Manidipine dihydrochloride (CV-4093) is a hydrochloride salt of manidipine that is a lipophilic, third-generation, highly vasoselective dihydropyridine calcium antagonist with an IC50 of 2.6 nM. Manidipine dihydrochloride (CV-4093) causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. Manidipine dihydrochloride (CV-4093) is used clinically as an antihypertensive. Manidipine dihydrochloride (CV-4093) suppressed the DNA synthesis of vascular smooth muscle cells (VSMC) dose dependently at concentrations of more than 10 nM. Mandipine hydrochloride (1 uM) suppressed proliferation of VSMC to 50% of the control value. Manidipine hydrochloride stimulated the synthesis of GAG at concentrations above 0.01 nM. Manidipine hydrochloride (10 nM) stimulated synthesis of glycosaminoglycans (GAG) to 450% of control.
|Cell lines||Mesangial cells|
|Preparation method||Measuring the mitogenic effect by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, seeding 1 ?105 quiescent cells into a 25-mL cell culture bottle and keeping in low serum medium (0.1% FCS). On the next day, the cells are preincubated for 3 hours with Manidipine (10 nM) followed by stimulation with PDGF-BB (10 ng/mL) or incubated with low serum medium abone. Replacing the medium each day, and counting the cells at days 1, 3 and 5.|
|Incubation time||Days 1, 3 and 5|
|Animal models||Normotensive male Wistar-Kyoto rats and male stroke-prone SHR|
|Dosages||1 mg/kg, 3 mg/kg and 10 mg/kg|
|Administration||Administered via p.o.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
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