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*  Gamma-aminobutyric acid receptor subunit alpha-1
2003). "Coupling of agonist binding to channel gating in the GABA(A) receptor". Nature. 421 (6920): 272-5. doi:10.1038/ ... GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated ... At least 16 distinct subunits of GABA-A receptors have been identified. The GABRA1 receptor is the specific target of the z- ... Sarto I, Wabnegger L, Dögl E, Sieghart W (2002). "Homologous sites of GABA(A) receptor alpha(1), beta(3) and gamma(2) subunits ...
*  GABA receptor agonist
A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative ... Alcohol is an indirect GABA agonist. GABA is the major inhibitory neurotransmitter in the brain, and GABA-like drugs are used ... The two receptors GABA-α and GABA-ρ are ion channels that signal chloride and diminish further action potentials. The GABA-β ... Alcohol is believed to mimic GABA's effect in the brain, binding to GABA receptors and inhibiting neuronal signaling. GABA ...
*  N4-Chloroacetylcytosine arabinoside
... is a GABA agonist.[dubious - discuss] Li, S; Zhang, Y; Liu, H; Yan, Y; Li, Y (2008). " ...
*  Diazepam
Chweh AY, Swinyard EA, Wolf HH, Kupferberg HJ (February 25, 1985). "Effect of GABA agonists on the neurotoxicity and ... "Effects of some anticonvulsant drugs on brain GABA level and GAD and GABA-T activities". Neurochemical Research. 9 (2): 225-31 ... Because it acts on the GABA receptor, the herb valerian may produce an adverse effect. Foods that acidify the urine can lead to ... Diazepam has no effect on GABA levels and no effect on glutamate decarboxylase activity, but has a slight effect on gamma- ...
*  Chlordiazepoxide
Chweh AY; Swinyard EA; Wolf HH; Kupferberg HJ (February 25, 1985). "Effect of GABA agonists on the neurotoxicity and ... It was later found that scopolamine impairment in learning was caused by an increase in benzodiazapine/GABA activity (and that ... May 6, 1983). "Enhancement of GABA binding by benzodiazepines and related anxiolytics". Eur J Pharmacol. 89 (3-4): 193-8. doi: ... part of the GABAA receptor/ion-channel complex and this results in an increased binding of the inhibitory neurotransmitter GABA ...
*  Picamilon
"Technical Description of Picamilon". Shephard RA (Jun 1987). "Behavioral effects of GABA agonists in relation to anxiety and ... GABA) and nicotinoyl-GABA as pro-drugs of GABA". Chemical & Pharmaceutical Bulletin. 32 (10): 4089-95. doi:10.1248/cpb.32.4089 ... The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response. The second released ... It was developed in the Soviet Union in 1969 and further studied in both Russia and Japan as a prodrug of GABA. In Russia, ...
*  Psychoactive drug
To induce unconsciousness, anesthetics affect the GABA and NMDA systems. For example, propofol is a GABA agonist, and ketamine ... Li X, Pearce RA; Pearce (2000). "Effects of halothane on GABA(A) receptor kinetics: evidence for slowed agonist unbinding". The ... Drugs that increase activity in particular neurotransmitter systems are called agonists. They act by increasing the synthesis ... also known as opioid receptor agonists. This class of drugs can be highly addictive, and includes opiate narcotics, like ...
*  Homotaurine
... has been reported as a GABA antagonist as well as a GABA agonist. In vitro studies have found that homotaurine is a ... becoming an antagonist and a displacing full agonist of GABA or baclofen at this receptor. In a study in rats, homotaurine ... 1998). "GABA(B) receptors and opioid mechanisms involved in homotaurine-induced analgesia". Gen. Pharmacol. 30: 411-5. doi: ... Page 308 Reyes-Haro D1, Cabrera-Ruíz E, Estrada-Mondragón A, Miledi R, Martínez-Torres A. (2014). "Modulation of GABA-A ...
*  Etizolam
Cases of intentional suicide by overdose using etizolam in combination with GABA agonists have been reported. Although etizolam ... Flumazenil, a GABA antagonist agent used to reverse benzodiazepine overdoses, inhibits the effect of etizolam as well as ... Etizolam acts as a full agonist at the benzodiazepine receptor to produce its range of therapeutic and adverse effects. ... "Effects of benzodiazepines and non-benzodiazepine compounds on the GABA-induced response in frog isolated sensory neurones". Br ...
