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|Title:||Potentiation of metabotropic GABAB receptors by L-amino acids and dipeptides in rat neocortex|
|Citation:||European Journal of Pharmacology, 2003; 468(2):103-108|
|Publisher:||Elsevier Science BV|
|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|
|Appears in Collections:||Anaesthesia and Intensive Care publications|
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