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Type: Journal article
Title: 3-Chloro,4-methoxyfendiline is a potent GABAB receptor potentiator in rat neocortical slices
Author: Ong, J.
Parker, D.
Marino, V.
Kerr, D.
Puspawati, N.
Prager, R.
Citation: European Journal of Pharmacology, 2005; 507(1-3):35-42
Publisher: Elsevier Science BV
Issue Date: 2005
ISSN: 0014-2999
Abstract: Using grease-gap recording from rat neocortical slices, the GABA(B) receptor agonist baclofen elicited reversible and concentration-dependent hyperpolarizing responses (EC50=18+/-2.3 microM). The hyperpolarizations were antagonised by the GABA(B) receptor antagonist Sch 50911 [(+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid). (+)-N-1-(3-chloro-4-methoxyphenyl)ethyl-3,3-diphenylpropylamine (3-chloro,4-methoxyfendiline; 3-Cl,4-MeO-fendiline) reversibly potentiated baclofen-induced hyperpolarizing responses, which were reduced by Sch 50911, producing leftward shifts of the baclofen concentration-response curves, with a marked increase in the maximal hyperpolarization (EC50=2+/-0.5 microM). In slices preincubated with either [3H]GABA or [3H]glutamic acid, 3-Cl,4-MeO-fendiline (1 microM) potentiated the inhibitory effect of baclofen (2 microM) on the electrically evoked release of [3H]GABA and had a similar effect on the release of [3H]glutamic acid at a concentration of 0.5 microM, without affecting the basal release. These effects were blocked by Sch 50911 (10 microM). Our findings suggest that 3-Cl,4-MeO-fendiline is a potent potentiator of pre- and postsynaptic GABA(B) receptor-mediated functions.
Keywords: Neocortex
Pre- and postsynaptic GABAB receptor
DOI: 10.1016/j.ejphar.2004.11.029
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