SB-200646A

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SB-200646A

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:

143797-62-0

SB-200646A 是第一个对5-HT_2B/2C的选择性超过 5-HT_2A的拮抗剂，5-HT_2B，5-HT_2C和 5-HT_2A的pK_i值分别为 7.5、6.9 和 5.2。SB-200646A 具有口服活性，在体内具有电生理和抗焦虑特性。

生物活性

SB-200646A is the first selective5-HT_2B/2Cover 5-HT_2Areceptor antagonist withpK_ivalues of 7.5, 6.9 and 5.2 for5-HT_2B,5-HT_2Cand 5-HT_2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo^[1]^[2].

IC₅₀& Target^[1]^[2]

5-HT_2BReceptor

7.5 (pKi)

5-HT_2CReceptor

6.9 (pKi)

5-HT_2AReceptor

5.2 (pKi)

体外研究
(In Vitro)

SB200646A (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency^[1].

体内研究
(In Vivo)

SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) treatment significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons^[1].
The i.v. administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and % events as bursts in spontaneously active VTA dopaminergic neurons and significantly increases the % events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons^[1].

Animal Model:	Male albino Sprague-Dawley rats (200-225 g at the beginning of treatment and 300-350 g at the time of the experiment)^[1]
Dosage:	20 mg/kg
Administration:	Intravenous injection; daily; for 21 days
Result:	Significantly decreased the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons.

分子量

302.76

性状

Solid

Formula

C₁₅H₁₅ClN₄O

CAS 号

143797-62-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 250 mg/mL(825.74 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.3029 mL	16.5147 mL	33.0295 mL
5 mM	0.6606 mL	3.3029 mL	6.6059 mL
10 mM	0.3303 mL	1.6515 mL	3.3029 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 (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。