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34661-75-1COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1.ClKTMLZVUAXJERAT-UHFFFAOYSA-N34661-75-1、64887-14-5DTXSID2045812CHEMBL1256716White to Off-White Crystalline Powder
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개요Urapidil is an antagonist of α1-adrenergic receptors (α1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. It selectively binds to α1- over α2-ARs (IC50s = 0.74 and 42 μM, respectively) and to 5-HT1A over 5-HT1B and 5-HT2 receptors (IC50s = 0.4, 20.4, and >10 μM, respectively) in rat cortex. Urapidil inhibits cAMP accumulation induced by forskolin in calf hippocampus as a functional model for 5-HT1A receptors (EC50 = 390 nM). It is also a β1-AR antagonist that inhibits the positive chronotropic response induced by isoproterenol in isolated rat atria (pA2 = 6.05). Urapidil (1 μmol/kg, i.v.) lowers mean arterial pressure (MAP) in anesthetized cats, an effect that is reduced by central administration of the 5-HT1A receptor antagonist spiroxatrine.
용도a1-Adrenergic antagonist; derivative of Uracil. Antihypertensive
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