Product Intro

Urapidil 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.

Function

Urapidil hydrochloride is suitable for various types of hypertension, hypertensive crisis, severe and extremely severe hypertension, refractory hypertension, and for controlling perioperative hypertension, including hypertension patients with liver and renal insufficiency, coronary heart disease, diabetes and pulmonary hypertension caused by chronic obstructive pulmonary disease. It also has a certain effect on prostatic hypertrophy.

Application

1.α1-Adrenergic antagonist; derivative of Uracil (U801000). Antihypertensive.
2.Antihypertensive;Serotonergic receptor agonist
3.a1-Adrenergic antagonist; derivative of Uracil. Antihypertensive