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.
GABAB receptor pharmacology.
- N. Bowery
- BiologyAnnual 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.
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…
GABAA and GABAB receptor site distribution in the rat central nervous system
(–)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.
Cortical-area specific block of genetically determined absence seizures by ethosuximide
GABA and glycine as neurotransmitters: a brief history
The realization that glycine receptors are involved in motor reflexes and nociceptive pathways together with the more recent advent of drugs that exhibit some subtype selectivity make the goal of designing selective therapeutic ligands for the glycine receptor that much closer.
GABAB receptor: a site of therapeutic benefit.
- N. Bowery
- Biology, PsychologyCurrent opinion in pharmacology (Print)
- 1 February 2006
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.
gamma-aminobutyric acid(B) receptors: first of the functional metabotropic heterodimers.
Besides being the first example of a functional heterodiameric metabotropic receptor, the components and molecular configuration of the GABA(B) receptor suggest novel mechanisms for producing pharmacologically distinct subtypes of G protein-coupled receptors.