| Potentiation of metabotropic GABAB receptors by L-amino acids and dipeptides in rat neocortex. | |
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MedLine Citation:
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PMID: 12742517 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Selected neutral L-alpha-amino acids, and their dipeptides, were reversible, stereospecific, potentiators of GABA(B) receptor-mediated hyperpolarizing responses to baclofen (3-100 microM) in rat neocortical slices. These responses were sensitive to the GABA(B) receptor antagonist (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch50911) (30 microM). Most potent were L-Leu, L-Ile and L-Phe, as were the dipeptides L-Phe-Phe and L-Phe-Leu, and less potent were L-Met, L-Val, L-Cys, L-Cystine, L-Tyr, L-Thr, L-Arg and L-Ser. Inactive were L-Trp, L-His, L-Lys and L-Pro. These potentiators gave leftward shifts of the baclofen concentration-response curves with a Hill slope of 2, and a marked increase in the maximal hyperpolarizing responses. Selected L-amino acids and dipeptides are a class of naturally occurring GABA(B) potentiators, which may be allosteric modulators. |
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Authors:
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David I B Kerr; Jennifer Ong |
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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: European journal of pharmacology Volume: 468 ISSN: 1879-0712 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 2003 May |
Date Detail:
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Created Date: 2003-05-13 Completed Date: 2009-02-27 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: Netherlands |
Other Details:
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Languages: eng Pagination: 103-8 Citation Subset: IM |
Affiliation:
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Department of Anaesthesia and Intensive Care, The University of Adelaide, South Australia, Adelaide, Australia |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Allosteric Regulation
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drug effects Amino Acids / pharmacology* Animals Baclofen / administration & dosage, pharmacology* Dipeptides / pharmacology* Dose-Response Relationship, Drug Drug Synergism GABA Agonists / administration & dosage, pharmacology Male Neocortex / drug effects, metabolism Rats Rats, Sprague-Dawley Receptors, GABA-B / agonists* Stereoisomerism |
| Chemical | |
Reg. No./Substance:
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0/Amino Acids; 0/Dipeptides; 0/GABA Agonists; 0/Receptors, GABA-B; 1134-47-0/Baclofen |
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