SB 243213 HYDROCHLORIDE

SB 243213 HYDROCHLORIDE

中文名称SB 243213 HYDROCHLORIDE
中文同义词化合物 T12859
英文名称SB 243213 dihydrochloride
英文同义词SB 243213 dihydrochloride;SB 243213 hydrochloride;2,3-Dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-Indole-1-carboxamide dihydrochloride;1H-Indole-1-carboxamide, 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-, hydrochloride (1:1)
CAS号200940-23-4
分子式C22H20ClF3N4O2
分子量464.87
EINECS号
相关类别
Mol文件200940-23-4.mol
结构式SB 243213 HYDROCHLORIDE 结构式

SB 243213 HYDROCHLORIDE 性质

储存条件Store at -20°C
溶解度在DMSO中溶解至50mM
形态粉末

SB 243213 HYDROCHLORIDE 用途与合成方法

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。

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)

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.

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.

安全信息

MSDS信息

更新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

SB 243213 HYDROCHLORIDE 上下游产品信息

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