MedChemExpress - Model Phentolamine mesylate -65-28-1

Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction[1][2][3].

Phentolamine mesylate

MCE China：Phentolamine mesylate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0362A

CAS：65-28-1

Synonyms：Phentolamine methanesulfonate

Purity：99.87%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.

In Vitro：Phentolamine (0.1-1 μM) inhibits the response to Clonidine in rat ileum, with the pA2 and pKB of 7.92 and 8.07, respectively[3]. Phentolamine (10-70 μg/mL; 48 h) inhibits proliferation of HDMECs and HBMECs in a dose-dependent manner, with IC50s of 50 μg/mL and 30 μg/mL without toxicity, respectively[4]. Phentolamine (10-20 or 20-40 μg/mL; 12-48 h) signi cantly delays scratch wound closure of HBMECs and HDMECs in a dose-dependent manner[4]. Phentolamine (30 or 50 μg/mL; 4-12 h) inhibits tube formation of HBMECs and HDMECs[4].

In Vivo：Phentolamine (1 mg/kg; i.v.) produces hypotension and tachycardia in rats[4].

IC50 & Target：α adrenergic receptor

References：

[1]. Gould L, et, al. Phentolamine. Am Heart J. 1976 Sep;92(3):397-402. [Content Brief]

[2]. Goldstein I, et, al. Oral phentolamine: an alpha-1, alpha-2 adrenergic antagonist for the treatment of erectile dysfunction. Int J Impot Res. 2000 Mar;12 Suppl 1:S75-80. [Content Brief]

[3]. Liu L, et, al. Evidence for functional alpha 2D-adrenoceptors in the rat intestine. Br J Pharmacol. 1996 Mar;117(5):787-92. [Content Brief]

[4]. Pan L, et, al. Phentolamine inhibits angiogenesis in vitro: Suppression of proliferation migration and differentiation of human endothelial cells. Clin Hemorheol Microcirc. 2017;65(1):31-41. [Content Brief]

[5]. Fioretti AC, et, al. Renal and femoral venous blood flows are regulated by different mechanisms dependent on α-adrenergic receptor subtypes and nitric oxide in anesthetized rats. Vascul Pharmacol. 2017 Dec;99:53-64. [Content Brief]

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MedChemExpress - Model Phentolamine mesylate -65-28-1

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Phentolamine mesylate