keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
6-hydroxy Buspirone是抗焦虑化合物buspirone的活性代谢产物,通过细胞色素P450(CYP)亚型CYP3A4从buspirone转化而来。该化合物在大鼠海马和背侧缝核的5-羟色胺(5-HT)受体亚型5-HT1A上具有亲和力(EC50s分别为4和1 µM),并作为多巴胺D2、D3、D4受体拮抗剂(IC50s分别为3.1、4.9、和0.85 µM)。同时,它还以浓度依赖性方式抑制表达人类转运体的S2近端小管细胞中的有机阳离子转运体1(OCT1)、OCT2和OCT3。
产品描述 | 6-Hydroxy Buspirone, an active metabolite of the anxiolytic compound buspirone, is produced via the cytochrome P450 (CYP) isoform CYP3A4. This compound exhibits affinity for the serotonin (5-HT) receptor subtype 5-HT1A, demonstrating efficacy in the rat hippocampus and dorsal raphe with half-maximal effective concentrations (EC50s) of 4 and 1 µM, respectively. Furthermore, 6-Hydroxy Buspirone acts as a potent antagonist against dopamine D2, D3, and D4 receptors with half-maximal inhibitory concentrations (IC50s) of 3.1, 4.9, and 0.85 µM, respectively, and inhibits the organic cation transporters 1 (OCT1), OCT2, and OCT3 in S2 proximal tubule cells expressing human transporters, showcasing a concentration-dependent mechanism. |
别名 | BMY 28674, BMS-52821 |
分子量 | 401.50 |
分子式 | C21H31N5O3 |
CAS No. | 125481-61-0 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Methanol: Soluble
Ethanol: Soluble
DMSO: Soluble
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
6-hydroxy Buspirone 125481-61-0 BMY 28674 BMS-52821 Inhibitor inhibitor inhibit