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CAS No.: 204512-90-3

Tecadenoson Catalog No. CSN21258

Synonyms: CVT-510

Tecadenoson is a selective A1 adenosine receptor agonist.

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生物活性

实验方案

技术信息

生物活性

描述Adenosine is an endogenous nucleoside that has potent antiarrhythmic effects on paroxysmal supraventricular tachycardia (PSVT) due to its negative dromotropic effects on the atrioventricular node. In addition to its electrophysiologic effects, adenosine has important effects on vascular smooth muscle cells, inflammatory cells, the central nervous system, and the kidney. Activation of the A1 adenosine receptor accounts for the negative chronotropic and dromotropic effects of adenosine, whereas A2A, A2B and A3 adenosine receptor activation are responsible for such effects as coronary vasodilation, bronchospasm, inhibition of platelet aggregation, and neuronal stimulation^[1].Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. In the atrial-paced isolated heart, Tecadenoson is approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval), a measure of slowing AV nodal conduction (EC50=41 nM) than to increase coronary conductance (EC50=200 nM). At concentrations of Tecadenoson (40 nM) and diltiazem (1 μM) that causes equal prolongation of S-H interval (∼10 ms), diltiazem, but not Tecadenoson, significantly reduces left ventricular developed pressure (LVP) and markedly increases coronary conductance. Tecadenoson shortens atrial (EC50=73 nM) but not the ventricular monophasic action potentials (MAP)^[2]. In atrial-paced anaesthetized guinea-pigs, intravenous infusions of Tecadenoson and diltiazem causes nearly equal prolongations of P-R interval. Tecadenoson (2, 5, 20 μg/kg i.p.) causes a rapid and sustained dose-dependent decrease in NEFA at doses that do not cause bradycardia. Tecadenoson given at 50 μg/kg causes a significant bradycardia (50% decrease in heart rate at 25 min^[3]. Pretreatment of mice with a phosphorylated prodrug of nitrobenzylmercaptopurine riboside, an inhibitor of mENT1, significantly decreased brain exposure to tecadenoson compared with that of the untreated (control) group, suggesting involvement of mENT1 in transport of tecadenoson across the blood-brain barrier (BBB){{ Eve-Irene Lepist,et al. Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1. Drug Metab Dispos . 2013 Apr;41(4):916-22.| https://pubmed.ncbi.nlm.nih.gov/23388705/}}.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00713401	Atrial Fibrillation	Phase 2	Completed	-	United States, California ... more >> CV Therapeutics, Inc. Palo Alto, California, United States, 94304 Collapse <<

参考文献

[1] Jim W Cheung, Bruce B Lerman. CVT-510: a selective A1 adenosine receptor agonist. Cardiovasc Drug Rev. Winter 2003;21(4):277-92.
[2] Snowdy S, et al. A comparison of an A1 adenosine receptor agonist (CVT-510) with diltiazem for slowing of AVnodal conduction in guinea-pig. Br J Pharmacol. 1999 Jan;126(1):137-46.
[3] Fraser H, et al. N-[3-(R)-tetrahydrofuranyl]-6-aminopurine riboside, an A1 adenosine receptor agonist, antagonizes catecholamine-induced lipolysis without cardiovascular effects in awake rats. J Pharmacol Exp Ther. 2003 Apr;305(1):225-31.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9645 mL
- 14.8223 mL
- 29.6446 mL
- 5 mM
- 0.5929 mL
- 2.9645 mL
- 5.9289 mL
- 10 mM
- 0.2964 mL
- 1.4822 mL
- 2.9645 mL

技术信息

CAS号

204512-90-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H19N5O5

运输

蓝冰

分子量

337.33

别名

CVT-510

溶解度

DMSO	130.0 mg/mL (385.4 mM)
Water	insoluble

动物实验配方

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