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200940-23-4

中文名称 SB 243213 HYDROCHLORIDE
英文名称 SB 243213 dihydrochloride
CAS 200940-23-4
分子式 C22H19F3N4O2.2HCl
分子量 464.87
MOL 文件 200940-23-4.mol
200940-23-4 结构式 200940-23-4 结构式

基本信息

中文别名
化合物 T12859
英文别名
SB 243213 hydrochloride
SB 243213 dihydrochloride
2,3-Dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-Indole-1-carboxamide dihydrochloride

物理化学性质

储存条件-20°C储存
溶解度在DMSO中溶解至50mM
形态粉末
SB 243213 HYDROCHLORIDE价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2023/03/20HY-103112SB 243213 HYDROCHLORIDE
SB 243213 hydrochloride
200940-23-45mg900元
2023/03/20HY-103112SB 243213 HYDROCHLORIDE
SB 243213 hydrochloride
200940-23-410mg1500元
2023/03/20HY-103112SB 243213 HYDROCHLORIDE
SB 243213 hydrochloride
200940-23-425mg3500元

常见问题列表

生物活性
SB 243213 hydrochloride 是一种口服有效的,选择性的,高亲和力的 5-HT2C 受体拮抗剂,对人 5-HT2C 受体的 pKi 为 9.37,pKb 为 9.8。SB 243213 hydrochloride 对多种神经递质受体、酶和离子通道具有超过 100 倍的选择性。SB 243213 hydrochloride 具有改善的抗焦虑特性,有用于精神分裂症和运动障碍的潜力。
靶点

Human 5-HT 2C Receptor

9.37 (pKi)

human 5-HT 1A Receptor

<5.3 (pKi)

human 5-HT 1B Receptor

5.5 (pKi)

human 5-HT 1D Receptor

6.32 (pKi)

human 5-HT 1E Receptor

<5.4 (pKi)

human 5-HT 1F Receptor

5.35 (pKi)

Human 5-HT 2A Receptor

7.01 (pKi)

human 5-HT 2B Receptor

7.2 (pKi)

Human 5-HT 6 Receptor

6.5 (pKi)

Human 5-HT 7 Receptor

5.64 (pKi)

体外研究

SB 243213 hydrochloride shows little affinity (pK i <6) for cloned human 5-HT 1A , 5-HT 1B , 5-HT 1E , 5- HT 1F and 5-HT 7 receptors. It shows weak affinity (pK i <6.5) for the cloned human 5-HT 1D and D3 receptors and moderate affinity (pK i =6.7) for the cloned human D2 receptor.
SB 243213 hydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels.

体内研究

SB 243213 hydrochloride (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
SB 243213 hydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction.

Animal Model: Male Sprague-Dawley experimentally naive rats (220-300 g)
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: PO; 1 hour pre-test
Result: Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
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