Nisoldipine (Sular) is a calcium channel blocker. It works by affecting the movement of calcium into the cells of the heart and blood vessels. As a result, it relaxes blood vessels and increases the supply of blood and oxygen to the heart while reducing its workload . [1, 2]
|Cell lines||Ventricular myocytes|
|Preparation method||Bathing the myocytes in normal Tyrode's solution, held at -80 mV, and depolarised after 200-ms prepulses (-40mV) to more positive potentials for 500 ms at 0.1 Hz, recording tail currents on repolarisations to -40mV. Exposing the myocytes to 10-100 mM Nisoldipine for 8-10 minutes. Then using an EPC-7 amplifier to record the whole-cell membrane currents.|
|Concentrations||Dissolved in DMSO, final concentration 10-100 μM|
|Incubation time||8-10 minutes|
|Animal models||Male Wistar rats with chronic intragastric ethanol exposure|
|Formulation||Dissolved in DMSO and diluted in saline|
|Administration||Oral every day|
|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 70 mg/mL|
|Related Calcium Channel Products|
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.
Ranolazine is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
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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