SB 243213

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SB 243213

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:

200940-22-3

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

SB 243213 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 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 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 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 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 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 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].

体内研究
(In Vivo)

SB 243213 (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 (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

428.41

性状

Solid

Formula

C₂₂H₁₉F₃N₄O₂

CAS 号

200940-22-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL(291.78 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.3342 mL	11.6711 mL	23.3421 mL
5 mM	0.4668 mL	2.3342 mL	4.6684 mL
10 mM	0.2334 mL	1.1671 mL	2.3342 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。