Gamma-aminobutyric acid (GABA) is an important inhibitory transmitter in central nervous system and is involved in pathophysiology of epilepsy. Pentylenete-trazole (PTZ), a convulsant agent, partly acts via anion channel of GABAA receptor. Ivermectin, an antiparasitic agent and a GABAA agonist, has anticonvulsant effect in animal seizure models. Cholestasis increases ...

In the CNS, gamma-aminobutyric acid (GABA) acts as an inhibitory transmitter via ligand-gated GABA(A) receptor channels and G protein-coupled GABA(B) receptors. Both of these receptor types mediate inhibitory postsynaptic transmission throughout the nervous system. For GABA(A) receptors, this inhibitory action is associated with a hyperpolarization due to an increase in conductance to chloride ...

Inhibition is crucial for normal function in the nervous system. In the CNS, inhibition is mediated primarily by the amino acid GABA via activation of two ionotropic GABA receptors, GABA(A) and GABA(C). GABA(A) receptor composition and function have been well characterized, whereas much less is known about native GABA(C) receptors. Differences in molecular composition, anatomical distributions,...

GABA(B) is a G protein-coupled receptor composed of two subunits, GABA(B1) and GABA(B2). GABA(B1) contains an endoplasmic reticulum-retention sequence and is trafficked to the cell surface only in association with GABA(B2). To determine whether the C-terminus of GABA(B2) regulates GABA(B) trafficking, we constructed forms of GABA(B2) with various C-terminal truncations and examined their surfac...

Kainate (KA) receptor activation depresses stimulus-evoked gamma-aminobutyric acid (GABA-mediated) synaptic transmission onto CA1 pyramidal cells of the hippocampus and simultaneously increases the frequency of spontaneous GABA release through an increase in interneuronal spiking. To determine whether these two effects are independent, we examined the mechanism by which KA receptor activation d...

GABA(A) receptors are the principal sites of fast synaptic inhibition in the brain. These receptors are hetero-pentamers that can be assembled from a number of subunit classes: alpha(1-6), beta(1-3), gamma(1-3), delta(1), epsilon, theta;, and pi, but the majority of receptor subtypes is believed, however, to be composed of alpha, beta, and gamma2 subunits. A major mechanism for modulating GABA(...

The metabotropic GABA receptor (GABA(B)R) regulates calcium influx in neurons. Whole cell voltage-clamp techniques were employed to determine the effects of internal calcium on the activity of GABA(B)Rs. GABA(B)R receptor apparent affinity was maximal when bis-(o-aminophenoxy)-N,N,N',N'-tetraacetic acid (BAPTA) maintained internal calcium below 70 nM. Apparent affinity was reduced as internal c...

UNLABELLED γ-aminobutyric acid (GABA)-A receptor-mediated neural transmission is important to promote practice-dependent plasticity after brain injury. This study investigated alterations in GABA-A receptor binding and functional and anatomic connectivity within the motor cortex in children with cerebral palsy (CP). METHODS We conducted (18)F-fluoroflumazenil PET on children with hemiplegic C...

introduction: in female rats sensitivity to antinociceptive treatment varies during estrous cycle stages. the role of gaba through gabab receptor in nociception has been established. the aim of the present study is to investigate the effect of intercerebroventicular injection of gabab receptor agonist (baclofen) and gabab antagonist (cgp35348) on pain sensitivity during different stages of estr...

INTRODUCTION y-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the mammalian brain. It mediates its effects via the specific interaction with the integral membrane proteins, the GABA receptors. GABA receptors can be classified according to their respective transduction mechanisms following activation, as the GABA and the GABAB receptor respectively. The focus of this review...