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 ...

GABA(C) receptors are the least studied of the three major classes of GABA receptors. The physiological roles of GABA(C) receptors are still being unravelled and the pharmacology of these receptors is being developed. A range of agents has been described that act on GABA(C) receptors with varying degrees of specificity as agonists, partial agonists, antagonists and allosteric modulators. Pharma...

The neutral amino acid gamma-aminobutyric acid (GABA) produced membrane hyperpolarization and increased membrane chloride ion conductance of spinal cord (SC) and cortical (CTX) neurons in cell culture. GABA dose-response curves were obtained for SC neurons by pressure applying known concentrations of GABA from micropipettes with large tips (miniperfusion pipettes). GABA response threshold was a...

Characteristics of ionotropic gamma-aminobutyric acid (GABA) receptors at bullfrog cone terminals were studied by patch clamp techniques in isolated cell and retinal slice preparations. GABA-induced inward currents from isolated cones reversed in polarity at a potential, very close to the chloride equilibrium potential, and they were completely suppressed by picrotoxin. Unexpectedly, the GABA c...

GABA (gamma-aminobutyric acid) is the primary inhibitory neurotransmitter in brain. The fast inhibitory effect of GABA is mediated through the GABA(A) receptor, a postsynaptic ligand-gated chloride channel. We propose that GABA can act as a ligand chaperone in the early secretory pathway to facilitate GABA(A) receptor cell surface expression. Forty-two hours of GABA treatment increased the surf...

GABA is the principal inhibitory neurotransmitter in the CNS and acts via GABA(A) and GABA(B) receptors. Recently, a novel form of GABA(A) receptor-mediated inhibition, termed "tonic" inhibition, has been described. Whereas synaptic GABA(A) receptors underlie classical "phasic" GABA(A) receptor-mediated inhibition (inhibitory postsynaptic currents), tonic GABA(A) receptor-mediated inhibition re...

[(3)H]Gamma-aminobutyric acid (GABA) binds to synaptic membrane fractions of rat brain in a selective fashion representing an interaction with postsynaptic GABA receptors. Inhibition of [(3)H]GABA binding by a variety of amino acids closely parallels their ability to mimic the synaptic inhibitory actions of GABA and does not correlate with their relative affinity for the presynaptic synaptosoma...

gamma-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the mammalian central nervous system and exerts its actions via both ionotropic (GABA(A)/GABA(C)) and metabotropic (GABA(B)) receptors (R). In addition to their location on neurons, GABA and functional GABA(B) receptors have been detected in nonneuronal cells in peripheral tissue. Although the GABA(B)R has been shown to ...

In the mammalian central nervous system, slow inhibitory neurotransmission is largely mediated by metabotropic GABA(B) receptors (where GABA stands for gamma-aminobutyric acid), which belong to the G-protein-coupled receptor gene family. Functional GABA(B) receptors are assembled from two subunits GABA(B1) (GABA(B) receptor subtype 1) and GABA(B2). For the GABA(B1) subunit, which binds the neur...