PURPOSE The cornea has an important role in vision, is highly innervated and many neurotransmitter receptors are present, e.g., muscarine, melatonin, and dopamine receptors. γ-aminobutyric acid (GABA) is the most important inhibitory neurotransmitter in the retina and central nervous system, but it is unknown whether GABA receptors are present in cornea. The aim of this study was to determine i...

GABA(C) receptors belong to the nicotinicoid superfamily of ionotropic receptors that include nicotinic acetylcholine receptors, bicuculline-sensitive GABA(A) receptors, strychnine-sensitive glycine receptors and 5HT3 serotonin receptors. The GABA(C) receptor concept arose from medicinal chemical studies of a conformationally restricted analog of GABA. Receptors matching the predicted propertie...

Amiloride, a diuretic used in the treatment of hypertension and congestive heart failure, and 2-guanidine-4-methylquinazoline (GMQ) are guanidine compounds that modulate acid-sensing ion channels. Both compounds have demonstrated affinity for a variety of membrane proteins, including members of the Cys-loop family of ligand-gated ion channels, such as the heteromeric GABA-A αβγ receptors. The a...

Amiloride, a diuretic used in the treatment of hypertension and congestive heart failure, and 2-guanidine-4-methylquinazoline (GMQ) are guanidine compounds that modulate acid-sensing ion channels. Both compounds have demonstrated affinity for a variety of membrane proteins, including members of the Cysloop family of ligand-gated ion channels, such as the heteromeric GABA-A abg receptors. The ac...

The G-protein-coupled receptor (GPCR) activated by the neurotransmitter GABA is made up of two subunits, GABA(B1) and GABA(B2). GABA(B1) binds agonists, whereas GABA(B2) is required for trafficking GABA(B1) to the cell surface, increasing agonist affinity to GABA(B1), and activating associated G proteins. These subunits each comprise two domains, a Venus flytrap domain (VFT) and a heptahelical ...

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...

The bed nucleus of the stria terminalis (BST) is known to contain estrogen (E)- concentrating neurons. In addition, injections of E into BST have been reported to potentiate the sympathoinhibitory arterial pressure (AP) and heart rate (HR) responses elicited by glutamate (Glu) stimulation. In this study, the effect of GABA-A antagonist receptors, bicuculline methiodide (BMI), in the rostral ven...

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...

The cloned cDNAs encoding the alpha 1 and beta 1 subunits of the bovine brain GABA(A) receptor have been co-transfected, using a dexamethasone-inducible promoter, into cultured hamster ovary cells, with selection to form a stable cell line. The use, alternatively, of a much stronger constitutive promoter led to cell death consequent upon high receptor density. After induction, the cells contain...

The interactions of dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEAS) were investigated with various binding sites of the gamma-aminobutyric acid (GABA(A)) receptor complex to rat brain membranes, and on GABA-induced [36Cl-] influx in mammalian cortical cultured neurons. DHEAS and DHEA did not affect the binding of [3H]flunitrazepam to the benzodiazepine binding sites. In...