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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V1287 | (+)-Bicuculline | 485-49-4 | Bicuculline (BRN-0098786; NSC-32192; BRN0098786; NSC32192), a phthalide-isoquinoline-based natural product isolated from Dicentra cucullaria, is a novel, light-sensitive and competitive antagonist of GABAA receptors with an IC50 of 2 μM. |
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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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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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V44175 | Abecarnil | 111841-85-1 | Abecarnil (ZK112119; ZK-112119) is a positive allosteric modulator of GABAA receptor, acting as aligand or a partial agonist for benzodiazepine (BZ) receptorwith anxiolytic and anticonvulsant effects. |
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V5333 | Acamprosate calcium (Campral EC) | 77337-73-6 | Acamprosate calcium (also known as Campral EC),a medication used in the treatment of alcohol dependence, is a GABA receptor agonist and modulator of glutamatergic systems; it reduces alcohol consumption in animal models of alcohol addiction. |
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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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V12272 | Baicalin | 21967-41-9 | Baicalin is naturally occuring flavonoid glycoside found in several species in the genus Scutellaria, including Scutellaria lateriflora (blue skullcap). |
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V12297 | Basmisanil (RG1662) | 1159600-41-5 | Basmisanil, formerly known as RG1662, RO5186582, is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome. |
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V1292 | Bemegride (Bemegrid) | 64-65-3 | Bemegride (3-Ethyl-3-methylglutarimide; Antibarbi; Agipnon; Ahypnon; Eukraton; Malysol; Mikedimide; Zentraleptin) is apotent central nervous system stimulant and effective antidote for barbiturate poisoning. |
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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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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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V4362 | EMAMECTIN BENZOATE | 155569-91-8 | Emamectin Benzoate (also known as MK-244) is a chloride channel activator that acts by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods. |
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V20683 | Ergoloid Mesylates | 8067-24-1 | Dihydroergotoxine mesylate is a series of alkaloid salt mixtures with high binding activity to GABAA receptors. |
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V1285 | Etomidate (R-16659) | 33125-97-2 | 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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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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V21034 | Fipronil | 120068-37-3 | Fipronil is a phenylpyrazole-based insecticide witha broad-spectrum insecticidal activity. |
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V1283 | Flumazenil (Ro 15-1788) | 78755-81-4 | Flumazenil (Flumazepil, Anexate, Romazicon, Lanexat;Ro-15-1788; Ro-15 1788)is a specific and competitive GABAA receptor antagonist that has been used for the treatment of benzodiazepine overdoses. |
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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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