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*  Sedative
In spite of the fact that each sedative acts in its own way, they produce beneficial relaxing effect by increasing GABA ... Alprazolam Clobazam Clorazepate Etizolam Nonbenzodiazepine hypnotics Eszopiclone Zaleplon Zolpidem Zopiclone Orexin antagonists ... Yi PL; Tsai CH; Chen YC; Chang FC (March 2007). "Gamma-aminobutyric acid (GABA) receptor mediates suanzaorentang, a traditional ... GABA), which are brain chemicals performing communication between brain cells. ...
*  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 ...
*  Pitrazepin
Murphy VF, Wann KT (November 1988). "The action of GABA receptor agonists and antagonists on muscle membrane conductance in ... Curtis DR, Gynther BD (November 1986). "Pitrazepin: a central glycine and GABA antagonist". European Journal of Pharmacology. ... 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 ...
*  Thujone
... acts on GABA as an antagonist (opposite to the effects of alcohol) and as a component of several essential oils, is ... These effects are in line with other GABA antagonists. Also, alpha-thujone is metabolized quickly in the liver in mice. ... Modulation of Ionotropic GABA Receptors by Natural Products of Plant Origin Dettling A, Grass H, Schuff A, Skopp G, Strohbeck- ... By inhibiting GABA receptor activation, neurons may fire more easily, which can cause muscle spasms and convulsions. Thujone is ...
*  Allobarbital
I. Effects of barbiturates on the convulsive action of GABA-antagonists". Acta Physiologica et Pharmacologica Bulgarica. 13 (3 ... Getova, D.; Georgiev, V. (1987). "GABA-ergic mechanisms in the anticonvulsive activity of newly synthesized barbiturates. ...
*  Illicium anisatum
Anisatin and its derivatives are suspected of acting as strong GABA antagonists. Illicium floridanum Illicium verum "Illicium ...
*  Convulsant
Advantages of an antagonist: bicuculline and other GABA antagonists. British Journal of Pharmacology. 2013 May;169(2):328-36. ... also GABA antagonist) Sinomenine Strychnine Thebaine Tutin Ionotropic glutamate receptor agonists AMPA Domoic acid Kainic acid ... Most convulsants are antagonists (or inverse agonists) at either the GABAA or glycine receptors, or ionotropic glutamate ... GABAA receptor antagonists, inverse agonists or negative allosteric modulators Bemegride Bicuculline Cicutoxin Cyclothiazide ...
*  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 ...
*  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 ... Ehrenberger, K.; Benkoe, E.; Felix, D. (1982). "Suppressive Action of Picrotoxin, a GABA Antagonist, on Labyrinthine ... Because it inhibits channels activated by GABA, GABA-enhancing drugs like barbiturates and benzodiazepines can be used as an ...
*  Spinosad
Spinosyn A resembles a GABA antagonist and is comparable to the effect of avermectin on insect neurons. Spinosyn A is highly ... Spinosad also has secondary effects as a γ-amino-butyric acid (GABA) neurotransmitter agonist. It kills insects by ...
*  GABA receptor
GABA agonist GABA antagonist Kuffler SW, Edwards C (November 1958). "Mechanism of gamma aminobutyric acid (GABA) action and its ... 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 ... Kusama T, Spivak CE, Whiting P, Dawson VL, Schaeffer JC, Uhl GR (May 1993). "Pharmacology of GABA rho 1 and GABA alpha/beta ...
*  1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid
... (TPMPA) is a GABA antagonist selective for the GABAA-ρ (previously known ...
*  Autapse
Upon using a GABA-antagonist to block autapses, the likelihood of an immediate subsequent second depolarization step increased ... Anti-epileptic drugs could potentially target this AR of GABA that seems to rampantly occur at FS neuron autapses. Using a glia ... Autapses can be either glutamate-releasing (excitatory) or GABA-releasing (inhibitory), just like their traditional synapse ... antagonists affect synaptic versus extrasynaptic NMDARs. Recently, it has been proposed that autapses could possibly form as a ...
*  Clobazam
It was also reported that these effects were inhibited by the GABA antagonist flumazenil, and that clobazam acts more ... 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, ... 2000). "Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype". Nature ...
*  Etizolam
Flumazenil, a GABA antagonist agent used to reverse benzodiazepine overdoses, inhibits the effect of etizolam as well as ... Cases of intentional suicide by overdose using etizolam in combination with GABA agonists have been reported. Although etizolam ... "Effects of benzodiazepines and non-benzodiazepine compounds on the GABA-induced response in frog isolated sensory neurones". Br ...
