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*  Sedative
Yi PL; Tsai CH; Chen YC; Chang FC (March 2007). "Gamma-aminobutyric acid (GABA) receptor mediates suanzaorentang, a traditional ... Alprazolam Clobazam Clorazepate Etizolam Nonbenzodiazepine hypnotics Eszopiclone Zaleplon Zolpidem Zopiclone Orexin antagonists ... In spite of the fact that each sedative acts in its own way, they produce beneficial relaxing effect by increasing GABA ... Advances in pharmacology have permitted more specific targeting of receptors, and greater selectivity of agents, which ...
*  5-HT2B receptor
Metadoxine: a 5ht2b antagonist and GABA-activity modulator SDZ SER-082: a mixed 5-HT2B/C antagonist EGIS-7625: high selectivity ... Moreover, 5-HT2B receptors were recently shown to be overexpressed in human failing heart and antagonists of 5-HT2B receptors ... "The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo". British Journal of ... a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction ...
*  5-HT receptor
"The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors". ... The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / ... 5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand- ... 5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors are found in the central and peripheral nervous systems ...
*  GABA receptor antagonist
GABA receptor antagonists are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant ... GABA antagonists at the US National Library of Medicine Medical Subject Headings (MeSH). ... Examples include bicuculline, securinine and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil. Also ... thujone, ginkgo biloba, kudzu and muira puama[citation needed] may have properties of GABAA receptor antagonism. ...
*  Effects of alcohol on memory
Alcohol Research & Health, 27(2),186-196 Paul, S. (2006). Alcohol-sensitive GABA receptors and alcohol antagonists. Published ... Alcohol acts as a positive allosteric modulator of GABA receptors, specifically type GABAA. Upon activation, these GABA ... Schummers, J.; Browning, M. D. (2001). "Evidence for a role for GABA(A) and NMDA receptors in ethanol inhibition of long-term ... Hodge, C. W.; Cox, A. A. (1998). "The discriminative stimulus effects of ethanol are mediated by NMDA and GABA(A) receptors in ...
*  Pitrazepin
Murphy VF, Wann KT (November 1988). "The action of GABA receptor agonists and antagonists on muscle membrane conductance in ... "Interaction of pitrazepin with the GABA/benzodiazepine receptor complex and with glycine receptors". European Journal of ... Pitrazepin is a competitive GABAA and glycine receptor antagonist. It has been used to study insect and snail nervous systems ... Sattelle DB, Pinnock RD, Wafford KA, David JA (January 1988). "GABA receptors on the cell-body membrane of an identified insect ...
*  Alcohol withdrawal syndrome
"Chronic ethanol produces a decreased sensitivity to the response-disruptive effects of GABA receptor complex antagonists". ... "Changes in GABA(A) receptor gene expression associated with selective alterations in receptor function and pharmacology after ... benzodiazepine receptor agonists and barbiturate receptor agonists) work via a GABAA receptor mechanism and are cross-tolerant ... Furthermore, disrupted GABA benzodiazepine receptor function is part of alcohol dependence and chronic benzodiazepines may ...
*  Picrotoxin
However, due to its antagonist effect on GABA receptors, it has been used as a central nervous system stimulant. It was also ... Other research suggests that the toxin acts instead as a non-competitive antagonist, or inhibitor, for GABA receptors. A study ... Newland, C F; Cull-Candy, S G (February 1992). "On the mechanism of action of picrotoxin on GABA receptor channels in ... Olsen, R. W.; DeLorey, T. M. (1999). "GABA Receptor Physiology and Pharmacology". In Siegel G. J.; Agranoff, B. W.; Albers, R. ...
*  Cicuta
It is a non-competitive gamma-aminobutyric acid (GABA) receptor antagonist. Cicutoxin acts on the GABAA receptor causing a ...
*  Cicutoxin
It is a potent, noncompetitive gamma-aminobutyric acid (GABA) receptor antagonist. In humans, cicutoxin rapidly produces ... Cicutoxin binds to the same place as GABA, because of this the receptor is not activated by GABA. The pore of the receptor ... Cicutoxin is a noncompetitive gamma-aminobytyric acid (GABA) antagonist in the central nervous system (CNS). GABA normally ... Cicutoxin is known to interact with the GABAa receptor and it also has been shown to block the potassium channel in T ...
