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GABA Receptor

GABA Receptor

Gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the central nervous system of vertebrates, activates a group of receptors known as GABA receptors. GABAA and GABAB are the two classes of GABA receptors. GABAB receptors are G protein-coupled receptors, also known as metabotropic receptors, while GABAA receptors are ligand-gated ion channels, also known as ionotropic receptors. It has long been known that direct anion channel activation causes neurons to respond quickly to GABA, which is blocked by bicuculline and picrotoxin. The GABAA receptor is the name given to this channel later. Fast-acting GABA receptors belong to the Cys-loop ligand-gated ion channel family. GABAB receptors, originally identified based on their pharmacological properties, mediate a slow response to GABA.

GABA Receptor related products

Structure Cat No. Product Name CAS No. Product Description
(-)-荷包牡丹碱甲氯化物 V38817 (-)-Bicuculline methochloride 53552-05-9 Bicuculline methochloride (l-Bicuculline methochloride),an enantiomer of (+)-bicuculline methochloride, is a highly potent GABAA receptor antagonist.
AZD-6280 V4231 AZD-6280 942436-93-3 AZD-6280 is a novel, potent and selectiveGABAA(α2/3) receptormodulator, used for treatment of generalized anxiety disorder.
Cgp 52432 V18042 Cgp 52432 139667-74-6 CGP52432 is a GABAB receptor blocker (antagonist) with IC50 of 85 nM.
CTP354 V18855 CTP354 1213669-91-0 CTP354, formerly known as C-21191, a novel deuterated subtype-selective GABA(A) modulator.
L-655708 V13578 L-655708 130477-52-0 L-655708 (FG-8094) is a novel and potent nootropic agent that acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor (Ki=0.45 nM).
N-甲基-beta-咔啉-3-羧酰胺 V40454 FG 7142 78538-74-6 FG 7142 (ZK 39106; LSU-65), a non-specificly benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).
NS-11394 V2899 NS-11394 951650-22-9 NS11394 is a potent, selective and novel positive allosteric modulator of GABA(A) receptor.
ONO-8590580 V4679 ONO-8590580 1802661-73-9 ONO-8590580 is a novel and potent GABAAα5 negative allosteric modulator which enhances long-term potentiation and improves cognitive deficits in preclinical models.
R-巴氯芬 V1291 (R)-baclofen (STX209) 69308-37-8 R)-baclofen (formerly STX-209;STX209;STX 209), a derivative of gamma-aminobutyric acid, is aselectiveGABAB receptoragonist that has been primarily used to treat spasticity.
rac-BHFF V13575 rac-BHFF 123557-91-5 rac-BHFF is a potent, orally bioactive, isomeric enhancer of GABAB receptors.
SSD-114盐酸盐 V0049 SSD114 HCl 2319790-02-6 SSD114 HCl is a novel positive allosteric modulator (PAM) of GABAB receptors.
二氢杨梅素 V1290 Dihydromyricetin (Ampelopsin) 27200-12-0 Dihydromyricetin (also known as Ampelopsin, Ampeloptin, DHM) is a naturally occuring flavonoid isolated from Ampelopsis grossedentata with antioxidant activity.
伊匹妥英 V2932 Imepitoin 188116-07-6 Imepitoin, formerly known as AWD 131-138 and ELB 138, is a novel partial BZD (benzodiazepine) receptor agonist that has the potential use as an antiepileptic drug for the treatment of canine idiopathic epilepsy.
依托咪酯 V1285 Etomidate (R-16659) 33125-97-2 This product is discontinued as it is DEA controlled substance. Etomidate (Amidate, Ethomidate, Hypnomidate,R-26490, R26490,Radenarkon),discovered at Janssen Pharmaceutica in 1964, is a GABAA receptor agonist that has been approved for use as a short-acting anaesthetic drug or sedative.
光甘草定 V9162 Glabridin 59870-68-7 Glabridin is an isoflavane extracted from Glycyrrhiza uralensis and can bind and activate PPARγ with EC50 of 6115 nM.
加巴喷丁 V1286 Gabapentin 60142-96-3 Gabapentin HCl (Neurontin; Aclonium; Convalis; Gabapentin Stada),the hydrochloride salt of gabapentin which is a GABA analog, is an orally bioavailable medication that was approved for use in the treatment of seizures and neuropathic pain.
加巴喷丁盐酸盐 V1284 Gabapentin HCl (Neurontin) 60142-95-2 Gabapentin HCl (Neurontin),the hydrochloride salt of gabapentin which is a GABA analogue, is an orally bioavailable and approved medication used to treat seizures and neuropathic pain.
去甲槟榔次碱盐酸盐 V4961 Guvacine HCl 6027-91-4 Guvacine HCl, the hydrochloride salt of Guvacine, is an alkaloid isolated from the nut ofAreca catechu whichacts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
哌夸林 V4434 Pipequaline 77472-98-1 Pipequaline (also known as PK-8165; PK 8165),a quinoline derivative and a ligand of the benzodiazepine binding site, is a clinically-effective anxiolytic, which is devoid of sedative and anticonvulsant properties, but it was never marketed.
噻加宾 V33761 Tiagabine 115103-54-3 Tiagabine (NO329;NNC-050328;NO 329; NNC-05-0328; NO-05-0328; trade name Gabitril) is a selective and potent GABA (gamma-aminobutyric acid) reuptake inhibitorwith anti-convulsive activity.
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