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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V38817 | (-)-Bicuculline methochloride | 53552-05-9 | Bicuculline methochloride (l-Bicuculline methochloride),an enantiomer of (+)-bicuculline methochloride, is a highly potent GABAA receptor antagonist. |
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V4231 | AZD-6280 | 942436-93-3 | AZD-6280 is a novel, potent and selectiveGABAA(α2/3) receptormodulator, used for treatment of generalized anxiety disorder. |
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V18042 | Cgp 52432 | 139667-74-6 | CGP52432 is a GABAB receptor blocker (antagonist) with IC50 of 85 nM. |
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V18855 | CTP354 | 1213669-91-0 | CTP354, formerly known as C-21191, a novel deuterated subtype-selective GABA(A) modulator. |
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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). |
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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). |
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V2899 | NS-11394 | 951650-22-9 | NS11394 is a potent, selective and novel positive allosteric modulator of GABA(A) receptor. |
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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. |
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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. |
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V13575 | rac-BHFF | 123557-91-5 | rac-BHFF is a potent, orally bioactive, isomeric enhancer of GABAB receptors. |
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V0049 | SSD114 HCl | 2319790-02-6 | SSD114 HCl is a novel positive allosteric modulator (PAM) of GABAB receptors. |
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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. |
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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. |
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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. |
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V9162 | Glabridin | 59870-68-7 | Glabridin is an isoflavane extracted from Glycyrrhiza uralensis and can bind and activate PPARγ with EC50 of 6115 nM. |
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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. |
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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. |
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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). |
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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. |
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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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