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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- ... 1999). "Dopamine receptor D2 and D4 genes, GABA(A) alpha-1 subunit genes and response to lithium prophylaxis in mood disorders ...
*  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 ... GABA-α and GABAreceptors produce sedative and hypnotic effects and have anti-convulsion properties. GABAreceptors too ... There are three receptors of the gamma-aminobutyric acid. The two receptors GABA-α and GABA-ρ are ion channels that signal ... Alcohol is an indirect GABA agonist. GABA is the major inhibitory neurotransmitter in the brain, and GABA-like drugs are used ...
*  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 ... work by enhancing GABA-activated chloride currents at GABAA-receptor-coupled Cl− channels. It was also reported that these ...
*  Bamaluzole
... is a GABA receptor agonist. It was patented as an anticonvulsant by Merck but was never marketed. Imidazopyridine ...
*  Gamma-Amino-beta-hydroxybutyric acid
GABOB is a GABA receptor agonist. It has two stereoisomers, and shows stereoselectivity in its actions. Specifically, (R)-(-)- ... GABOB is a partial agonist of the GABAB receptor and an agonist of the GABAA receptor. (S)-(+)-GABOB is around twice as potent ... 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 ...
*  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 ... dopamine receptor density and postsynaptic receptor responsivity to dopamine while reducing striatal cholinergic activity so as ...
*  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 ... Sattelle DB, Pinnock RD, Wafford KA, David JA (January 1988). "GABA receptors on the cell-body membrane of an identified insect ... Anthony NM, Harrison JB, Sattelle DB (1993). "GABA receptor molecules of insects". Exs. 63: 172-209. doi:10.1007/978-3-0348- ...
*  Emamectin
McGonigle, I.; Lummis, S. C. R. (2010). "Molecular Characterization of Agonists That Bind to an Insect GABA Receptor". ... Emamectin works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride ... the release of GABA from the synapses between nerve cells and while additionally increasing GABA's affinity for its receptor on ... The stronger binding of GABA increases the cells permeability to chloride ions within the cell due to the hypotonic ...
*  SL-75102
... , or progabide acid, is an active metabolite of progabide and an anticonvulsant GABA receptor agonist. "Progabide and ...
*  Spasticity
... is often treated with the drug baclofen, which acts as an agonist at GABA receptors, which are inhibitory. Spastic ... Receptors in the muscles receive messages from the nervous system, which sense the amount of stretch in the muscle and sends ... Agonist contractions are performed first in small ranges progressing to larger arcs of movement Highly stressful activities be ... GABA's inhibitory actions contribute to baclofen's efficacy as an anti-spasticity agent. Spasticity mostly occurs in disorders ...
*  Adinazolam
... binds to peripheral-type benzodiazepine receptors that interact allosterically with GABA receptors as an agonist to ... NDMAD has an approximately 25-fold high affinity for benzodiazepine receptors as compared to its precursor, accounting for the ...
*  Z)-4-Amino-2-butenoic acid
... receptors in the peripheral antinociceptive effect induced by GABA(C) receptor agonist cis-4-aminocrotonic acid". Life Sciences ... Z)-4-Amino-2-butenoic acid (CACA, cis-4-aminocrotonic acid) is a GABA receptor partial agonist selective for the GABAA-ρ ( ... cis-4-Aminocrotonic acid at Sigma-Aldrich Qian, H; Dowling, JE (1996). "Selective agonists for GABAC receptors". Trends in ... GABA(C) receptors". Journal of Neurochemistry. 75 (6): 2602-10. doi:10.1046/j.1471-4159.2000.0752602.x. PMID 11080214. Reis, GM ...
*  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. ...
*  Tolgabide
... and therefore as an indirect agonist of the GABA receptors. Progabide Fengabine David J. Triggle (1996). Dictionary of ... It is an analogue of progabide and acts similarly to it as a prodrug of GABA, ...
*  Alcohol detoxification
This drug acts as a GABA B receptor agonist and this may be beneficial. Drug detoxification Detoxification, the process, real ... This drug enhances GABA neurotransmission and reduces glutamate levels. It is used in Italy in small amounts under the trade ...
*  CI-966
GABA-T) inhibitor (and hence also an indirect and non-selective GABA receptor agonist) vigabatrin has also been associated with ... and hence indirect and non-selective GABA receptor full agonist. It was investigated as a potential anticonvulsant, anxiolytic ... Jan Egebjerg; Arne Schousboe; Povl Krogsgaard-Larsen (4 October 2001). Glutamate and GABA Receptors and Transporters: Structure ... GABA: Receptors, Transporters and Metabolism. Birkhäuser. pp. 70-. ISBN 978-3-0348-8990-2. Linda Pullan; Jitendra Patel (13 ...