*  Ventral tegmental area
Temporary inactivation of CA3 via GABA agonists prevented context induced reinstatement of lever pressing for intravenous ... The tVTA was initially described in rats as a bilateral cluster of GABA neurons within the posterior VTA, dorsolateral to the ... Barrot M, Sesack SR, Georges F, Pistis M, Hong S, Jhou TC (October 2012). "Braking dopamine systems: a new GABA master ... The tVTA/RMTg sends dense GABA projections to VTA and substantia nigra neurons. ... Indeed, tVTA/RMTg cells express high levels ...
*  General anaesthesia
Halothane has been found to be a GABA agonist, and ketamine is an NMDA receptor antagonist. Prior to a planned procedure, the ... "Effects of halothane on GABA(A) receptor kinetics: evidence for slowed agonist unbinding". J. Neurosci. 20 (3): 899-907. PMID ... One commonly used premedication is clonidine, an alpha-2 adrenergic agonist. Clonidine premedication reduces the need for ... Potential pharmacologic targets of general anaesthetics are GABA, glutamate receptors, voltage-gated ion channels, and glycine ...
*  Paroxysmal sympathetic hyperactivity
Baclofen is a GABA agonist that helps control muscle spasms, proving to be helpful in treating dystonia. Benzodiazepines bind ... Bromocriptine is a dopamine agonist that helps lower blood pressure. Its effects are modest, but they are not well understood. ... Clonidine is an alpha receptor agonist that helps reduces sympathetic activity leaving the hypothalamus and reduces circulating ... Other drugs that have been used and have in some cases been helpful are dopamine agonists, other various opiates, ...
*  Clobazam
... is a GABA-A receptor agonist action and may affect sodium channels and voltage-sensitive calcium channels. Like other ... GABA Receptor Agonists". Drugs and Diseases. Medccape. Retrieved 10 July 2005. Ralvenius WT, Acuña MA, Benke D, Matthey A, ... It was also reported that these effects were inhibited by the GABA antagonist flumazenil, and that clobazam acts more ... 2000). "Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype". Nature ...
*  Progabide
Via conversion into GABA, progabide behaves as an agonist of the GABAA, GABAB, and GABAA-ρ receptors. Progabide is approved in ... "GABA receptor agonists and extrapyramidal motor function: therapeutic implications for Parkinson's disease." Advances in ... "The potential use of GABA agonists in psychiatric disorders: evidence from studies with progabide in animal models and clinical ... "Gamma-aminobutyric acid agonists for neuroleptic-induced tardive dyskinesia". The Cochrane Database of Systematic Reviews (4): ...
*  GABA receptor
GABA agonist GABA antagonist Kuffler SW, Edwards C (November 1958). "Mechanism of gamma aminobutyric acid (GABA) action and its ... This mechanism is responsible for the sedative effects of GABAA allosteric agonists. In addition, activation of GABA receptors ... Although the term "GABAС receptor" is frequently used, GABAС may be viewed as a variant within the GABAA receptor family. ... The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief ...
*  Absence seizure
In particular, the GABA agonists vigabatrin and tiagabine are used to induce, not to treat, absence seizures and absence status ...
*  Bamaluzole
... is a GABA receptor agonist. It was patented as an anticonvulsant by Merck but was never marketed. Imidazopyridine ...
*  Ligand-gated ion channel
Ligands: Agonists: GABA, muscimol, progabide, gaboxadol Antagonists: bicuculine, gabazine Partial agonist: piperidine-4- ... 2014). "Baclofen, a GABA B Agonist, reduces risk-taking and reveals the relationship between brain responses to drug cues and ... Ligands: Agonists: GABA, Baclofen, gamma-Hydroxybutyrate, Phenibut etc. Positive Allosteric Modulators: CGP-7930, Fendiline, ... Primary endogenous co-agonists: glutamate and either D-serine or glycine Other agonists : aminocyclopropanecarboxylic acid; D- ...
