PMID: 6112742Feb 1, 1981Paper

alpha-adrenergic antagonists as possible calcium channel inhibitors

Proceedings of the National Academy of Sciences of the United States of America
D Atlas, M Adler

Abstract

The effects of various organic Ca2+ channel inhibitors were investigated on the binding of the alpha 1-antagonist 3H-labeled 2-[(2',6'-dimethoxyphenoxyethyl)aminomethyl]-1,4-benzodioxane ([3H]WB-4101) to membranes from rat brain and neuroblastoma-glioma hybrid cells (NG108-15). As found by monitoring binding of [3H]WB-41-1, the Ca2+ channel inhibitors methoxyverapamil (D600), verapamil, and the nifedipine analogue YC-93 bind to two different sites in rat brain: a high-affinity site (dissociation constant Kd = 2.9 nM and binding capacity B = 360 fmol/mg of protein) and a low-affinity site (Kd = 260 nM and B = 2700 fmol/mg of protein). In NG108-15 cells, where no alpha 1 receptors were detected with [3H]WB-4101, the Ca2+ antagonists were found to bind to nonadrenergic sites in the membrane with a capacity B = 976 fmol/mg of protein. The binding of Ca2+ antagonists to [3H]WB-41-1 sites led to the investigation of WB-4101 as a Ca2+ inhibitor by electrophysiological techniques. WB-4101 depressed the amplitude and reduced the rate of rise of the CA2+ spike with an affinity slightly greater than that observed for D600. The concentration for 50% inhibition of the Ca2+ spike amplitude was 48 microM for WB-4101 and 80 microM for D600. Th...Continue Reading

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Citations

Sep 1, 1983·Naunyn-Schmiedeberg's Archives of Pharmacology·E Müller-Schweinitzer
Sep 1, 1982·Cellular and Molecular Neurobiology·R P Ebstein, J W Daly
Sep 24, 1985·European Journal of Pharmacology·J J Descombes, J C Stoclet
Mar 26, 1984·Life Sciences·R J Miller, S B Freedman
Mar 1, 1990·Pharmacology, Biochemistry, and Behavior·A ArgiolasG L Gessa
Aug 1, 1986·Psychiatry Research·S L DubovskyJ Murphy
Feb 9, 1989·Biochimica Et Biophysica Acta·G K ScottC A Tse
May 1, 1995·Progress in Neuro-psychopharmacology & Biological Psychiatry·A LenziG B Cassano
May 1, 1982·Molecular and Cellular Endocrinology·P N de GraanF C van de Veerdonk
Jan 1, 1983·General Pharmacology·P BolliF R Bühler
Jan 1, 1985·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·J Nwoga, E E Bittar
Jan 1, 1985·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·E E Bittar, G Chambers
Feb 13, 2001·European Journal of Pharmacology·G PalitM P Dubey
Sep 16, 1982·The New England Journal of Medicine·W G StricklandJ H Exton
Aug 31, 1984·The American Journal of Medicine·A M KatzA J Pappano
Sep 1, 1985·Biological Psychiatry·S L DubovskyD Schrier
Dec 1, 1985·The American Journal of Emergency Medicine·A M KatzA J Pappano
Jan 1, 1984·Annals of the New York Academy of Sciences·F X Witkowski, P B Corr
Feb 1, 1982·European Journal of Clinical Investigation·F R Bühler, L Hulthén
Aug 1, 1990·Annals of Emergency Medicine·S GandoM Kubota
Feb 1, 1983·American Heart Journal·D TzivoniS Stern
Jan 1, 1983·Biochemical Pharmacology·P V Kaplita, D J Triggle

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