[42] Assay for calcium channels

摘要: Publisher Summary This chapter focuses on biochemical assays for Ca 2+ -selective channels in electrically excitable membranes, which are blocked electrophysiological and pharmacological experiments by verapamil, 1,4-dihydro-pyridines, diltiazem (and various other drugs), as well inorganic di- or trivalent cations. The strategy employed is to use radiolabeled 1,4-dihydropyridine derivatives, block calcium with ED 50 values the nanomolar range. affinity their drug receptor site within channel can be very high. Their interaction membrane components, including sodium neurotransmitter receptors, negligible, makes choice of tissue preparation purity respective fraction less critical. A spectrum compounds exists that regulate function from blockade opening. also discusses specificity labeling, complex interactions divalent cations nimodipine-labeled channels, allosteric regulation nimodipine binding optically pure enantiomers phenylalkylamine benzothiazepine blockers.