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GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $45 | In Stock | |
| 50 mg | $68 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $29 | In Stock |
| Description | GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism. |
| Targets&IC50 | GABAA:100 nM |
| In vitro | In the presence of U93631 at 5 UM, the peak amplitude decreased as a function of GABA concentration, with the half-maximal inhibitory concentration being approximately 100 nM, which is close to the Kd for the high affinity GABA site(85 nM). It appears that the drug interacts with GABA-bound receptors (at least monoliganded) and accelerates receptor desensitization, rather than acting as an open channel blocker. |
| Molecular Weight | 299.37 |
| Formula | C17H21N3O2 |
| Cas No. | 152273-12-6 |
| Smiles | CC(C)(C)OC(=O)c1ncn-2c1C(C)(C)Nc1ccccc-21 |
| Relative Density. | 1.19g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (183.72 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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