2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB 243213 dihydrochloride

SB 243213 dihydrochloride 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 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。

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SB 243213 dihydrochloride Chemical Structure

SB 243213 dihydrochloride Chemical Structure

CAS No. : 1780372-25-9

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SB 243213 dihydrochloride 的其他形式现货产品:

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Other Forms of SB 243213 dihydrochloride:

SB 243213 dihydrochloride 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. 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-HT2C Receptor

9.37 (pKi)

human 5-HT1A Receptor

<5.3 (pKi)

human 5-HT1B Receptor

5.5 (pKi)

human 5-HT1D Receptor

6.32 (pKi)

human 5-HT1E Receptor

<5.4 (pKi)

human 5-HT1F Receptor

5.35 (pKi)

Human 5-HT2A Receptor

7.01 (pKi)

human 5-HT2B Receptor

7.2 (pKi)

Human 5-HT6 Receptor

6.5 (pKi)

Human 5-HT7 Receptor

5.64 (pKi)

体外研究
(In Vitro)

SB 243213 dihydrochloride shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows weak affinity (pKi<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pKi=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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SB 243213 dihydrochloride 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C22H21Cl2F3N4O2
CAS 号
性状

固体

颜色

Light yellow to yellow

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)

纯度 & 产品资料

纯度: ≥99.0%

COA (272 KB)

产品使用指南 (1538 KB)
参考文献

SB 243213 dihydrochloride 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB 2432131780372-25-9SB243213SB-2432135-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorOrally5-hydroxytryptamineanxiolyticprofileschizophreniamotordisordersneurotransmitterreceptorsenzymesionchannelsInhibitorinhibitorinhibit

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目录号：
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