ISSN:
1432-1912
Keywords:
Calcium channel blocker
;
Radioligand
;
Differential labelling
;
Skeletal muscle
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary Four 1,4-dihydropyridine calcium channel blockers [3H]-nifedipine, [3H]-nitrendipine, [3H]-nimodipine and [3H]-PN 200 110 (Isopropyl 4-(2,1,3,benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimethyl-5-methoxy-carbonylpyridine-3-carboxylate) were employed to label putative calcium channels in guinea-pig hind limb skeletal muscle membranes. The four radioligands differed with respect to the number of sites (B max) which were labelled. The following rank order of B max values was found: PN 200 110 〉 nimodipine = nitrendipine 〉 nifedipine. d-cis-Diltiazem caused an increase in the density of high-affinity binding sites for all four calcium channel blockers. The relative stimulation was smallest for PN 200 110. It is suggested that 1,4-dihydropyridines exhibit different efficacies for induction of a channel state with high affinity for these drugs.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00497674
