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Type: Journal article
Title: Arylalkylamines are a novel class of positive allosteric modulators at GABAB receptors in rat neocortex
Author: Kerr, D.
Ong, J.
Puspawati, N.
Prager, R.
Citation: European Journal of Pharmacology, 2002; 451(1):69-77
Publisher: Elsevier Science BV
Issue Date: 2002
ISSN: 0014-2999
Abstract: Using grease-gap recording from rat neocortical slices, the gamma-aminobutyric acid(B) (GABA(B)) receptor agonists baclofen (3-100 microM) and SKF 97541 (3-aminopropyl-methylphosphinic acid) (1-30 microM) elicited reversible and concentration-dependent hyperpolarizing responses, with EC(50) values of 10 and 3 microM, respectively. The hyperpolarizations were antagonised by the GABA(B) receptor antagonist Sch 50911 ((+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid) (1, 5 and 10 microM). Fendiline (N-[3,3-diphenylpropyl)-alpha-methylbenzylamine) (5-50 microM) and its congeners, prenylamine (N-[3,3-diphenylpropyl)-alpha-methylphenylethylamine) (10-100 microM) and F551 (N-[3,3-diphenylpropyl)-alpha-methyl-3-methoxybenzylamine) (1-30 microM) reversibly enhanced hyperpolarizing responses to the agonists; such effects were reduced by Sch 50911. These arylalkylamines produced leftward shifts of the concentration-response curves, with a marked increase in the maximal hyperpolarization obtained, compared with the agonists alone, F551 being the most potent. These findings suggest that these arylalkylamines represent a new class of positive modulators of GABA(B) receptor-mediated function.
Keywords: Neocortex; Animals; Rats; Rats, Sprague-Dawley; Fendiline; Prenylamine; Baclofen; Drug Synergism; Male; GABA-B Receptor Agonists
RMID: 0020020108
DOI: 10.1016/s0014-2999(02)02195-7
Appears in Collections:Anaesthesia and Intensive Care publications

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