GABA Receptor Inhibitor

Vigabatrin (Standard) is the analytical standard of Vigabatrin. This product is intended for research and analytical applications. Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.

mGAT-IN-1 (compound 28) is a potent and non-selective GAT inhibitor. mGAT-IN-1 has a high inhibitory potency toward mGAT3, with an IC₅₀ of 2.5 μM and pIC₅₀ of 5.61.

Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.

Riluzole hydrochloride (Standard) is the analytical standard of Riluzole hydrochloride. This product is intended for research and analytical applications. Riluzole hydrochloride is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.

Aminooxyacetic acid (hemihydrochloride) (Standard) is the analytical standard of Aminooxyacetic acid (hemihydrochloride). This product is intended for research and analytical applications. Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.

Riluzole-¹³C₆ (PK 26124-¹³C₆) is ¹³C labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na⁺ channel blocker which can also inhibit GABA uptake with an IC₅₀ of 43 μM.

MGAT2-IN-5 (Compound 17b) is a selective inhibitor for mouse GABA transit protection subsidity 2 (mGAT2) with an IC₅₀ of 45 μM. MGAT2-IN-5 exhibits anticonvulsive efficacy in audiogenic seizure (AGS) susceptible frings mouse model with an ED₅₀ of 20.4 mg/kg.

Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABA_A receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.

SKF89976A is a selective GABA transporter (GAT-1) inhibitor with IC₅₀s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

3-Hydroxy desalkylflurazepam is a benzodiazepine with potential sedative and anxiolytic effects.

Bicuculline methiodide (Standard) is the analytical standard of Bicuculline methiodide (HY-103474). This product is intended for research and analytical applications. Bicuculline methiodide ((-)-Bicuculline methiodide) is a potent GABAA blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.

Tiagabine-d₄ (NO050328-d₄) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.

MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABA_AR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone (HY-B0214). MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.

DMCM (hydrochloride) (Standard) is the analytical standard of DMCM (hydrochloride). This product is intended for research and analytical applications. DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively.

D-DABA is the enantiomeric form of L-DABA. D-DABA is also a weak inhibitor of GABA-T, but which has only one twentieth of the potency of the L-isomer in inhibiting GABA uptake.

U93631 (Standard) is the analytical standard of U93631 (HY-100686). This product is intended for research and analytical applications. 0

SCS (Standard) is the analytical standard of SCS (HY-103528). This product is intended for research and analytical applications. SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC₅₀ of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions.

Arecaidine hydrochloride (Standard) is the analytical standard of Arecaidine hydrochloride (HY-N2368A). This product is intended for research and analytical applications. Arecaidine hydrochloride is a GABA transport system inhibitor. Arecaidine hydrochloride inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrochloride inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrochloride inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine hydrochloride can be used in research related to neurological diseases.

Tiagabine-d₆ (NO050328-d₆) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.

Vigabatrin (hydrochloride) (Standard) is the analytical standard of Vigabatrin (hydrochloride). This product is intended for research and analytical applications. Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.