1、(R)-(-)-PhenylephrineCat. No.: HY-B0769CAS No.: 59-42-7分式: CHNO分量: 167.21作靶点: Adrenergic Receptor作通路: GPCR/G Protein储存式: Please store the product under the recommended conditions in the COA.BIOLOGICAL ACTIVITY物活性 (R)-(-)-Phenylephrine是选择性的 1-肾上腺素受体激动剂，主要作减充剂 。体外研究 (R)-(-)-Phenylephrine is a selectiv
2、e 1-adrenoceptor agonist with pKi values of 5.86, 4.87 and 4.70 for 1D, 1B and 1A receptors respectively12. Phenylephrine promotes cardiac fibroblast proliferation. Phenylephrine activates CaN and evokes NFAT3 nuclear translocation. It suggests that the Ca(2+)/CaN/NFAT pathway mediates phenylephrine
3、 -induced cardiac fibroblast proliferation, and this pathway might be a possible therapeutic target in cardiac fibrosis3.体内研究 Perfusion of hearts with 100 M phenylephrine causes a rapid (maximal at 10 min) 12-fold activation of two p38-MAPK isoforms. 1-adrenoceptor agonists such as phenylephrine inc
4、rease the contractility of the heart. Phenylephrine also activates SAPKs/JNKs in neonatal ventricular myocytes4. Phenylephrine could increase the alveolar fluid clearance in high tidal volume-ventilated rats and accelerate the absorption of pulmonary edema5.PROTOCOLAnimal Administration 5Rats: A tot
5、al of 170 male Wistar rats are randomLy allocated into 17 groups (n=10) using random number tables. Short-term (40 minutes) mechanical ventilation with high tidal volume is performed to induce lung injury, impair active Na+ transport and lung liquid clearance in the rats. Unventilated rats serves as
6、 controls. To demonstrate the effect of phenylephrine on alveolar fluid clearance, phenylephrine at different concentrations (10, 1, 0.1, 0.01, and 0.001 M) is injected into the alveolar space of the HVT ventilated rats5.MCE has not independently confirmed the accuracy of these methods. They are for
7、 reference only.客户使本产品发表的科研献See more customer validations on www.MedChemEProduct Data Sheet InhibitorsAgonistsScreening Libraries J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Aug 15;1092:220-227.www.MedChemE1REFERENCES1. Ford AP, et al. Pharmacological pleiotropism of the human recombinant al
8、pha1A-adrenoceptor: implications foralpha1-adrenoceptor classification. Br J Pharmacol. 1997 Jul;121(6):1127-35.2. Minneman KP, et al. Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. Mol Pharmacol. 1994 Nov;46(5):929-36.3. Wang J, et al. Phenylephrine promotes cardiac fibrob
9、last proliferation through calcineurin-NFAT pathway. Front Biosci (Landmark Ed). 2016 Jan 1;21:502-13.4. Lazou A, et al. Activation of mitogen-activated protein kinases (p38-MAPKs, SAPKs/JNKs and ERKs) by the G-protein-coupled receptor agonist phenylephrine in the perfused rat heart. Biochem J. 1998
10、 Jun 1;332 ( Pt 2):459-65.5. Li NJ, et al. Effect of phenylephrine on alveolar fluid clearance in ventilator-induced lung injury. Chin Med Sci J. 2013 Mar;28(1):1-6.McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.Tel: 400-820-3792; 021-58955995 Fax: 021-53700325 E-mail: techMedChemEMaster of Small Molecules 您边的抑制剂师www.MedChemE2