*  GABAergic
Some different classes of GABAergic drugs include the following: GABA receptor agonists, GABA receptor antagonists, and GABA ... A GABAergic neuron produces GABA. A substance is GABAergic if it produces its effects via interactions with the GABA system, ... GABAergic means "pertaining to or affecting the neurotransmitter GABA". A synapse is GABAergic if it uses GABA as its ... A GABAergic or GABAergic agent is any chemical that modifies the effects of GABA in the body or brain. ...
*  Illicium verum
... which are noncompetitive antagonists of GABA receptors. Swamp star anise Illicium parviflorum a similar tree found in the ...
*  Levorphanol
... also acts as a glycine receptor antagonist and GABA receptor antagonist at very high concentrations. Levorphanol is 6 to 8 ... κ-opioid receptor (KOR), and the nociceptin receptor (NOP), as well as an NMDA receptor antagonist and a serotonin- ... Levorphanol acts predominantly as an agonist of the μ-opioid receptor (MOR), but is also an agonist of the δ-opioid receptor ( ... NMDA receptor antagonist), and weakly active opioid. DXO is an active metabolite of the pharmaceutical drug dextromethorphan ( ...
*  Isopregnanolone
The progesterone metabolite isoallopregnanolone is a subunit-selective antagonist of the GABA-A receptor. Chicago Bäckström T, ... "Treatment of premenstrual dysphoric disorder with the GABAA receptor modulating steroid antagonist Sepranolone (UC1010)-A ... It has been reported to act as a subunit-selective negative allosteric modulator of the GABAA receptor, and antagonizes in ... Isopregnanolone has no hormonal effects and appears to have no effect on the GABAA receptor by itself; it selectively ...
*  GABA receptor
Additional information on GABAB receptors has been reviewed elsewhere. GABA agonist GABA antagonist Kuffler SW, Edwards C ( ... 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 ... GABA receptors influence neural function by coordinating with glutamatergic processes. A subclass of ionotropic GABA receptors ...
*  GABAB receptor
... the first GABA(B) receptor antagonist in clinical trials". Biochemical Pharmacology. 68 (8): 1479-87. doi:10.1016/j.bcp.2004.07 ... GABA receptor GABAA receptor GABAA-ρ receptor Chen K, Li HZ, Ye N, Zhang J, Wang JJ (2005). "Role of GABAB receptors in GABA ... GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) that are linked via G- ... Hyland, NP; Cryan, JF (2010). "A Gut Feeling about GABA: Focus on GABA(B) Receptors". Frontiers in Pharmacology. 1: 124. doi: ...
*  Tetramethylenedisulfotetramine
Its effect is similar to but stronger than picrotoxin, a GABA-A receptor antagonist widely used in research. As one of the most ... may indicate the benefits of benzodiazepine-NMDA receptor antagonist regimens used to treat TMDT exposed patients. Strychnine ... When considering GABAA receptor activity, diazepam and pregnanolone reversed TMDT activity when applied to cell cultures ... Curtis and Johnson were the first to hypothesize TMDT antagonistic behavior on GABA. An in-vitro study using superior cervical ...
*  Serotonin syndrome
Other neurotransmitters may also play a role; NMDA receptor antagonists and GABA have been suggested as affecting the ... Nisijima K, Yoshino T, Yui K, Katoh S (January 2001). "Potent serotonin (5-HT)(2A) receptor antagonists completely prevent the ... Dopamine receptor blockade (NMS) has a slow onset and typically evolves over several days after administration of a neuroleptic ... The 5-HT1A receptor may still contribute through a pharmacodynamic interaction in which increased synaptic concentrations of a ...
*  Levosulpiride
... is a substituted benzamide antipsychotic, reported to be a selective antagonist of dopamine D2 receptor activity ... Sulpiride appears to lack effects on norepinephrine, acetylcholine, serotonin, histamine, or gamma-aminobutyric acid (GABA) ... receptors. Sulpiride is a substituted benzamide derivative and a selective dopamine D2 antagonist with antipsychotic and ... In contrast to most other neuroleptics which block both dopamine D1 and D2 receptors, sulpiride is more selective and acts ...
