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Overview
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Background
Phenylephrine HCl is a selective agonist of α1-adrenergic receptor [1].
α1-adrenergic receptors are one of the three main families of adrenergic receptors regulating the actions of norepinephrine and epinephrine [1].
Phenylephrine exhibits significant selectivity for α1-adrenergic receptors subtypes. When tested with hamster α1B-AR, bovine α1C-AR , and rat αA/D-AR, Phenylephrine showed inhibition of I-BE binding with pKi values of 4.87, 4.70 and 5.86 for α1B, α1C and αA/D receptors respectively and intrinsic activities of activating cloned α1-adrenergic receptors subtypes with pEC50 values of 6.47, 6.77 and 7.01 for α1B, α1C and αA/D receptors respectively [1].
In high tidal volume ventilated rats, although 1×10-9 mol/L phenylephrine did not raise alveolar fluid clearance, alveolar space injection of phenylephrine at different concentrations of 1×10-5, 1×10-6, 1×10-7 and 1×10-8 increased the alveolar fluid clearance and promoted the absorption of pulmonary edema in a dose-dependent manner. [2].[1]. Minneman KP, Theroux TL, Hollinger S, et al. Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. Molecular Pharmacology. 1994, 46(5):929-36.
[2]. Li NJ, Gu X, Li W, et al. Effect of phenylephrine on alveolar fluid clearance in ventilator-induced lung injury. Chinese Medical Sciences Journal. 2013, 28(1):1-6.
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