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SummaryThe neurotransmitter γ-aminobutyric acid (GABA) activates more than one receptor subtype, including the metabotropic receptor, GABAB. GABAB receptors are located at pre- and postsynaptic sites…
GABA agonists and antagonists
Phaclofen: a peripheral and central baclofen antagonist
2-Hydroxy-saclofen: an improved antagonist at central and peripheral GABAB receptors
Attenuation of morphine withdrawal signs by the GABA(B) receptor agonist baclofen.
Arylalkylamines are a novel class of positive allosteric modulators at GABA(B) receptors in rat neocortex.
3-amino-2-(4-chlorophenyl)-nitropropane is a new GABAB receptor agonist, more active peripherally.
Characterization of GABAB ligands in vivo.
GABAA- and GABAB-receptor-mediated modification of intestinal motility.
Clinical potential of GABAB receptor modulators.
A new class of phenylalkylamines are presented, based on the lead compound fendiline, that are potent positive potentiators of GABAB receptor-mediated function and discussed their putative clinical applications.