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Calcium uptake studies of 1,4-dihydropyridine agonists into rabbit aortic smooth muscle cells in culture

Journal Article · · Life Sci.; (United States)
; ;
The effects of the three dihydropyridine calcium channel agonists (/plus minus/)BAY K 8644, (+)202-791 and (/plus minus/)CGP 28392 on /sup 45/Ca/sup + +/ uptake were studied in cultures of rabbit aortic smooth muscle cells. At 10/sup /minus/7/M each agonist enhanced /sup 45/Ca/sup + +/ uptake in 15-50 mM K/sup +/ but had no effect on the basal /sup 45/Ca/sup + +/ uptake at 5 mM K/sup +/. At the uptake threshold of 15 mM K/sup +/ each agonist potentiated /sup 45/Ca/sup + +/ uptake in a dose-dependent manner with half maximal effects at 2.4 nM for (/plus minus/)BAY K 8644, 22 nM for (+)202-791 and 18 nM for (/plus minus/)CGP 28392. The agonists showed no significant antagonistic activity. Responses were antagonized competitively by nifedipine and non-competitively by (/plus minus/)D-600. The /sup 45/Ca/sup + +/ uptake-dose response curves and the half maximal effects of the three agonists were over the same range of concentrations as their inhibition of (/sup 3/H)nitrendipine binding to rat ventricular receptor membrane preparations. The data suggest that these cells mimic the calcium uptake by the intact aorta better than commercial vascular smooth muscle lines or cardiac cells.
Research Organization:
G.D. Searle and Company, Skokie, IL (USA)
OSTI ID:
6101764
Journal Information:
Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 44:23; ISSN LIFSA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ALKALINE EARTH ISOTOPES
ALKALINE EARTH METAL COMPOUNDS
ANIMAL CELLS
ANIMALS
AORTA
ARTERIES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BLOOD VESSELS
BODY
CALCIUM 45
CALCIUM COMPOUNDS
CALCIUM ISOTOPES
CARDIOVASCULAR SYSTEM
CELL CONSTITUENTS
CELL MEMBRANES
DAYS LIVING RADIOISOTOPES
DOSE-RESPONSE RELATIONSHIPS
ENZYME INHIBITORS
EVEN-ODD NUCLEI
INTERMEDIATE MASS NUCLEI
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
MUSCLES
NUCLEI
ORGANIC COMPOUNDS
ORGANS
PORINS
PROTEINS
RABBITS
RADIOISOTOPES
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
UPTAKE
VERTEBRATES