2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

GABA Receptor

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GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100140R
    Pipequaline (Standard)
    		Agonist
    Pipequaline (Standard) is the analytical standard of Pipequaline. This product is intended for research and analytical applications. Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline (Standard)
  • HY-W705371
    α-Hydroxy etizolam
    α-Hydroxy etizolam is the primary metabolite of Etizolam, possessing nearly identical pharmacological potency and high affinity for benzodiazepine receptors as Etizolam.
    α-Hydroxy etizolam
  • HY-118696
    MGAT2-IN-5
    		Inhibitor
    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.
    MGAT2-IN-5
  • HY-17030R
    Acamprosate calcium (Standard)
    		Agonist
    Acamprosate (calcium) (Standard) is the analytical standard of Acamprosate (calcium). This product is intended for research and analytical applications.
    Acamprosate calcium (Standard)
  • HY-101165R
    Cyclothiazide (Standard)
    		Inhibitor
    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 GABAA 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.
    Cyclothiazide (Standard)
  • HY-100228
    SKF 89976A
    		Inhibitor
    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.
    SKF 89976A
  • HY-171028
    3-Hydroxy desalkylflurazepam
    		Inhibitor
    3-Hydroxy desalkylflurazepam is a benzodiazepine with potential sedative and anxiolytic effects.
    3-Hydroxy desalkylflurazepam
  • HY-B1494R
    Picrotoxinin (Standard)
    		Antagonist
    Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
    Picrotoxinin (Standard)
  • HY-W101673R
    Dipropofol (Standard)
    		Activator
    Dipropofol (Standard) is the analytical standard of Dipropofol. This product is intended for research and analytical applications. Dipropofol is an antioxidant agent.
    Dipropofol (Standard)
  • HY-123801A
    MIDD0301 sodium
    		Inhibitor
    MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) 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.
    MIDD0301 sodium
  • HY-100369AR
    DMCM hydrochloride (Standard)
    		Inhibitor
    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.
    DMCM hydrochloride (Standard)
  • HY-U00228R
    Rilmazafone hydrochloride (Standard)
    Rilmazafone hydrochloride (450191S) is a benzodiazepine (omega) ligand.
    Rilmazafone hydrochloride (Standard)
  • HY-A0173R
    Progabide (Standard)
    		Agonist
    Progabide (Standard) is the analytical standard of Progabide. This product is intended for research and analytical applications. Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.
    Progabide (Standard)
  • HY-128469
    Inaperisone
    		99.0%
    Inaperisone is a centrally acting muscle relaxant. Inaperisone can inhibit the micturition reflex by acting indirectly on GABAB receptors in the brainstem.
    Inaperisone
  • HY-W028389
    Pyrazolam
    Pyrazolam, a Benzodiazepines psychoactive substance, is a central nervous system depressant. Pyrazolam can cause psychomotor impairment.
    Pyrazolam
  • HY-B0353R
    Chlormezanone (Standard)
    Chlormezanone (Standard) is the analytical standard of Chlormezanone. This product is intended for research and analytical applications. Chlormezanone resembles benzodiazepine. The action of Chlormezanone is similar to benzodiazepine-type agents. Chlormezanone is used as an anxiolytic and a muscle relaxant.
    Chlormezanone (Standard)
  • HY-124463S1
    Epiallopregnanolone-d5
    		Antagonist
    Epiallopregnanolone-d5 (5α,3β-THDOC-d5) is deuterium labeled Epiallopregnanolone. Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer.
    Epiallopregnanolone-d<sub>5</sub>
  • HY-N0700R
    alpha-Asarone (Standard)
    		Activator
    alpha-Asarone (Standard) is the analytical standard of alpha-Asarone. This product is intended for research and analytical applications. alpha-Asarone (α-Asarone) is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.
    alpha-Asarone (Standard)
  • HY-W291165
    D-DABA
    		Inhibitor
    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.
    D-DABA
  • HY-119687R
    Bifenazate (Standard)
    		Agonist
    Bifenazate (Standard) is the analytical standard of Bifenazate. This product is intended for research and analytical applications. Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor. Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III.
    Bifenazate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity