| Cat.No. | Name | Information |
|---|---|---|
| M2347 | (+)-Bicuculline | (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. |
| M5442 | Baclofen | Baclofen is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research. |
| M5653 | Flumazenil | Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses. |
| M30053 | Bicuculline methiodide | Bicuculline methiodide is a potent GABA(A) receptors 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. |
| M30031 | Bicuculline methochloride | Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders. |
| M29887 | BPDBA | BPDBA is a selective and noncompetitive betaine/GABA transporter (BGT-1) inhibitor with IC50s of 20 μM and 35 μM against human BGT-1 and mouse GAT2, respectively. |
| M29774 | Flutazolam | Flutazolam (MS 4101; Ro 7-6102) is a medicine acts on benzodiazepine receptors of the brain and relieves anxiety or tension. |
| M29705 | mGAT3/4-IN-2 | mGAT3/4-IN-2 (compound 27b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.44 and 5.25, respectively. |
| M29696 | TPA 023 | TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM. |
| M29341 | Radequinil | Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively. |
| M29148 | RWJ-51204 | RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors. |
| M28688 | PF-06372865 | PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy. |
| M28621 | (S)-SNAP5114 | (S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant agent. |
| M28556 | S-8510 phosphate | S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively. |
| M28120 | Gidazepam | Gidazepam is an agonist of GABA receptor channels (GABA RCs). |
| M27881 | 2-Hydroxysaclofen | 2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats. |
| M27809 | Abecarnil | Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research. |
| M20865 | L-DAB HBR | L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity. |
| M19412 | Anisatin | Anisatin acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM. |
| M19318 | α-Thujone | α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. |
| M14217 | DL-Borneol | DL-Borneol is a racemic mixture of D-Borneol and L-Borneol. DL-Borneol is widely used for the treatment of cardiovascular and cerebrovascular diseases in China. |
| M14215 | 4-Acetamidobutanoic acid | 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities. |
| M8847 | Valnoctamide | Valnoctamide, a GABA receptor activator, is a derivative of Valproic Acid, which has antiepileptic and anticonvulsant properties, and has shown stronger antiepileptic effects than Valproic Acid in a variety of animal models. |
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