Tecadenoson (CVT-510) 是选择性的腺苷受体 (A1 adenosine receptor) 激动剂。

Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.

Solid

Target: A1 adenosine receptor

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

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

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[1]. 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.
[2]. 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.

In Vitro: DMSO : 200 mg/mL (592.89 mM; Need ultrasonic)配制储备液