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抑制剂描述:

产品名称:Phenylephrine hydrochloride

产品别名:见爱必信官网

英文别名:Phenylephrine hydrochloride

靶点:Adrenergic Receptor

CAS:61-76-7

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Phenylephrine hydrochloride used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure. Phenylephrine has recently been marketed as a substitute for pseudoephedrine.

溶解性:DMSO :20.4 mg/mL (100 mM)
Water :20.4 mg/mL (100 mM)

体外研究:

Phenylephrine causes a rapid translocation of PKC-epsilon (EC50 = 0.9 mM) but the proportion lost from the soluble fraction is less than with ET-1. Phenylephrine at pCa 7 causes a dose-dependent increase in contractile force of the hyperpermeable cells, which is reversible on addition of phentolamine. Phenylephrine also protects cardiomyocytes against subsequent 24 h treatment with hypoxia and serum deprivation. Phenylephrine prevents the down-regulation of Bcl-2 and Bcl-X mRNA/protein and induces hypertrophic growth. Phenylephrine-mediated protection is abrogated by the phosphatidylinositol 3-kinase (PI 3-kinase) inhibitor wortmannin and is mimicked by the caspase-9 peptidic inhibitor LEHD-fmk. Phenylephrine stimulates phosphoinositide (PI) hydrolysis, cell growth, and expression of several genes often associated with cardiac hypertrophy. Phenylephrine (1 礛) markedly potentiates HGF-induced hepatocyte DNA synthesis and proliferation. Phenylephrine (10 mM) reversibly increases I(Ca,L) (51.3%; n = 40) and shifted peak I(Ca,L) activation voltage by -10 mV. Phenylephrine also increases local, subsarcolemmal SR Ca2+ release via IP3-dependent signaling. Phenylephrin-induced NOi release requires stimulation of both PI-3K/Akt and IP3-dependent Ca2+ signaling. Phenylephrine-induced NOi release is inhibited by each of 1 mM prazocin, 10 mM L-NIO, 10 mM W-7, 10 mM LY294002, 2 mM H-89, 10 mM ryanodine, 5 mM thapsigargin, 2 mM 2-APB or 10 mM xestospongin C.

体内研究:Perfusion of hearts with 100 μM phenylephrine causes a rapid (maximal at 10 min) 12-fold activation of two p38-MAPK isoforms. α1-adrenoceptor agonists such as phenylephrine increase the contractility of the heart. Phenylephrine also activates SAPKs/JNKs in neonatal ventricular myocytes. Phenylephrine could increase the alveolar fluid clearance in high tidal volume-ventilated rats and accelerate the absorption of pulmonary edema.

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