Powder: -20°C for 3 years | In solvent: -80°C for 2 years
ABT-724 是高度选择性的多巴胺D4受体激动剂,对人多巴胺D4受体的EC50=12.4 nM。它是大鼠D4(EC50为 14.3 nM) 和雪貂D4受体 (EC50为 23.2 nM) 的有效部分激动剂,对多巴胺 D1,D2,D3或 D5受体没有影响。它可用于勃起功能障碍的研究,并具有较少的副作用。
产品描述 | ABT-724 is an agonist of dopamine D4 receptor(EC50: 12.4 nM) |
靶点活性 | D4:12.4 nM(EC50), dopamine D4 receptor:12.4 nM(EC50) |
体外活性 | ABT-724 is a selective dopamine D(4) receptor agonist that activates human dopamine D(4) receptors with an EC(50) of 12.4 nM and 61% efficacy, with no effect on dopamine D(1), D(2), D(3), or D(5) receptors[1]. |
体内活性 | ABT-724 dose-dependently facilitates penile erection when given s.c. to conscious rats, an effect that is blocked by haloperidol and clozapine but not by domperidone.?A proerectile effect is observed after intracerebroventricular but not intrathecal administration, suggesting a supraspinal site of action.?s.c. injections of ABT-724 increase intracavernosal pressure in awake freely moving rats.?In the presence of sildenafil, a potentiation of the proerectile effect of ABT-724 is observed in conscious rats.?The ability of ABT-724 to facilitate penile erection together with the favorable side-effect profile indicates that ABT-724 could be useful for the treatment of erectile dysfunction[1]. |
动物实验 | ABT-724 (maleate salt) was freshly prepared and administered to rats via s.c. injection into the back neck area (1 ml/kg injection volume). For intracerebroventricular (ICV) or intrathecal administrations, rats were allowed at least 1 week of recovery from surgery before behavioral testing. The compounds of interest were infused ICV (left lateral ventricle) in a 5-μl volume or 10 μl intrathecally. After the experiment was completed, infusion of 0.5% fast-green dye in saline solution and subsequent dissection were carried out to confirm the diffusion of the injection solution[1]. |
别名 | 2 - [(4-吡啶-2-基哌嗪-1-基)甲基]-1H-苯并咪唑 |
分子量 | 293.37 |
分子式 | C17H19N5 |
CAS No. | 70006-24-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 10 mg/mL (34.09 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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。
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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。
ABT-724 70006-24-5 GPCR/G Protein Neuroscience Dopamine Receptor ABT 724 Inhibitor penile erection D4-receptor Dopamine inhibit ABT724 potentiation,side-effect 2 - [(4-吡啶-2-基哌嗪-1-基)甲基]-1H-苯并咪唑 inhibitor