SB 243213 hydrochloride

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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。

CAS NO:

200940-23-4

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价
50mg	询价
100mg	询价

SB 243213 hydrochloride 是一种口服有效的，选择性的，高亲和力的5-HT_2C受体拮抗剂，对人 5-HT_2C受体的pK_i为 9.37，pK_b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-HT_2Creceptorantagonist with apK_iof 9.37 and apK_bof 9.8 for human 5-HT_2Creceptor. 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-HT_2CReceptor

9.37 (pKi)

human 5-HT_1AReceptor

<5.3 (pKi)

human 5-HT_1BReceptor

5.5 (pKi)

human 5-HT_1DReceptor

6.32 (pKi)

human 5-HT_1EReceptor

<5.4 (pKi)

human 5-HT_1FReceptor

5.35 (pKi)

Human 5-HT_2AReceptor

7.01 (pKi)

human 5-HT_2BReceptor

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 (pK_i<6) for cloned human 5-HT_1A, 5-HT_1B, 5-HT_1E, 5- HT_1Fand 5-HT₇receptors. It shows weak affinity (pK_i<6.5) for the cloned human 5-HT_1Dand D3 receptors and moderate affinity (pK_i=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.