*  Neuropsychopharmacology
The plausible cause of HPPD is damage to the inhibitory GABA circuit in the visual pathway (GABA agonists such as midazolam can ... and GABA agonist tranquilizers (benzodiazepines). New endogenous chemicals are continually identified. Specific receptors have ... GABA-ergic neurons from the SCN inhibit the paraventricular nucleus, which signals the superior cervical ganglion (SCG) through ... For the six more important neurotransmitters Glu, GABA, Ach, NE, DA, and 5HT (listed at neurotransmitter) there are at least 29 ...
*  GABAA receptor
Orthosteric agonists: GABA, gaboxadol, isoguvacine, muscimol, progabide, piperidine-4-sulfonic acid (partial agonist). ... selective inverse agonist for α5 subtype) SL-651,498 (full agonist at α2 and α3 subtypes, and as a partial agonist at α1 and α5 ... highly α1-selective agonist) bretazenil (subtype-selective partial agonist) imidazenil and L-838,417 (both partial agonists at ... Orthosteric agonists and antagonists: bind to the main receptor site (the site where GABA normally binds, also referred to as ...
*  Gamma-Amino-beta-hydroxybutyric acid
GABOB is a GABA receptor agonist. It has two stereoisomers, and shows stereoselectivity in its actions. Specifically, (R)-(-)- ... GABOB, or β-hydroxy-GABA, is a close structural analogue of GABA (see GABA analogue), as well as of γ-hydroxybutyric acid (GHB ... phenibut (β-phenyl-GABA), baclofen (β-(4-chlorophenyl)-GABA), and pregabalin (β-isobutyl-GABA). GABOB has been referred to by ... It is a GABA analogue, or an analogue of the neurotransmitter γ-aminobutyric acid (GABA), and has been found to be an ...
*  Rostral ventromedial medulla
... the GABA A agonist muscimol was tested in conjuncture with SP. Intrathecal muscimol significantly enhanced SP-induced ... On-cells displayed a greater response to P2X agonists vs P2Y agonists. For example, α,β-methylene ATP, a P2X agonist, activated ... Off-cells were also activated by UTP, but lacked any response to adenosine, a P1 agonist. Activation of off-cells by ATP was ... All on-cells showed a response to the non-specific P2 agonist uridine triphosphate (UTP). Activation of on cells by ATP was ...
*  BL-1020
... it's an ester of GABA and perphenazine, and pharmacologically it acts as a D2 antagonist and GABA agonist. It has shown pro- ...
*  Alfaxalone
... near the actual GABA binding site) and acts as a GABA agonist, similar to benzodiazepines. Alfaxalone, however, does not share ... Alfaxalone works as a positive allosteric modulator on GABAA receptors and, at high concentrations, as a direct agonist of the ...
*  Nucleus accumbens
GABA: A recent study on rats that used GABA agonists and antagonists indicated that GABAA receptors in the NAc shell have ... GABA is one of the main neurotransmitters in the NAcc, and GABA receptors are also abundant. These neurons are also the main ... GABA is one of the main neurotransmitters in the NAcc, and GABA receptors are also abundant. Function: The nucleus accumbens ... Barrot, M.; Sesack, S. R.; Georges, F.; Pistis, M.; Hong, S.; Jhou, T. C. (2012). "Braking Dopamine Systems: A New GABA Master ...
*  List of investigational anxiolytics
... mGluR2 and mGluR3 agonist [13] Tianeptine oxalate (TNX-601) - atypical μ-opioid receptor agonist [14] Verucerfont (GSK-561679, ... "GABA modulator" / undefined mechanism of action[22] JNJ-42165279 - FAAH inhibitor[23] MP-20X - CB1 and 5-HT1A receptor ... Agomelatine (AGO-178; Valdoxan) - melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist[1] Riluzole sublingual ( ... 5-HT1A receptor agonist, 5-HT2A receptor antagonist [4] Vilazodone (EMD-68843, SB-659746A; Viibryd) - 5-HT1A receptor partial ...
*  Median preoptic nucleus
... as demonstrated by increased time in NREM sleep in response to microinjections of GABA agonists into the median preoptic area ... The amount of time spent in NREM sleep increases with the number of activated GABA receptors in the median preoptic area, ... GABA, in wakefulness areas of the brain, such as the tuberomammillary nucleus and the locus coeruleus. This leads to the ...