Key result
Diphenylalkylamines, diphenylpiperazines, and diphenylbutylpiperdine antischizophrenic drugs are more potent on brain than heart [3H]nitrendipine binding sites, suggesting tissue heterogeneity.
The study demonstrates tissue heterogeneity of calcium channel binding sites, suggesting potential for developing brain-selective calcium channel antagonists.
May support brain-selective calcium antagonists; animal data leaves open human translation and clinical relevance.
Dihydropyridines are potent agents on [3H]nitrendipine binding sites in heart and brain membranes. Like the phenylalkylamines, they are slightly more active on heart than on brain [3H]nitrendipine binding sites. On the other hand, the diphenylalkylamines, the diphenylpiperazines and the antischizophrenic drugs of the diphenylbutylpiperdine type are more potent on brain [3H]nitrendipine binding sites. The findings suggest tissue heterogeneity of [3H]nitrendipine binding sites and the possible development of diphenylbutylpiperidine-diphenylbutylpiperazine analogues that could selectively act on brain calcium channel antagonist binding sites.
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Quirion et al. (1985) studied this question. Calcium channel antagonists and antischizophrenic drugs was evaluated on [3H]nitrendipine binding sites in heart and brain membranes. Diphenylalkylamines, diphenylpiperazines, and diphenylbutylpiperdine antischizophrenic drugs are more potent on brain than heart [3H]nitrendipine binding sites, suggesting tissue heterogeneity.
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