| 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. |
| 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. |
| M28615 | GABAA receptor agent 1 | GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity. |
| 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. |
| M14216 | DAA-1106 | DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor. |
| 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. |
| M6995 | MRK 016 | MRK 016 is a gABAA receptor inverse agonist selective for the α5-subtype (EC50 = 3 nM). |
| M6720 | Etifoxine hydrochloride | Etifoxine hydrochloride is a ligand of the translocator protein (TSPO); also GABAA receptor potentiator. |
| M6009 | Tiagabine | Tiagabine is an anticonvulsant compound that acts as an inhibitor of GABA reabsorption. |
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