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人甲状旁腺腺瘤腺苷酸环化酶:组胺刺激作用可被西咪替丁阻断。

Human parathyroid adenoma adenylate cyclase: stimulation by histamine that is blocked by cimetidine.

作者信息

Klein I, Lehotay D C, Watson C G, Rogerson B, Levey G S

出版信息

Metabolism. 1981 Jul;30(7):635-7. doi: 10.1016/0026-0495(81)90075-5.

Abstract

Recent evidence suggests that the histamine receptor blocking agent cimetidine can decrease parathyroid hormone release from human parathyroids. To determine the mechanism for inhibition we examined the ability of histamine 1 X 10(-5) moles/liter to stimulate adenylate cyclase in a particulate membrane preparation from 13 human parathyroid glands. Histamine significantly increased adenylate cyclase activity as compared to control; however, the degree of stimulation was variable among the individual tissue samples. Enzyme stimulation was dose dependent over the concentration range of 1 X 10(-7) to 1 X 10(-4) moles/liter. Cimetidine at 1 X 10(-4) moles/liter completely abolished the histamine mediated increase in activity, but did not block the epinephrine-induced stimulation. The identification of an adenylate cyclase system in certain human parathyroid adenomas that is stimulated by histamine and blocked by cimetidine may offer a basis for the pharmacologic alteration of parathyroid hormone secretion.

摘要

最近有证据表明,组胺受体阻断剂西咪替丁可减少人甲状旁腺释放甲状旁腺激素。为确定抑制机制,我们检测了1×10⁻⁵摩尔/升组胺刺激13个人类甲状旁腺颗粒膜制剂中腺苷酸环化酶的能力。与对照组相比,组胺显著增加了腺苷酸环化酶活性;然而,各个组织样本中的刺激程度有所不同。在1×10⁻⁷至1×10⁻⁴摩尔/升的浓度范围内,酶刺激呈剂量依赖性。1×10⁻⁴摩尔/升的西咪替丁完全消除了组胺介导的活性增加,但并未阻断肾上腺素诱导的刺激。在某些人甲状旁腺腺瘤中鉴定出一种受组胺刺激并被西咪替丁阻断的腺苷酸环化酶系统,这可能为甲状旁腺激素分泌的药理学改变提供依据。

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