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SB 243213 hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SB 243213 hydrochloride图片
CAS NO:200940-23-4
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

SB 243213 hydrochloride is an orally active, selective and high-affinity5-HT2Creceptorantagonist with apKiof 9.37 and apKbof 9.8 for human 5-HT2Creceptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].

IC50& Target[1]

Human 5-HT2CReceptor

9.37 (pKi)

human 5-HT1AReceptor

<5.3 (pKi)

human 5-HT1BReceptor

5.5 (pKi)

human 5-HT1DReceptor

6.32 (pKi)

human 5-HT1EReceptor

<5.4 (pKi)

human 5-HT1FReceptor

5.35 (pKi)

Human 5-HT2AReceptor

7.01 (pKi)

human 5-HT2BReceptor

7.2 (pKi)

Human 5-HT6Receptor

6.5 (pKi)

Human 5-HT7Receptor

5.64 (pKi)

体外研究
(In Vitro)

SB 243213 hydrochloride shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1Fand 5-HT7receptors. It shows weak affinity (pKi<6.5) for the cloned human 5-HT1Dand D3 receptors and moderate affinity (pKi=6.7) for the cloned human D2 receptor[1].
SB 243213 hydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels[1].

体内研究
(In Vivo)

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[1].
SB 243213 hydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction[1].

Animal Model:Male Sprague-Dawley experimentally naive rats (220-300 g)[1]
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.
分子量

464.87

Formula

C22H20ClF3N4O2

CAS 号

200940-23-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.