxiety Agents
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chemistry,
metabolism,
pharmacology* Anti-Infective Agents / chemistry, metabolism, pharmacology* Fluoroquinolones / chemistry, metabolism, pharmacology* Humans Protein Binding Receptors, GABA-A / metabolism Recombinant Proteins / metabolism gamma-Aminobutyric Acid / metabolism |
| Grant Support | |
ID/Acronym/Agency:
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MH60527/MH/NIMH NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Anti-Anxiety Agents; 0/Anti-Infective Agents; 0/Fluoroquinolones; 0/Receptors, GABA-A; 0/Recombinant Proteins; 56-12-2/gamma-Aminobutyric Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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