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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V10946 | Loreclezole | 117857-45-1 | Loreclezole (R-72063; R 72063; R72063), a triazole analog, is a sedative, anti-seizure/anticonvulsant and antiepileptic agent thatacts as a positive allosteric modulator (PAM) ofGABAAreceptor. |
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V24395 | Lorediplon | 917393-39-6 | Lorediplon, a nonbenzodiazepine of the pyrazolopyrimidine family, is a non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep. |
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V24414 | Lotilaner | 1369852-71-0 | Lotilaner (Credelio) is a potent insecticide agent (veterinary drug)acting as a non-competitive antagonist of insect GABA receptors. |
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V70279 | MIDD0301 (GL-II-93) | 2187489-08-1 | MIDD0301 (GL-II-93) is an orally bioactive, anti-asthmatic PAM (positive allosteric modulator) of GABAA receptors. |
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V80795 | MmTx1 toxin (Microrotoxin 1) | MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor sensitivity to agonists. | |
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V80796 | MmTx2 toxin (Microrotoxin 2) | MmTx2 toxin is a GABAA receptor modulator that enhances the sensitivity of GABAA receptors to agonists. | |
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V71802 | MRK-016 | 342652-67-9 | MRK-016 is a selective, orally bioavailable, BBB (blood-brain barrier) permeable (penetrable) GABAA α5 receptor antagonist (inhibitor) with EC50 of 3 nM for GABAA α5 and human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2 and GABAA α5β3γ2 The Kis were 0.83, 0.85, 0.77 and 1.4 nM respectively. |
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V71798 | MRK-898 | 461450-30-6 | MRK-898 is an orally bioavailable GABA(A) receptor modulator. |
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V71805 | Muscimol hydrochloride (Agarin hydrochloride; Agarine hydrochloride) | 3579-03-1 | Muscimol (Agarin; Agarine) HCl is a psychoactive isoxazole. |
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V70273 | N-Arachidonyl-GABA | 128201-89-8 | N-Arachidonyl-GABA is a fatty amino acid (AA) related to anandamide found in bovine brain. |
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V71828 | NCS-382 | 520505-01-5 | NCS-382 is a potent GABA receptor antagonist and a GHBR receptor antagonist. |
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V70280 | NCS-382 sodium | 131733-92-1 | NCS-382 (sodium) is a potent GABA receptor antagonist. |
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V71807 | Nipecotic acid (3-Piperidine; (±)-β-Homoproline; Hexahydronicotinic acid; 3-Carboxypiperidine) | 498-95-3 | Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial aminobutyric acid (GABA) uptake in vitro. |
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V71835 | NNC 05-2090 | 184845-43-0 | NNC 05-2090 is a potent mGAT2 inhibitor (antagonist) with Ki of 1.4 μM. |
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V71834 | NNC05-2090 hydrochloride | 184845-18-9 | NNC05-2090 HCl is a GABA uptake inhibitor. |
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V12242 | Norepinephrine bitartrate | 51-40-1 | Norepinephrine bitartrate(Levarterenol; L-Noradrenaline) is a potent and β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. |
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V1934 | Oxiracetam (ISF 2522) | 62613-82-5 | Oxiracetam (also known as ISF 2522), a novel cyclic derivative of gamma-aminobutyric acid (GABA) which acts as a positive allosteric modulator of the AMPA receptors, is widely used as a nootropic drug to improve memory and learning in patients with cognitive impairments. |
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V71841 | Phaclofen | 114012-12-3 | Phaclofen is a selective GABAB receptor antagonist. |
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V71806 | Phenibut hydrochloride (β-Phenyl-GABA hydrochloride; 4-Amino-3-phenylbutanoic acid hydrochloride) | 3060-41-1 | Phenibut (β-Phenyl-GABA) HCl is an orally bioactive GABA-B agonist. |
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V10395 | Picrotoxin | 124-87-8 | Picrotoxin (cocculin) is a naturally occuring and poisonous crystalline plant compound. |
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