Dilevalol is a "dual-mechanism" antihypertensive reportedly suitable for a wide range of
patients. Its partial beta2-agonist action is expected to induce vasodilation, whereas its
beta1-antagonist component may protect against stress-induced hemodynamic charges
without altering the cardiac output. Dilevalol is the R,R-isomer of labetalol.
Specific competitive antagonist at both α-and β-adrenergic receptor sites. Antihypertensive.
(R,R)-Labetalol is a specific competitive antagonist at both α-and β-adrenergic receptor sites. (R,R)-Labetalol is used as an antihypertensive.
ChEBI: (R,R)-labetalol is a 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide that has 1R,2R-configuration. It is a conjugate base of a dilevalol(1+).
World Health Organization (WHO)
Dilevalol, a beta-adrenoreceptor antagonist, was introduced into
medicine in 1989 for the treatment of hypertension. Shortly afterwards, its use
became associated with isolated cases of hepatic toxicity. Although few cases
were reported, the manufacturer discontinued sales in Japan and Portugal, the
only countries where the drug was marketed, and withdrew applications for
registration elsewhere.
