Manidipine (Manyper) is a lipophilic, third-generation, highly vasoselective dihydropyridine calcium antagonist with an IC50 of 2.6 nM. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. It is used clinically as an antihypertensive. At a holding potential of −37 mV, manidipine decreased the Ca2+ current at concentrations above 0.1 nM, and abolished it at 100 nM. The voltage-dependent effect of manidipine on the Ca2+ current may explain the weak negative inotropism of manidipine in ventricular muscles, and provide an electrophysiological basis for its vascular selectivity.
|Source||Acta Pharmacol Sin (2007). Figure 5. Manidipine|
|Results||Manidipine treatment also provided moderate relief of oxidative stress-related DNA injury|
|Source||Acta Pharmacol Sin (2007). Figure 3. Manidipine|
|Incubation Time||6 weeks|
|Results||β-cell mass was quite low in the db/db control group, and it was rescued greatly after 6 weeks’ treatment by both candesartan 1 mg/kg and 10 mg/kg|
|Animal models||stroke-prone spontaneously hypertensive rat|
|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 100 mg/mL|
Manidipine improves spermatogenesis in the stroke-prone spontaneously hypertensive rat.
Akagashi K, et al. J Androl. 1997 Mar-Apr;18(2):210-6. PMID: 9154516.
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L-Phenylalanine is an antagonist at α2δ calcium channels with a Ki of 980 nM.
Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure.
Lercanidipine hydrochloride is a calcium channel blocker of the dihydropyridine class.
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