*  Gabapentinoid
... gabapentin and pregabalin do not bind to the GABA receptors, do not convert into GABA or GABA receptor agonists in vivo, and do ... In addition, phenibut has been found to act as a gabapentinoid in addition to its action of being a GABAB receptor agonist. ... However, phenibut uniquely also binds to and acts as an agonist of the GABAB receptor with lower affinity (~5- to 10-fold in ... GABA) (i.e., GABA analogues) which block α2δ subunit-containing voltage-dependent calcium channels (VDCCs). This site has been ...
*  Buspirone
... it is not a GABA receptor agonist), and so buspirone does not carry the risk of physical dependence and withdrawal symptoms for ... It is a preferential full agonist of presynaptic 5-HT1A receptors, which are inhibitory autoreceptors, and a partial agonist of ... a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex". Naunyn Schmiedebergs Arch. Pharmacol. ... and 5-HT7 receptors. In addition to binding to serotonin receptors, buspirone is an antagonist of the dopamine D2 receptor with ...
*  Isovaline
Puil E. (Jan 2010). "R-Isovaline: a subtype-specific agonist at GABA(B)-receptors?". Neuroscience. 201: 85-95. doi:10.1016/j. ... Jun 28, 2012). "GABA(B) receptor-mediated selective peripheral analgesia by the non-proteinogenic amino acid, isovaline". ... The structure of isovaline is similar to the amino acids GABA and glycine, the chief inhibitory neurotransmitters in the ... Isovaline acts as an analgesic in mice by activating peripheral GABAB receptors. In a mouse model of osteoarthritis isovaline ...
*  Erminio Costa
"Brain allopregnanolone regulates the potency of the GABA(A) receptor agonist muscimol". Neuropharmacology. 39 (3): 440-448. doi ... His research interests covered brain serotonergic activity in health and disease, benzodiazepine-GABA interactions, ... benzodiazepine action at GABAA receptors, neurophysiological role of neurosteroids, and GABAergic dysfunction and changes in ...
*  Allopregnanediol
It has been found to act like a partial agonist of an allosteric site of the GABA receptor and hence might play a biological ... It has also been found to act as an agonist of the human pregnane X receptor, albeit with an EC50 that is more than an order of ... Belelli D, Gee KW (1989). "5 alpha-pregnan-3 alpha,20 alpha-diol behaves like a partial agonist in the modulation of GABA- ... "Evolution of pharmacologic specificity in the pregnane X receptor". BMC Evolutionary Biology. 8 (1): 103. doi:10.1186/1471-2148 ...
*  Psychoactive drug
For example, propofol is a GABA agonist, and ketamine is an NMDA receptor antagonist. Psychoactive drugs are often prescribed ... Li X, Pearce RA; Pearce (2000). "Effects of halothane on GABA(A) receptor kinetics: evidence for slowed agonist unbinding". The ... also known as opioid receptor agonists. This class of drugs can be highly addictive, and includes opiate narcotics, like ... Conversely, overstimulation of receptors for a particular neurotransmitter may cause a decrease in both number and sensitivity ...
*  General anaesthesia
... and glycine and serotonin receptors. Halothane has been found to be a GABA agonist, and ketamine is an NMDA receptor antagonist ... "Effects of halothane on GABA(A) receptor kinetics: evidence for slowed agonist unbinding". J. Neurosci. 20 (3): 899-907. PMID ... Potential pharmacologic targets of general anaesthetics are GABA, glutamate receptors, voltage-gated ion channels, ... Muscle relaxants work by preventing acetylcholine from attaching to its receptor. Paralysis of the muscles of respiration-the ...
*  Isonipecotic acid
"Activation of single heteromeric GABA(A) receptor ion channels by full and partial agonists". The Journal of Physiology. 557 ( ... Isonipecotic acid is a heterocyclic compound which acts as a GABAA receptor partial agonist. It consists of a piperidine ring ...
*  JWH-018
... are full agonists. THC has been shown to inhibit GABA receptor neurotransmission in the brain via several pathways. JWH-018 may ... "Δ9-tetrahydrocannabinol is a full agonist at CB1 receptors on GABA neuron axon terminals in the hippocampus". Neuropharmacology ... JWH-018 is a full agonist of both the CB1 and CB2 cannabinoid receptors, with a reported binding affinity of 9.00 ± 5.00 nM at ... Cannabinoid receptor full agonists may present serious dangers to the user when used to excess. Various physical and ...
*  List of investigational anxiolytics
5-HT1A receptor agonist, 5-HT2A receptor antagonist [4] Vilazodone (EMD-68843, SB-659746A; Viibryd) - 5-HT1A receptor partial ... "GABA modulator" / undefined mechanism of action[22] JNJ-42165279 - FAAH inhibitor[23] MP-20X - CB1 and 5-HT1A receptor ... 5-HT1A receptor agonist, 5-HT2A receptor antagonist [18] Verucerfont (GSK-561679, NBI-77860) - CRF1 receptor antagonist [19] ... Agomelatine (AGO-178; Valdoxan) - melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist[1] Riluzole sublingual ( ...