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

SB 243213 

目录号: HY-103112B
产品使用指南

SB 243213 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 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 Chemical Structure

SB 243213 Chemical Structure

CAS No. : 200940-22-3

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Description

SB 243213 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 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)

In Vitro

SB 243213 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].

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.
Molecular Weight

428.41

Formula

C₂₂H₁₉F₃N₄O₂

CAS No.

200940-22-3

SMILES

O=C(N1CCC2=C1C=C(C(F)(F)F)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SB 243213SB243213SB-2432135-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorOrally5-hydroxytryptamineanxiolyticprofileschizophreniamotordisordersInhibitorinhibitorinhibit

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SB 243213
目录号:
HY-103112B
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