Calcium in Drug Action by L. Rosenberger, D. J. Triggle (auth.), George B. Weiss

By L. Rosenberger, D. J. Triggle (auth.), George B. Weiss (eds.)

Anyone surveying physiological and pharmacological journals can without difficulty see that the organic activities of calcium ion are of more and more frequent present curiosity. The scope of investi­ gated activities and reactions during which a job for calcium ion is of a few value is so quite a few as to express the impact that calcium ion is in all places and interacts with every little thing. This being so, the problem in modern study is to target research of these activities of calcium ion which, in a few demeanour, impact both major physiological parameters or the style during which pharmacological brokers act. This multi-authored ebook originated from a extra constrained Symposium on "Importance of Calcium as a main Locus of Drug motion" co-chaired on my own and Dr. Frank R. Goodman on the April, 1977 FASEB assembly in Chicago. This Symposium was once geared up based on a perceived want for elevated conversation between 2 employees in numerous parts of Ca +-related examine. within the professional­ cess of choosing the utmost of six components for presentation in the structure supplied, it quickly grew to become obvious that this is able to lead to just a restricted sampling of present study efforts. growth of the variety of components to 14 inside a publication structure the main logical mechanism to supply a extra coherent inter­ disciplinary method of attention of assorted facets of the two roles of Ca + in drug motion. this isn't to indicate that each one rele­ 2 vant Ca +-related parts are surveyed inside this volume.

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Langer (1975). , 1976a; Fabiato and Fabiato, 1977). The controversy centers about whether all the Ca 2 + required for full activation, approximately 90 ~moles Ca 2 +/kg wet wt, comes from superficial sites on the cell or whether intracellular deposits playa role in Ca 2 + release. , 1971; Langer and Frank, 1972). , 1976b). The external portion of the sarcolemma, a region of the cell whose function has been overlooked, is now the focus of studies attempting to locate the Ca 2+ involved in E-C coupling in the heart.

72: 4459. , 1972, A regenerative calcium response in Paramecium, J. Exp. Biol. 56: 667. , 1971, Adenosine triphosphatedependent calcium-binding vesicles: magnesium, calcium, adenosine triphosphatase and sodium-potassium adenosine triphosphatase distributions in dog brain, Arch. Biochem. Biophys. 144: 16. , Ten Eick, R. , McDonald, T. , 1977, On the mechanism underlying the action of 0-600 on slow inward current and tension in mammalian myocardium, Circ. Res. 40: 408. , 1975, The lanthanide ions as structural probes in biological and model systems, Structure and Bonding 22: 1.

23 CALCIUM ENTRY AND ANTAGONISTS SUMMARY There is strong evidence that calcium entry through an electrophysiologically and pharmacologically defined calcium channel is an important calcium entry route in many cells. A group of agents, including verapamil, 0-600 and Nifedipine appear to act as quite selective inhibitors of ion translocation through this channel. However the mechanism(s) of action of these agents remain to be defined. Although these agents appear to be very useful as probes of calcium entry processes in cellular systems, their possible actions at other sites should not be ignored.

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