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

Sulamserod  (Synonyms: RS-100302)

目录号: HY-101668
产品使用指南

Sulamserod 是一种 5-HT4 receptor 拮抗剂,具有抗心律失常的功效。

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Sulamserod Chemical Structure

Sulamserod Chemical Structure

CAS No. : 219757-90-1

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.

IC50 & Target

5-HT4 Receptor

 

体内研究
(In Vivo)

Sulamserod (30 mg/kg) prolongs mean ERP (11568 versus 14667 ms, P,0.01) and wavelength (8.360.9 versus 9.960.8 cm, P,0.01), reduces dispersion of ERP (1565 versus 861 ms, P,0.01), and minimally slows conduction velocity (7264 versus 6765 cm/s, P,0.01) in pigs. Sulamserod produces no ventricular electrophysiological effects. Sulamserod terminates atrial flutter in 6 of 8 animals and atrial fibrillation in 8 of 9 animals and prevents reinduction of sustained tachycardia in all animals[1].

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

分子量

445.96

Formula

C19H28ClN3O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
Animal Administration
[1]

After completion of baseline electrophysiological measurements and induction of sustained AFL or AF, the 5-HT4 receptor antagonist RS-100302 is administered in a dose of 30 μg/kg over 10 minutes. This dose of RS-100302 is previously determined to maximally inhibit 5-HT-induced tachycardia in pigs. After completion of drug infusion, each animal is monitored for 20 minutes to observe arrhythmia response. If AFL or AF does not terminate spontaneously within 20 minutes after completion of drug infusion, sinus rhythm is restored by burst pacing or DC cardioversion, respectively. Electrophysiological measurements are then repeated as during control, and a venous blood sample is drawn for plasma levels of RS-100302. Attempts are then made to reinduce AFL or AF as performed at control. Reinduced arrhythmias are defined as sustained if lasting >10 minutes, nonsustained if lasting >30 seconds but <10 minutes, or none if lasting <30 seconds. Sustained arrhythmias are terminated after 10 minutes by burst pacing or DC cardioversion. Cisapride is then administered at a dose of 0.1 mg/kg over 10 minutes, after which electrophysiological measurements are repeated. Attempts are again made to reinduce AFL or AF, and the same definitions as those used after RS-100302 infusion regarding sustained, nonsustained, or no arrhythmias are applied. The study is then terminated, and animals are euthanized by an overdose of pentobarbital (150 mg/kg)[1].

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

参考文献
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  • 稀释计算器

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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HY-101668
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