Manidipine

Biological Activity

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.

Customer Product Validations & Biological Datas

	Source	Acta Pharmacol Sin (2007). Figure 5. Manidipine
	Method	Immunohistochemical staining
	Cell Lines	8-OHdG
	Concentrations	50 μm
	Incubation Time
	Results	Manidipine treatment also provided moderate relief of oxidative stress-related DNA injury

	Source	Acta Pharmacol Sin (2007). Figure 3. Manidipine
	Method	insulin staining
	Cell Lines	β-cell
	Concentrations	50 μm
	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

Protocol

Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time

Animal Experiment
Animal models	stroke-prone spontaneously hypertensive rat
Formulation
Dosages	20 mg/kg
Administration	oral

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information

References

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.