*  CD90
... receptor antagonists. This suggests that Thy-1 KO mice have excessive GABAergic inhibition in the dentate gyrus and regional ... This failure can be rescued by the transgenic expression of Thy-1 or pharmacologic treatment with a GABA (A) ... "Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic Stem Cells". Science. 329 (5997): 1345-8. ... Acting through several integrins and probably a few yet unknown other receptors Thy-1 mediates adhesion of leukocytes and ...
*  Thujone
... is a GABAA receptor antagonist and more specifically, a GABAA receptor positive allosteric modulator. By inhibiting ... Thujone acts on GABA as an antagonist (opposite to the effects of alcohol) and as a component of several essential oils, is ... Modulation of Ionotropic GABA Receptors by Natural Products of Plant Origin Dettling A, Grass H, Schuff A, Skopp G, Strohbeck- ... These effects are in line with other GABA antagonists. Also, alpha-thujone is metabolized quickly in the liver in mice. ...
*  Gabazine
Behrens, CJ; Van Den Boom, LP; Heinemann, U (2007). "Effects of the GABA(A) receptor antagonists bicuculline and gabazine on ... Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA receptors. It is used in scientific research and has no role ... Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel ... Gabazine has been found to bind to and antagonize α4βδ subunit-containing GABAA receptors, which may represent the GHB receptor ...
*  Benzodiazepine withdrawal syndrome
GABA mediates the influx of chloride ions through ligand-gated chloride channels called GABAA receptors. When chloride enters ... This is of interest as benzodiazepine receptor antagonists are neutral and have no clinical effects. The author of the study ... The change in symptoms has been proposed to be due to changes in receptor sensitivity for GABA during the process of tolerance ... Benzodiazepines potentiate the action of GABA, by binding a site between the α and γ subunits of the 5-subunit receptor thereby ...
*  Paradoxical disinhibition
... could be attained by an NMDA-receptor antagonist - ketamine. It is thought that blockage of presynasptic GABA receptors of ... GABA, is blocked. Neale, G; Smith, AJ (May 2007). "Self-harm and suicide associated with benzodiazepine usage" (PDF). Br J Gen ... theory is that it occurs secondary to inhibition of the restraining influences of the cortex and frontal lobe due to the GABA- ...
*  Cajal-Retzius cell
... a light-sensitive competitive antagonist of GABA-A receptors, suggesting activation of GABA-A receptors in these sPSCs. ... showed that CR cells expressed GABA-A and GABA-B receptors, ionotropic and metabotropic glutamate receptors, vesicular ... including the very low density lipoprotein receptor (VLDLR), the apolipoprotein E receptor type 2 (ApoER2), and the cytoplasmic ... In 1994, a subpopulation of CR cells was shown to be GABAergic (using GABA as a transmitter). In 2003, CR cells in rodents and ...
*  List of investigational anxiolytics
5-HT6 receptor antagonist [21] BNC-210 (IW-2143) - "GABA modulator" / undefined mechanism of action[22] JNJ-42165279 - FAAH ... 5-HT1A receptor agonist, 5-HT2A receptor antagonist [18] Verucerfont (GSK-561679, NBI-77860) - CRF1 receptor antagonist [19] ... 5-HT1A receptor agonist, 5-HT2A receptor antagonist [4] Vilazodone (EMD-68843, SB-659746A; Viibryd) - 5-HT1A receptor partial ... Agomelatine (AGO-178; Valdoxan) - melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist[1] Riluzole sublingual ( ...
*  Ligand-gated ion channel
Antagonists: ketamine, PCP, dextropropoxyphene, ketobemidone, tramadol, kynurenic acid (endogenous), etc. GABA receptors are ... GABAA receptors are ligand-gated ion channels. GABA (gamma-aminobutyric acid), the endogenous ligand for these receptors, is ... The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, or quisqualate receptor) is a ... The N-methyl-D-aspartate receptor (NMDA receptor) - a type of ionotropic glutamate receptor - is a voltage-dependent ligand- ...