| 产品描述： | S-14506 hydrochloride is a potent 5-HT1A agonist, as well as 5-HT2A/2C antagonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent |
| 靶点： |
5-HT Receptor;Dopamine Receptor |
| 体外研究： |
S-14506 hydrochloride 作为5-HT1A受体激动剂，似乎是 G(i) 蛋白依赖性。 S-14506 hydrochloride (0.1 nM-100 μM；10 min) 在百日咳毒素处理的 HeLa 细胞中，对 5-HT 受体的 G 蛋白解偶联状态显示出高亲和力 |
| 体内研究： |
S-14506 hydrochloride (0.2-3.38 mg/kg；IP；单剂量) 剂量依赖性拮抗 Apomorphine (0.75 mg/kg, s.c) 诱导的小鼠刻板攀登和嗅探。S-14506 hydrochloride 阻断多巴胺D2受体显示多巴胺拮抗剂特性。 S-14506 hydrochloride (0.63 mg/kg；SC；单剂量) 在大鼠强迫游泳试验中有活性。它能诱导大鼠一动不动。 Animal Model: Male swiss albino mice (25-30 g) and male Wistar rats (170-230 g) Dosage: 0.2 mg/kg, 0.8 mg/kg, 3.2 mg/kg, 3.8 mg/kg Administration: IP; single dose, 30 min before test Result: Inhibited stereotyped climbing and sniffing behaviours induced by dopamine agonists in mice and on spontaneous behaviours. Animal Model: Male Wistar rats (200-220 g) Dosage: 0.01 mg/kg, 0.63 mg/kg Administration: SC; and gave antagonist 30 min after agonist Result: Induced a dose-dependent imobility in rats. |
| 参考文献： |
1. Protais P, et al. Dopamine receptor antagonist properties of S 14506, 8-OH-DPAT, raclopride and clozapine in rodents. Eur J Pharmacol. 1994 Dec 12;271(1):167-77. 2. Francis C. Colpaert, et al. S 14506: A novel, potent, high-efficacy 5-HT1A agonist and potential anxiolytic agent. 1992, 21-48. 3. Schreiber R, et al. The potent activity of the 5-HT1A receptor agonists, S 14506 and S 14671, in the rat forced swim test is blocked by novel 5-HT1A receptor antagonists. Eur J Pharmacol. 1994 Dec 27;271(2-3):537-41. 4. Assié MB, et al. Correlation between low/high affinity ratios for 5-HT(1A) receptors and intrinsic activity. Eur J Pharmacol. 1999 Dec 10;386(1):97-103. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.253 ml |
11.263 ml |
22.525 ml |
| 5 mM |
0.451 ml |
2.253 ml |
4.505 ml |
| 10 mM |
0.225 ml |
1.126 ml |
2.253 ml |
| 50 mM |
0.045 ml |
0.225 ml |
0.451 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