SB 243213 dihydrochloride

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CAS NO:

1780372-25-9

SB 243213 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride 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 dihydrochloride 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 dihydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels^[1].

体内研究
(In Vivo)

SB 243213 dihydrochloride (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 dihydrochloride (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:	p.o.; 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

501.33

性状

Solid

Formula

C₂₂H₂₁Cl₂F₃N₄O₂

CAS 号

1780372-25-9

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)