Formaat : 10mg
Synonyms:
| Description | GABAA receptor modulator-10 is an orally active and potent positive allosteric modulator (PAM) of the α1β2γ2GABAA receptor, exhibiting good blood-brain barrier permeability. It enhances the function of the α1β2γ2 GABAA receptor and increases GABA-induced currents. In mouse models of epilepsy induced by Pentetrazol (PTZ) and Kainic Acid (KA), GABAA receptor modulator-10 demonstrates strong antiepileptic efficacy. This compound shows potential for epilepsy research. |
| In vitro | GABAA receptor modulator-10 (Compound 10) (10 μM) enhances the function of α1β2γ2 GABA_A receptors in HEK293T cells overexpressing α1β2γ2 GABA_A receptors through an MQAE-based fluorescence assay. At concentrations ranging from 0.1 to 100 μM, GABAA receptor modulator-10 increases GABA-induced currents in these cells in a concentration-dependent manner, as determined by patch-clamp technique (EC50 = 1.99 μM, Emax = 80.1%). |
| In vivo | GABAA receptor modulator-10 (Compound 10) (10 μM, pre-exposure 3 hours before PTZ treatment) reduced the total distance moved in AB strain zebrafish 6 days post-fertilization. Additionally, GABAA receptor modulator-10 (0.3-30 mg/kg, administered orally 1 hour before PTZ injection) increased the latency of stage I and stage III seizures, decreased the duration of stage III seizures, and prevented stage V seizures in a PTZ-induced mouse seizure model. Furthermore, GABAA receptor modulator-10 (30 mg/kg, orally administered 30 minutes prior to KA injection) mitigated seizure severity and reduced mortality in a KA-induced mouse temporal lobe epilepsy model. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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