产品
编 号：F050611
分子式：C21H20FN3O5S
分子量：445.46
分子式：C21H20FN3O5S
分子量：445.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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询价
结构图
CAS No: 1159600-41-5
产品详情
生物活性：
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.
体内研究：
Basmisanil (3-100 mg/kg, p.o.) occupies GABAA-α receptor in dose-dependent in rat brain.Basmisanil (3-600 mg/kg p.o.) improves cognition in rats and non.human primates and not show anxiogenic or proconvulsant effects.Animal Model:Sprague Dawley rats(180 g; female)
Dosage:3-100 mg/kg
Administration:p.o.
Result:Decreased the binding of [3H]-Ro 15-4513 in a dose-dependent manner.Reduced specific binding in the hippocampus by 70% at the highest dose (100 mg/kg).
Animal Model:Lister Hooded rats, Wistar rats and F-344 Fischer rats (Lister Hooded rats: 220-250 g; male)(Wistar rats: 200-220 g; male and female)(F-344 Fischer rats: 170-180 g; male)
Dosage:3-600 mg/kg
Administration:p.o.
Result:Significantly attenuated the diazepam-induced deficit.Showed plasma concentrations in dose- and time-dependent manner and reached a maximal level of 903 ng/mL (379 nM free plasma) 30 min after the administration at 10 mg/kg.
Animal Model:Male cynomolgus macaques(Macaca fascicularis; 7-10 kg)
Dosage:1-600 mg/kg
Administration:p.o.
Result:Significantly improved the percentage of correct first reaches during difficult trials of the object retrieval task at the 3 and 10 mg/kg doses.Exhibited an inverted U-shaped dose response in this paradigm with the 1 and 30 mg/kg doses producing no marked improvement on performance.Increased the total plasma exposure in dose-dependent.
体外研究：
Basmisanil (0.1 nM-100 μM) has high affinity for bounding to recombinant human GABAA-α5 receptors with a Ki value of 5 nM and more than 90-fold selectivity versus α1 (Ki = 1031 nM), α2 (Ki = 458 nM), and α3 (Ki = 510 nM) subunit-containing receptors.Basmisanil (1 nM-1 μM) shows a highly selective inhibition of GABAA-α5 with a IC50 value of 8 nM.Basmisanil (1 μM) inhibits GABA-induced currents at GABAA-α5 yet had little or no effect at the other receptor subtypes.
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.
体内研究：
Basmisanil (3-100 mg/kg, p.o.) occupies GABAA-α receptor in dose-dependent in rat brain.Basmisanil (3-600 mg/kg p.o.) improves cognition in rats and non.human primates and not show anxiogenic or proconvulsant effects.Animal Model:Sprague Dawley rats(180 g; female)
Dosage:3-100 mg/kg
Administration:p.o.
Result:Decreased the binding of [3H]-Ro 15-4513 in a dose-dependent manner.Reduced specific binding in the hippocampus by 70% at the highest dose (100 mg/kg).
Animal Model:Lister Hooded rats, Wistar rats and F-344 Fischer rats (Lister Hooded rats: 220-250 g; male)(Wistar rats: 200-220 g; male and female)(F-344 Fischer rats: 170-180 g; male)
Dosage:3-600 mg/kg
Administration:p.o.
Result:Significantly attenuated the diazepam-induced deficit.Showed plasma concentrations in dose- and time-dependent manner and reached a maximal level of 903 ng/mL (379 nM free plasma) 30 min after the administration at 10 mg/kg.
Animal Model:Male cynomolgus macaques(Macaca fascicularis; 7-10 kg)
Dosage:1-600 mg/kg
Administration:p.o.
Result:Significantly improved the percentage of correct first reaches during difficult trials of the object retrieval task at the 3 and 10 mg/kg doses.Exhibited an inverted U-shaped dose response in this paradigm with the 1 and 30 mg/kg doses producing no marked improvement on performance.Increased the total plasma exposure in dose-dependent.
体外研究：
Basmisanil (0.1 nM-100 μM) has high affinity for bounding to recombinant human GABAA-α5 receptors with a Ki value of 5 nM and more than 90-fold selectivity versus α1 (Ki = 1031 nM), α2 (Ki = 458 nM), and α3 (Ki = 510 nM) subunit-containing receptors.Basmisanil (1 nM-1 μM) shows a highly selective inhibition of GABAA-α5 with a IC50 value of 8 nM.Basmisanil (1 μM) inhibits GABA-induced currents at GABAA-α5 yet had little or no effect at the other receptor subtypes.
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