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Anion-selective Cys-loop receptors (GABARs and GlyRs) provide main inhibitory drive in CNS. Both types of receptors are operating via chloride-selective ion channels, however with different kinetics, pharmacological profiles and localization. Disequilibrium in their function leads to a variety of disorders, which are often treated with allosteric modulators. The few available GABAR and GlyR channel blockers effectively suppress inhibitory currents in neurons, but their systemic administration is highly toxic. Aiming to develop an efficient light-controllable modulator of GABA receptors we constructed Azo-NZ1, which is composed of a nitrazepam moiety merged to an azobenzene photoisomerizable group.
This article was published in the following journal.
Name: British journal of pharmacology
Many synapses, including parallel fiber synapses in the cerebellum, express presynaptic GABA receptors. However, reports of the functional consequences of presynaptic GABA receptor activation are vari...
The stream of visual information sent from photoreceptors to second-order bipolar cells is intercepted by laterally interacting horizontal cells that generate feedback to optimize and improve the effi...
GABA is the most abundant neurotransmitter in the circadian pacemaker circuits of mammals and insects. In the Madeira cockroach the accessory medulla (AME) in the brain's optic lobes is the circadian ...
γ-aminobutyric acid (GABA) mediates its physiological effects through the GABA and GABA receptors. In this study the putative expression of GABAR and GABAR subunits in human myometrium tissue was inv...
The γ-aminobutyric acid type A (GABA) receptor is an important pentameric inhibitory neurotransmitter receptor, and the γ2 subunit of this receptor plays a key role in potentiation of the GABA respo...
The purpose of this study is to investigate which combination therapy is more effective for improving the blood pressure (BP) and reducing target organ damage in Japanese hypertensive pati...
The antihypertensive effect of the increased dose of angiotensin II receptor blocker (AII antagonist) is compared with that of the additional combined use of amlodipine in hypertensive pat...
Learning Implementation of Guideline-based Decision Support System for Hypertension Treatment: Testing Alternative Antihypertensive Regimens Using ACE-Inhibitors, Calcium Channel Blockers and Diuretics (LIGHT-ACD)
This trial aims to compare the efficacy of several streamlined guideline-based hypertensive medication regimens initiated with Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor ...
The purpose of this study is to compare the blood pressure lowering efficacy of a treatment regimen based on a dihydropyridine calcium-channel blocker combined with an angiotensin II type-...
This pilot study is a feasibility, safety, and preliminary benefits study to look at whether giving the calcium channel blocker amlodipine to people with hereditary pancreatitis as a proph...
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.
Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.
Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.
Neurology - Central Nervous System (CNS)
Alzheimer's Disease Anesthesia Anxiety Disorders Autism Bipolar Disorders Dementia Epilepsy Multiple Sclerosis (MS) Neurology Pain Parkinson's Disease Sleep Disorders Neurology is the branch of me...