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

SB 243213 hydrochloride 是一種口服有效的，選擇性的，高親和力的 5-HT2C 受體拮抗劑，對(duì)人 5-HT2C 受體的 pKi 為 9.37，pKb 為 9.8。SB 243213 hydrochloride 對(duì)多種神經(jīng)遞質(zhì)受體、酶和離子通道具有超過 100 倍的選擇性。SB 243213 hydrochloride 具有改善的抗焦慮特性，有用于精神分裂癥和運(yùn)動(dòng)障礙的潛力。

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SB 243213 hydrochloride Chemical Structure

SB 243213 hydrochloride Chemical Structure

CAS No. : 200940-23-4

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SB 243213 hydrochloride 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of SB 243213 hydrochloride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

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

體外研究
(In Vitro)

SB 243213 hydrochloride 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 hydrochloride 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.
體內(nèi)研究
(In Vivo)

SB 243213 hydrochloride (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 hydrochloride (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: 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

464.87

Formula

C22H20ClF3N4O2
CAS 號(hào)
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
純度 & 產(chǎn)品資料
參考文獻(xiàn)

SB 243213 hydrochloride 相關(guān)分類

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

The molarity calculator equation

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

質(zhì)量   濃度   體積   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

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SB 243213 hydrochloride
目錄號(hào)：
HY-103112
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