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来自病理性人类甲状旁腺组织的分散甲状旁腺细胞上的组胺受体。

Histamine receptors on dispersed parathyroid cells from pathological human parathyroid tissue.

作者信息

Brown E M

出版信息

J Clin Endocrinol Metab. 1980 Dec;51(6):1325-9. doi: 10.1210/jcem-51-6-1325.

Abstract

The effects of histamine on cAMP accumulation and parathyroid hormone (PTH) release were studied in dispersed cell preparations from pathological parathyroid tissue of 13 patients with primary hyperparathyroidism. Histamine stimulated cAMP accumulation 1.4- to 110-fold in a dose- and time-dependent manner. The increased cAMP content was inhibited by the H2 antagonist cimetidine and the H1 antagonist promethazine, with Ki values of 0.14--0.46 and 0.2--0.37 micrometer, respectively. Moreover, in one cell preparation, the H2 agonist dimaprit stimulated cAMP accumulation 2- to 3-fold, while the H1 agonist 2-pyridylethylamine had no effect on cAMP levels. The potent alpha-and beta-adrenergic antagonists phentolamine and propranolol did not inhibit histamine-stimulated cAMP accumulation significantly. Histamine also caused a dose- and time-dependent increase in PTH release, with a Ka in reasonable agreement with that for cAMP accumulation (0.5--1 vs. 3 micrometer, respectively), indicating that enhanced cAMP accumulation was linked to increased secretion. These results indicate that pathological human parathyroid cells have histamine receptors, probably H2 in subtype, which mediate enhanced cAMP accumulation and PTH release.

摘要

在13例原发性甲状旁腺功能亢进患者的病理性甲状旁腺组织分散细胞制剂中,研究了组胺对环磷酸腺苷(cAMP)积累和甲状旁腺激素(PTH)释放的影响。组胺以剂量和时间依赖性方式刺激cAMP积累1.4至110倍。H2拮抗剂西咪替丁和H1拮抗剂异丙嗪抑制了cAMP含量的增加,其Ki值分别为0.14 - 0.46和0.2 - 0.37微米。此外,在一种细胞制剂中,H2激动剂二甲双胍刺激cAMP积累2至3倍,而H1激动剂2-吡啶乙胺对cAMP水平无影响。强效α和β肾上腺素能拮抗剂酚妥拉明和普萘洛尔并未显著抑制组胺刺激的cAMP积累。组胺还导致PTH释放呈剂量和时间依赖性增加,其Ka与cAMP积累的Ka合理一致(分别为0.5 - 1对3微米),表明cAMP积累增强与分泌增加有关。这些结果表明,病理性人甲状旁腺细胞具有组胺受体,可能是H2亚型,其介导cAMP积累增强和PTH释放增加。

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