Celiprolol

Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with K_i values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure^[1][4]. In Vitro: Celiprolol (0-3 mM, 90 min) is uptaken by human small intestinal transporter OATP-A/1A2 in Xenopus Laevis oocytes^[5].
Celiprolol (10 μM, 0-50 min) is transported across human intestinal epithelial (Caco-2) cells by mediation of multiple transporters including P-glycoprotein^[6]. In Vivo: Celiprolol (Oral administration, 100 mg/kg/day for 31 days) improves endothelial function in the arteries of in Otsuka Long-Evans Tokushima Fatty (OLETF) rats, and restores it 4 weeks after endothelial denudation in the arteries of OLETF rats^[2].
Celiprolol (Treated in drinking water, 10 mg/kg/day for 5 weeks) suppresses VCAM-1 expression by inhibition of oxidative stress, NF-κB, signal transduction, and increases eNOS via stimulation of the PI3K-Akt pathway, and improves cardiovascular remodeling in deoxycorticosterone acetate (DOCA)-salt hypertensive rats^[3].