product name Urapidil HCl
Description: Urapidil HCl is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. Urapidil is a sympatholytic antihypertensive drug. It acts as an α1-adrenoceptor antagonist and as an 5-HT1A receptor agonist. Although an initial report suggested that urapidil was also an α2-adrenoceptor agonist, this was not substantiated in later studies that demonstrated it was devoid of agonist actions in the dog saphenous vein and the guinea-pig ileum.
References: Br J Pharmacol. 1991 Apr; 102(4): 998–1002.
423.94
Formula
C20H29N5O3.HCl
CAS No.
64887-14-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 24 mg/mL (56.61 mM)
Water: 85 mg/mL (200.5 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Urapidil hydrochloride is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT1A receptors in the central nervous system. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT1A receptors in the central nervous system. Several studies have suggested that oral urapidil is effective and well tolerated when used as second-line therapy in patients with BP inadequately controlled with other agents. Urapidil has also been shown to improve glucose and lipid metabolism in hypertensive patients with concomitant diabetes and/or hyperlipidemia. Kinase Assay: Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A receptor agonist. Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Naunyn Schmiedebergs Arch Pharmacol. 1987 Dec;336(6):597-601; Adv Ther. 2010 Jul;27(7):426-43. |
