| Nipecotic acid directly activates GABA(A)-like ion channels. | |
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MedLine Citation:
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PMID: 11429391 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The GABA-related compound nipecotic acid is commonly used to inhibit GABA uptake. This report shows that nipecotic acid can also directly activate GABA(A)-like chloride channels. When applied to outside-out patches of paraventricular neurones, nipecotic acid (1 mM) activated inward unitary currents (approximately 3 pA at a holding potential of -60 mV, E(Cl)+44 mV). The EC(50) for ion channel activation was approximately 300 microM, 3 fold greater than that found for GABA itself in this preparation. The nipecotic acid activated channels had similar conductance and kinetic properties to those of GABA activated channels in the same patches, reversed near E(Cl) and were inhibited by bicuculline (3 microM). This study indicates that for experiments in which relatively high concentrations of nipecotic acid are used, possible direct GABA(A) receptor agonist properties should be considered. |
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Authors:
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R Barrett-Jolley |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: British journal of pharmacology Volume: 133 ISSN: 0007-1188 ISO Abbreviation: Br. J. Pharmacol. Publication Date: 2001 Jul |
Date Detail:
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Created Date: 2001-06-28 Completed Date: 2001-08-09 Revised Date: 2009-11-18 |
Medline Journal Info:
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Nlm Unique ID: 7502536 Medline TA: Br J Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 673-8 Citation Subset: IM |
Affiliation:
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Department of Physiology, The Medical School, University of Birmingham, Edgbaston, Birmingham, B15 2TT. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Bicuculline / pharmacology Chloride Channels / drug effects, physiology Dose-Response Relationship, Drug GABA Agonists / pharmacology GABA Antagonists / pharmacology Ion Channels / drug effects*, physiology Membrane Potentials / drug effects Neurons / drug effects, physiology Nipecotic Acids / pharmacology* Paraventricular Hypothalamic Nucleus / cytology, drug effects, physiology Rats Receptors, GABA-A / drug effects*, physiology gamma-Aminobutyric Acid / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Chloride Channels; 0/GABA Agonists; 0/GABA Antagonists; 0/Ion Channels; 0/Nipecotic Acids; 0/Receptors, GABA-A; 485-49-4/Bicuculline; 498-95-3/nipecotic acid; 56-12-2/gamma-Aminobutyric Acid |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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