TecadeNOSon 是 A1 腺苷受体的选择性激动剂。
产品描述
Tecadenoson is a selective agonist of A1 adenosine receptor.
体外活性
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) in the atrial-paced isolated heart. Tecadenoson shortens atrial (EC50=73?nM) but not the ventricular monophasic action potentials (MAP). At concentrations of Tecadenoson (40?nM) and diltiazem (1?μM) that induces equal prolongation of S-H interval (~10?ms), diltiazem, but not Tecadenoson, significantly decreases left ventricular developed pressure (LVP) and markedly increases coronary conductance [1].
体内活性
Intravenous infusions of Tecadenoson and diltiazem causes nearly equal prolongations of P-R interval In atrial-paced anaesthetized guinea-pigs. 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 (50 μg/kg) treatment induces a significant bradycardia (50% decrease in heart rate at 25 min) [1][2].
Cas No.
204512-90-3
分子式
C14H19N5O5
分子量
337.33
别名
CVT-510
储存和溶解度
DMSO:155 mg/mL (459.49 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years