An α1-AR antagonist and partial 5-HT1A agonist; selectively binds to α1- over α2-ARs (IC50s = 0.74 and 42 μM

Urapidil (hydrochloride) – 500 mg

Brand:
Cayman
CAS:
64887-14-5
Storage:
-20
UN-No:
Non-Hazardous - /

Urapidil is an antagonist of α1-adrenergic receptors (α1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A.{52077,52078} 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.{52077} Urapidil inhibits cAMP accumulation induced by forskolin in calf hippocampus as a functional model for 5-HT1A receptors (EC50 = 390 nM).{52079} It is also a β1-AR antagonist that inhibits the positive chronotropic response induced by isoproterenol (Item No. 15592) in isolated rat atria (pA2 = 6.05).{52080} 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.{52081}  

 

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SKU: 29004 - 500 mg Category:

Description

An α1-AR antagonist and partial 5-HT1A agonist; 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; inhibits forskolin-induced cAMP accumulation in calf hippocampus as a functional model for 5-HT1A receptors (EC50 = 390 nM); inhibits the isoproterenol-induced positive chronotroptic response in isolated rat atria (pA2 = 6.05); lowers MAP in anesthetized cats at 1 μmol/kg, i.v.

Formal name: 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione monohydrochloride

Synonyms: 

Molecular weight: 423.9

CAS: 64887-14-5

Purity: ≥98%

Formulation: A solid

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