Etilefrine

Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output^[1][2][3]. In Vitro:Etilefrine (10 μM; 1-2 h) significantly activates AMPKα (Thr172) phosphorylation and inhibits Akt (Ser473) phosphorylation in PC-3 and 293T cells^[1]. In Vivo:Etilefrine (0.1 mg/kg; intravenous injection; single dose) causes an increase in blood pressure and heart rate in anesthetized mongrel dog models, which may be related to the constriction of resistance vessels and the increase in cardiac contractility and heart rate^[2].
Etilefrine (50 μg/kg, 200 μg/kg; intravenous injection; single dose) can increase cardiac output, right heart filling pressure and blood pressure at rest and reduce total peripheral resistance in New Zealand white rabbit experimental models. Total peripheral resistance increased at a dose of 200 μg/kg^[3].