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https://hdl.handle.net/2440/5979
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Type: | Journal article |
Title: | Potentiation of metabotropic GABAB receptors by L-amino acids and dipeptides in rat neocortex |
Author: | Kerr, D. Ong, J. |
Citation: | European Journal of Pharmacology, 2003; 468(2):103-108 |
Publisher: | Elsevier Science BV |
Issue Date: | 2003 |
ISSN: | 0014-2999 1879-0712 |
Abstract: | 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. |
Keywords: | Neocortex Animals Rats Rats, Sprague-Dawley Baclofen Amino Acids Dipeptides GABA Agonists Allosteric Regulation Dose-Response Relationship, Drug Drug Synergism Stereoisomerism Male GABA-B Receptor Agonists |
DOI: | 10.1016/S0014-2999(03)01675-3 |
Published version: | http://dx.doi.org/10.1016/s0014-2999(03)01675-3 |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 5 |
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