Characterization of a Specific Binding Site for [3H] Nitrendipine in Brain and Heart
Miller, Charles J.
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The binding of the calcium entry blocker [3H] Nitrendipine ([3H] NDP) to brain and heart membranes is characterized.and described. The binding is saturable, specific, and of very high affinity. In brain, binding is enriched in crude nuclear and synaptosomal fractions. The forebrain is enriched in binding, with low levels in the cerebellum and pons. Calcium has a marked stimulatory effect, as does lanthanum and cobalt. Zinc and copper have inhibitory effects, along with EDTA or EGTA treatment. Of the organic compounds tested, only Verapamil inhibits binding, with a non-competitive and incomplete profile. The [3H] NDP binding site is probably a protein since it is sensitive to heat,Trypsin, and sulfhydryl reagents.With honors.