A PDE4-selective phosphodiesterase inhibitor and an L-type voltage-dependent calcium channel blocker with in vivo antispasmodic efficacy.
Drotaverine (Drotaverin) is an isoquinoline-based PDE4-selective phosphodiesterase (PDE) inhibitor and an L-type voltage-dependent (voltage-operated) calcium channel (L-VDCC or L-VOCC) blocker that exhibits in vivo antispasmodic efficacy without anticholinergic effects.
It is a benzylisoquinoline derivative. Drotaverine acts as a smooth muscle relaxant.[1]
Eksperimental'naia i klinicheskaia farmakologiia, 61(4), 17-19 (1998-10-23)
The study was conducted on experimental models of pain sense induced in mice by exposure to thermic or chemical factors and in rats by exposure to electric factors. Nitrosorbide and no-spa possess a dose-dependent analgesic effect. Both drugs excelled analgin
European journal of pharmacology, 449(1-2), 55-60 (2002-08-07)
The effect of the isoquinoline derivative, drotaverine on the specific binding of [(3)H]nitrendipine and [(3)H]diltiazem to pregnant rat uterine membranes was examined. Drotaverine inhibited the specific [(3)H]nitrendipine and [(3)H]diltiazem bindings with IC(50) values of 5.6 and 2.6 microM, respectively. Saturation
The Journal of pharmacology and experimental therapeutics, 359(3), 442-451 (2016-10-16)
Drotaverine is considered an inhibitor of cyclic-3',5'-nucleotide-phophodiesterase (PDE) enzymes; however, published receptor binding data also support the potential L-type voltage- operated calcium channel (L-VOCC) blocking effect of drotaverine. Hence, in this work, we focus on the potential L-VOCC blocking effect
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