O'Farrell M, Marley P D
Department of Pharmacology, University of Melbourne, Parkville, Victoria, Australia.
Cell Calcium. 1999 Mar;25(3):209-17. doi: 10.1054/ceca.1999.0025.
Histamine stimulates catecholamine release and tyrosine hydroxylase activity in a Ca(2+)-dependent manner in bovine adrenal chromaffin cells. The role of voltage-sensitive Ca2+ channels in these two responses has been investigated. Using an EC50 concentration of histamine, 1 microM, catecholamine release was enhanced by (+/-)BayK8644, and partially inhibited by nitrendipine and omega-agatoxin IVA, blockers of L- and P/Q-type Ca2+ channels. omega-Conotoxin GVIA gave small and variable inhibitory effects. With a maximal histamine concentration, 10 microM, similar results were obtained except that now omega-conotoxin GVIA reliably reduced release. In contrast, neither (+/-)BayK8644 nor any of the individual Ca2+ channel antagonists had any significant effect on tyrosine hydroxylase (TOH) activation induced by either an EC50 or a maximal concentration of histamine. When high concentrations of nitrendipine, omega-conotoxin GVIA and omega-agatoxin IVA were combined with omega-conotoxin MVIIC (a non-selective blocker of N, P and Q channels) to block voltage-sensitive Ca2+ channels in these cells, release induced by K+ depolarization was completely blocked. Release caused by histamine, however, was substantially reduced but not abolished. The combination of antagonists also only partially inhibited TOH activation by histamine. The results show that the G protein-coupled receptor agonist histamine activates several different types of voltage-sensitive Ca2+ channels in chromaffin cells to mediate its cellular effects. Histamine may also activate additional pathways for Ca2+ entry. The results also suggest that the manner by which Ca2+ controls release and TOH activation once it has entered chromaffin cells through these channels are different.
组胺以Ca(2+)依赖的方式刺激牛肾上腺嗜铬细胞中儿茶酚胺的释放和酪氨酸羟化酶的活性。研究了电压敏感性Ca2+通道在这两种反应中的作用。使用1 microM的组胺EC50浓度,(+/-)BayK8644增强了儿茶酚胺的释放,而尼群地平和ω-芋螺毒素IVA(L型和P/Q型Ca2+通道阻滞剂)则部分抑制了儿茶酚胺的释放。ω-芋螺毒素GVIA产生的抑制作用较小且不稳定。使用10 microM的组胺最大浓度时,得到了类似的结果,只是此时ω-芋螺毒素GVIA可靠地降低了释放量。相比之下,(+/-)BayK8644和任何一种单独的Ca2+通道拮抗剂对EC50或最大浓度组胺诱导的酪氨酸羟化酶(TOH)激活均无显著影响。当高浓度的尼群地平、ω-芋螺毒素GVIA和ω-芋螺毒素IVA与ω-芋螺毒素MVIIC(N、P和Q通道的非选择性阻滞剂)联合使用以阻断这些细胞中的电压敏感性Ca2+通道时,K+去极化诱导的释放被完全阻断。然而,组胺引起的释放量大幅减少但并未消除。拮抗剂的组合也仅部分抑制了组胺对TOH的激活。结果表明,G蛋白偶联受体激动剂组胺激活嗜铬细胞中几种不同类型的电压敏感性Ca2+通道以介导其细胞效应。组胺还可能激活其他Ca2+内流途径。结果还表明,Ca2+一旦通过这些通道进入嗜铬细胞后,其控制释放和TOH激活的方式是不同的。