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International Union of Pharmacology. XXXIII. Mammalian γ-Aminobutyric AcidB Receptors: Structure and Function
The emergence of high-affinity antagonists for GABAB receptors has enabled a synaptic role to be established, however, the antagonists have generally failed to establish the existence of pharmacologically distinct receptor types within the GABAB receptor class. Expand
GABAB receptor pharmacology.
- N. Bowery
- Annual review of pharmacology and toxicology
The discovery that GABAB antagonism can suppress absence seizures in rats has provided an important therapeutic target and the emergence of brain-penetrating GABAB antagonists being discovered makes future studies an exciting prospect. Expand
International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function.
The gamma-aminobutyric acid(B) (GABA(B)) receptor was first demonstrated on presynaptic terminals where it serves as an autoreceptor and also as a heteroreceptor to influence transmitter release by… Expand
GABAA and GABAB receptor site distribution in the rat central nervous system
An autoradiographic procedure has been used to determine the quantitative distributions of gamma-aminobutyric acid (GABAA and GABAB) receptor subtypes in rat brain. Although the concentrations of… Expand
(–)Baclofen decreases neurotransmitter release in the mammalian CNS by an action at a novel GABA receptor
GABA clearly decreased the evoked release of accumulated 3H-noradrenaline from rat atria in vitro and3H-acetylcholine from preganglionic terminals in the rat superior cervical ganglion in vitro without affecting the basal release of tritium. Expand
Cortical-area specific block of genetically determined absence seizures by ethosuximide
- Jon-Paul A Manning, D. Richards, N. Leresche, V. Crunelli, N. Bowery
- Medicine, Psychology
- 31 December 2004
The data suggest that the ability of ETX to abolish genetically determined absence seizures is cortical-area specific and support the involvement of S1po in the initiation of SWDs. Expand
GABAB receptor: a site of therapeutic benefit.
- N. Bowery
- Biology, Medicine
- Current opinion in pharmacology
- 1 February 2006
Evidence from preclinical studies suggests that antagonism of the GABAB receptor produces beneficial clinical effects, and activation of this receptor can produce numerous effects that might be amenable to drug development. Expand
3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain
It is reported that high-affinity saturable binding of 3H-baclof en and3H-G AB A to the GABAB site can be detected in fragments of crude synaptic membranes prepared from rat brain and that GABA and baclofen can compete for the same recognition site. Expand
GABAB receptors: drugs meet clones
The long-awaited cloning of the GABAB receptors, the last of the major known neurotransmitter receptors to be identified, has been reported and advances in discerning the specific coupling partners in the brain are being made. Expand
GABA and its receptors in the spinal cord.
The current status of GABA in relation to nociception and skeletal muscle tone is reviewed, and it is indicated that its contribution to spinal cord function should not be overlooked. Expand