Gamma-aminobutyric acid receptor subunit alpha-1

Description:

Description
  • Accession: P14867
  • Swissprot: GBRA1_HUMAN
  • Organism: Homo sapiens
  • Gene: GABRA1
  • Target class: Ion channel

Drug Relations:

acamprosate
The mechanism of action of acamprosate in maintenance of alcohol abstinence is not completely understood. Chronic alcohol exposure is hypothesized to alter the normal balance between neuronal excitation and inhibition. In vitro and in vivo studies in animals have provided evidence to suggest acamprosate may interact with glutamate and GABA neurotransmitter systems centrally, and has led to the hypothesis that acamprosate restores this balance. Bioactivity details MOA
adinazolam
Bioactivity details MOA
alprazolam
A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238) Bioactivity details MOA
butalbital
management of butalbital withdrawal can be simplified by using a phenobarbital-loading protocol; RN given refers to parent cpd Bioactivity details MOA
chlordiazepoxide
An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. Bioactivity details MOA
clobazam
A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY. Bioactivity details MOA
clonazepam
An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses. Bioactivity details MOA
clorazepate
A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. Bioactivity details MOA
desflurane
A fluorinated ether that is used as a volatile anesthetic for maintenance of general anesthesia. Bioactivity details MOA
diazepam
A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. Bioactivity details MOA
estazolam
A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM. Bioactivity details MOA
eszopiclone
A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA. Bioactivity details MOA
ethchlorvynol
A sedative and hypnotic that has been used in the short-term management of INSOMNIA. Its use has been superseded by other drugs. Bioactivity details MOA
etomidate
Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic. Bioactivity details MOA
flumazenil
A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses. Bioactivity details MOA
flunitrazepam
A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug. Bioactivity details MOA
flurazepam
A benzodiazepine derivative used mainly as a hypnotic. Bioactivity details MOA
fospropofol
Bioactivity details MOA
glutethimide
A hypnotic and sedative. Its use has been largely superseded by other drugs. Bioactivity details MOA
halazepam
Bioactivity details MOA
halothane
A nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required. (From AMA Drug Evaluations Annual, 1994, p178) Bioactivity details MOA
isoflurane
A stable, non-explosive inhalation anesthetic, relatively free from significant side effects. Bioactivity details MOA
lorazepam
A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. Bioactivity details MOA
meprobamate
A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) Bioactivity details MOA
metharbital
Bioactivity details MOA
methohexital
An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia. Bioactivity details MOA
methoxyflurane
An inhalation anesthetic. Currently, methoxyflurane is rarely used for surgical, obstetric, or dental anesthesia. If so employed, it should be administered with NITROUS OXIDE to achieve a relatively light level of anesthesia, and a neuromuscular blocking agent given concurrently to obtain the desired degree of muscular relaxation. (From AMA Drug Evaluations Annual, 1994, p180) Bioactivity details MOA
methyprylon
Bioactivity details MOA
midazolam
A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH. Bioactivity details MOA
nitrazepam
A benzodiazepine derivative used as an anticonvulsant and hypnotic. Bioactivity details MOA
oxazepam
A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia. Bioactivity details MOA
pentobarbital
A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236) Bioactivity details MOA
prazepam
A benzodiazepine that is used in the treatment of ANXIETY DISORDERS. Bioactivity details MOA
primidone
A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite. Bioactivity details MOA
propofol
An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS. Bioactivity details MOA
quazepam
Bioactivity details MOA
secbutabarbital
Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital Bioactivity details MOA
secobarbital
A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity. Bioactivity details MOA
sevoflurane
A non-explosive inhalation anesthetic used in the induction and maintenance of general anesthesia. It does not cause respiratory irritation and may also prevent PLATELET AGGREGATION. Bioactivity details MOA
talbutal
Bioactivity details MOA
temazepam
A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. Bioactivity details MOA
thiamylal
A barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. (From Martindale, The Extra Pharmacopoeia, 30th ed, p919) Bioactivity details MOA
thiopental
A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration. Bioactivity details MOA
topiramate
The precise mechanisms by which topiramate exerts its anticonvulsant and migraine prophylaxis effects are unknown; however, preclinical studies have revealed four properties that may contribute to topiramate's efficacy for epilepsy and migraine prophylaxis. Electrophysiological and biochemical evidence suggests that topiramate, at pharmacologically relevant concentrations, blocks voltage-dependent sodium channels, augments the activity of the neurotransmitter gamma-aminobutyrate at some subtypes of the GABA-A receptor, antagonizes the AMPA/kainate subtype of the glutamate receptor, and inhibits the carbonic anhydrase enzyme, particularly isozymes II and IV. Bioactivity details MOA
triazolam
A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Bioactivity details MOA
triclofos
derivative 7 metabolic precursor of trichloroethanol; RN given refers to parent cpd; structure Bioactivity details MOA
zaleplon
an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam Bioactivity details MOA
zolpidem
An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA. Bioactivity details MOA
zopiclone
S(+)-enantiomer of racemic zopiclone; azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; was term of zopiclone 2004-2007 Bioactivity details MOA
alfaxalone
Bioactivity details MOA
amoxapine
The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression. Bioactivity details MOA
baicalin
has iron chelating activity; chemical component of Chinese medicinal herb Huang-chin (Scutellaria baicalensis); do not confuse with baicalein Bioactivity details MOA
brexanolone
Brexanolone is a neuroactive steroid gamma-aminobutyric acid (GABA) A receptor positive modulator indicated for the treatment of postpartum depression (PPD) in adults. Bioactivity details MOA
bromazepam
One of the BENZODIAZEPINES that is used in the treatment of ANXIETY DISORDERS. Bioactivity details MOA
carbamazepine
A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties. Bioactivity details MOA
clomethiazole
A sedative and anticonvulsant often used in the treatment of alcohol withdrawal. Chlormethiazole has also been proposed as a neuroprotective agent. The mechanism of its therapeutic activity is not entirely clear, but it does potentiate GAMMA-AMINOBUTYRIC ACID receptors response and it may also affect glycine receptors. Bioactivity details MOA
delorazepam
Bioactivity details MOA
desalkylflurazepam
Bioactivity details MOA
eltanolone
A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties. Bioactivity details MOA
etizolam
Bioactivity details MOA
hexobarbital
A barbiturate that is effective as a hypnotic and sedative. Bioactivity details MOA
lindane
Any of several polyhalogenated organic compounds consisting of a six-carbon ring with one chlorine and one hydrogen attached to each carbon. Bioactivity details MOA
liothyronine
A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3. Bioactivity details MOA
loprazolam
Bioactivity details MOA
methaqualone
A quinazoline derivative with hypnotic and sedative properties. It has been withdrawn from the market in many countries because of problems with abuse. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604) Bioactivity details MOA
methylphenobarbital
A barbiturate that is metabolized to PHENOBARBITAL. It has been used for similar purposes, especially in EPILEPSY, but there is no evidence mephobarbital offers any advantage over PHENOBARBITAL. Bioactivity details MOA
nordazepam
An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam. Bioactivity details MOA
norfloxacin
A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE. Bioactivity details MOA
phenobarbital
A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations. Bioactivity details MOA
progabide
GABA agonist; structure Bioactivity details MOA
thiocolchicoside
used in combination with glafenine and meprobamate to tranquilize patients undergoing hysterosalpingography; structure Bioactivity details MOA
tubocurarine
A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae. Bioactivity details MOA