| 产品描述： | 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 |
| 靶点： |
IC50: 8 nM (GABAAα5) Ki: 5 nM (GABAAα5); 1031 nM (GABAAα1); 458 nM (GABAAα2); 510 nM (GABAAα3);GABAReceptor |
| 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 |
| 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. |
| 参考文献： |
1. Joerg F Hipp, et al. Basmisanil, a highly selective GABA A-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man. Sci Rep. 2021 Apr 8;11(1):7700. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.245 ml |
11.224 ml |
22.449 ml |
| 5 mM |
0.449 ml |
2.245 ml |
4.49 ml |
| 10 mM |
0.224 ml |
1.122 ml |
2.245 ml |
| 50 mM |
0.045 ml |
0.224 ml |
0.449 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京