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• W2068525573 abstract "Three objectives were defined when planning this study: (i) to identify binding sites for [125I]-apamin in intact bovine adrenal medulla chromaffin cells and to estimate their density and selectivity; (ii) to determine whether apamin modified the release of catecholamines evoked by brief pulses of dimethylphenylpiperazinium (DMPP, 1 or 5 μM for 10 sec), histamine (10 μM for 10 sec) or high K+ (20, 35 or 70 mM for 10 sec) applied to superfused cells; and (iii) to test whether apamin affected the profiles of the changes in cytosolic Ca2+ concentrations [Ca2+]i obtained in suspensions of cells loaded with fura-2 and stimulated with DMPP or histamine. At equilibrium, increasing concentrations of [125I]-apamin gave a saturation curve whose Scatchard transformation produced a Kd of 132 pM and a Bmax of 0.72 fmol/106 cells. Quinine, tetraethylammonium, charybdotoxin or glibenclamide (blockers of various subtypes of K+ channels) did not inhibit [125I]apamin binding. Binding was blocked by apamin and by d-tubocurarine, two blockers of small-conductance Ca2+-activated K+ channels (SK channels). The number of binding sites for [125I]apamin amounted to approx. 900 per single chromaffin cell, 0.72 sites per μm2 surface area. Apamin (1 μM) enhanced the secretory response to histamine (10 μM), DMPP (1 or 5 μM) and high K+ (20 or 35 mM) by 2–3-fold. The response to 70 mM K+, however, was unaffected. Apamin also enhanced the peak [Ca2+]i increase produced by DMPP or histamine by approx. 30%. Overall, these results strongly support the hypothesis that under physiological conditions, SK channels control some of the electrical activity of chromaffin cells and indirectly, the opening of voltage-dependent Ca2+ channels, the access of Ca2+ to the secretory machinery and the rate of catecholamine release to the circulation from the intact adrenal gland." @default.
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• W2068525573 date "1995-05-01" @default.
• W2068525573 modified "2023-09-27" @default.
• W2068525573 title "Density of apamin-sensitive Ca2+-dependent K+ channels in bovine chromaffin cells: Relevance to secretion" @default.
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• W2068525573 doi "https://doi.org/10.1016/0006-2952(94)00524-p" @default.
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