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Assay for calcium channels

Journal Article · · Methods Enzymol.; (United States)
;

This chapter focuses on biochemical assays for Ca/sup 2 +/-selective channels in electrically excitable membranes which are blocked in electrophysiological and pharmacological experiments by verapamil, 1,4-dihydropyridines, diltiazen (and various other drugs), as well as inorganic di- or trivalent cations. The strategy employed is to use radiolabeled 1,4-dihydropyridine derivatives which block calcium channels with ED/sub 50/ values in the nanomolar range. Although tritiated d-cis-diltiazem and verapamil can be used to label calcium channels, the 1,4-dihydropyridines offer numerous advantages. The various sections cover tissue specificity of channel labeling, the complex interactions of divalent cations with the (/sup 3/H)nimodipine-labeled calcium channels, and the allosteric regulation of (/sup 3/H)nimodipine binding by the optically pure enantiomers of phenylalkylamine and benzothiazepine calcium channel blockers. A comparison of the properties of different tritiated 1,4-dihydropyridine radioligands and the iodinated channel probe (/sup 125/I)iodipine is given.

OSTI ID:
6801688
Journal Information:
Methods Enzymol.; (United States), Journal Name: Methods Enzymol.; (United States) Vol. 109; ISSN MENZA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ALKALINE EARTH METAL COMPOUNDS
AZINES
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
CALCIUM COMPOUNDS
CATIONS
CELL CONSTITUENTS
CELL MEMBRANES
CHANNELING
CHARGED PARTICLES
DATA
DAYS LIVING RADIOISOTOPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EXPERIMENTAL DATA
HETEROCYCLIC COMPOUNDS
INFORMATION
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
IONS
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGANDS
MEMBRANE TRANSPORT
MEMBRANES
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PYRIDINES
RADIOISOTOPES
REACTION KINETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS