| Description: |
Nitrendipine is a calcium channel blocker with marked vasodilator action.Nitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension to decrease blood pressure. Nitrendipine blocked Ca2+ currents very potently, with half-block by subnanomolar concentrations. The concentration dependence of block had the form expected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM. In contrast, when cells were held at hyperpolarized potentials, nitrendipine blocked Ca2+ currents much less potently (Kd approximately equal to 700 nM). Nitrendipine, a potent analogue of nifedipine, binds in a reversible and saturable manner to partially purified guinea-pig heart membranes. [3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response. |
