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GABAB Receptors
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 sitesExpand
GABA agonists and antagonists
  • D. Kerr, J. Ong
  • Chemistry, Medicine
  • Medicinal research reviews
  • 1 November 1992
Arylalkylamines are a novel class of positive allosteric modulators at GABA(B) receptors in rat neocortex.
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) (1-30Expand
Phaclofen: a peripheral and central baclofen antagonist
Phaclofen, the phosphonic acid derivative of baclofen, reversibly antagonized the depression of the cholinergic twitch response of the guinea pig ileum and distal colon by either baclofen or GABA.Expand
2-Hydroxy-saclofen: an improved antagonist at central and peripheral GABAB receptors
2-hydroxy-saclofen (2-OH-S), a sulphonic analogue of baclofen, slightly increased the twitch height and reversibly antagonised the GABA- and baclofen-induced depression of twitch contractions in theExpand
Antagonism of GABAB‐receptor‐mediated responses in the guinea‐pig isolated ileum and vas deferens by phosphono‐analogues of GABA
1 The phosphono‐analogues of γ‐aminobutyric acid (GABA), 4‐amino‐butylphosphonic acid (4‐ABPA), 3‐amino‐2‐(4‐chlorophenyl)‐propylphosphonic acid (phaclofen) and 3‐amino‐2‐cyclohexylpropylphosphonicExpand
3-amino-2-(4-chlorophenyl)-nitropropane is a new GABAB receptor agonist, more active peripherally.
The activity of the nitropropane analog of baclofen, 3-amino-2-(4-chlorophenyl)-nitropropane (N-BAC), has been examined at central and peripheral GABAB receptors. N-BAC was less potent than baclofenExpand
Characterization of GABAB ligands in vivo.
1. While GABAB antagonists have been examined in vitro, very few have been tested in vivo. A range of GABAB antagonists were tested against baclofen-induced muscle relaxation and hypothermia. 2. TheExpand
Central influences on spinal afferent conduction.
IT HAS BEEN SHOWN that in mammals the small efferent gamma fibers of the ventral root are capable of influencing the activity of muscle spindle afferents (11,12,14,X). More recently, Granit and KaadaExpand
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