Abstract

The binding properties of the calcium antagonist, [ 3H]nitrendipine, were investigated in homogenates of the rat cerebral cortex and myocardium. The specific component of [ 3H]nitrendipine binding was consistent with mass action behavior and was described by a high affinity dissociation constant in the range of 0.1 – 0.3 nM. [ 3H]nitrendipine binding was sensitive to inhibition by other calcium antagonists and by the cations Ca +2 and La +3. The inhibition of [ 3H]nitrendipine binding by verapamil was not of the simple competitive type but resembled allosteric inhibition, suggesting that there are at least two binding sites for calcium antagonists.

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