*  Cicutoxin
... is a noncompetitive gamma-aminobytyric acid (GABA) antagonist in the central nervous system (CNS). GABA normally ... 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 ...
*  Oenanthotoxin
It is a central nervous system poison, and acts as a noncompetitive gamma-aminobutyric acid (GABA) antagonist. A case has been ... When oenanthotoxin is introduced to the body, it non-competitively binds to the same beta-domain receptor as GABA would have ... Oenanthotoxin is part of a group of C17 conjugated polyacetylenes that act as noncompetitive gamma-aminobutyric acid (GABA) ... inhibitors in the central nervous system (CNS). GABA binds to the beta-domain of the GABAA receptor in the CNS and activates ...
*  Pentylenetetrazol
Ts65Dn mice injected with a 2-week regimen of either of two compounds picrotoxin or bilobalide (both GABA antagonists) showed ... Many GABA-A ligands are effective anticonvulsants, such as the sedatives diazepam and phenobarbital, but presumably ... "Convulsant potencies of tetrazoles are highly correlated with actions on GABA / benzodiazepine / picrotoxin receptor complexes ... found that in vivo convulsant potency was strongly correlated to in vitro affinity to the picrotoxin binding site on the GABA-A ...
*  Anxiogenic
GABA antagonists such as DMCM, FG-7142 and ZK-93426, serotonergic agents such as mCPP and LY-293,284, adrenergic agents such as ... yohimbine, antipsychotics/dopamine antagonists such as ecopipam and reserpine, and cholecystokinin (CCK) (especially the ...
*  Cicuta
It is a non-competitive gamma-aminobutyric acid (GABA) receptor antagonist. Cicutoxin acts on the GABAA receptor causing a ...
*  Dendrobine
While structurally related to picrotoxinin, dendrobine is not an antagonist of GABA. Kreis, L. M., Consice textbook of forensic ... Kudo, Y; Tanaka, A; Yamada, K (1983). "Dendrobine, an antagonist of beta-alanine, taurine and of presynaptic inhibition in the ... Dendrobine is a strongly selective competitive antagonist of β-alanine, taurine, and glycine. ...
*  Ro15-4513
Also because of its GABA antagonist effects, Ro15-4513 causes serious side-effects including both anxiety, and at higher doses ... It acts as a competitive antagonist, and can therefore be an antidote to the acute impairment caused by alcohol. Ro15-4513 is ... The specificity of the compound to a small number of GABA receptor sub-types leads to the generation, with accurate modelling, ... Another problem is that alcohol's effects are not purely mediated by GABA receptors; at higher doses alcohol binds to several ...
*  Nucleus raphe pallidus
Microinjections of a GABA-a antagonist into the nucleus raphe pallidus, induces an increased heart rate. Conversely, ... In both of these cases, GABA is mediating two different sympathetic responses, so clearly the nucleus raphe pallidus is a far ... with GABA. When the preoptic area receives immune signals from the body, the inhibition stops and the rostral portion of the ... microinjections of muscimol, a GABA-a agonist, inhibit tachycardia in rats under air-stress stimuli. ...
*  Serotonin syndrome
Other neurotransmitters may also play a role; NMDA receptor antagonists and GABA have been suggested as affecting the ... If this is not sufficient, a serotonin antagonist such as cyproheptadine may be used. In those with a high body temperature ... The serotonin antagonist cyproheptadine is the recommended initial therapy, although there have been no controlled trials ... Nisijima K, Yoshino T, Yui K, Katoh S (January 2001). "Potent serotonin (5-HT)(2A) receptor antagonists completely prevent the ...
*  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 ...
*  List of investigational anxiolytics
5-HT6 receptor antagonist [21] BNC-210 (IW-2143) - "GABA modulator" / undefined mechanism of action[22] JNJ-42165279 - FAAH ... 5-HT2A receptor antagonist [18] Verucerfont (GSK-561679, NBI-77860) - CRF1 receptor antagonist [19] Vilazodone (EMD-68843, SB- ... Agomelatine (AGO-178; Valdoxan) - melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist[1] Riluzole sublingual ( ... 5-HT2A receptor antagonist [4] Vilazodone (EMD-68843, SB-659746A; Viibryd) - 5-HT1A receptor partial agonist and serotonin ...
*  Levorphanol
... also acts as a glycine receptor antagonist and GABA receptor antagonist at very high concentrations. Levorphanol is 6 to 8 ... NMDA receptor antagonist), and weakly active opioid. DXO is an active metabolite of the pharmaceutical drug dextromethorphan ( ... as well as an NMDA receptor antagonist and a serotonin-norepinephrine reuptake inhibitor (SNRI). Levorphanol, similarly to ...