HISTAMINE H1 RECEPTOR OCCUPANCY TRIGGERS INOSITOL PHOSPHATES AND INTRACELLULAR CALCIUM MOBILIZATION IN HUMAN NONPIGMENTED CILIARY EPITHELIAL-CELLS
HISTAMINE H1 RECEPTOR OCCUPANCY TRIGGERS INOSITOL PHOSPHATES AND INTRACELLULAR CALCIUM MOBILIZATION IN HUMAN NONPIGMENTED CILIARY EPITHELIAL-CELLS
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DOI：
10.3109/02713689109013851
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发表时间：
1991-07-01
影响因子：
2
通讯作者：
POLANSKY, JR
中科院分区：
文献类型：
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作者：
CROOK, RB;BAZAN, NG;POLANSKY, JR
用组胺激动剂和拮抗剂研究了组胺对培养的人睫状体非色素上皮（NPE）细胞磷酸肌醇形成和胞内Ca ~（2+）升高的刺激作用。 对H-1组胺受体亚型特异性的激动剂比所测试的H-2特异性激动剂的效力高20至200倍，并且在肌醇磷酸刺激中的效力是组胺的5-16%。 H-1拮抗剂在阻断组胺刺激磷酸肌醇方面比H-2拮抗剂强10，000倍。 H-1激动剂也模仿和H-1拮抗剂抑制组胺引起的细胞内Ca 2+升高。 第一阶段的Ca 2+响应组胺在很大程度上是独立的细胞外Ca 2+，而第二阶段需要细胞外Ca 2+。 组胺升高细胞内Ca 2+（EC 50 = 10 μ M，最大值为100 μ M）和肌醇磷酸盐（EC 50 = 2 μ M，最大值为100 μ M）的剂量反应曲线相似。 这些数据支持NPE组胺受体作为H-1受体与磷酸肌醇和细胞内Ca 2+升高相关的表征。
Agonists and antagonists of histamine were used to characterize the stimulation of inositol phosphates formation and elevation of intracellular Ca2+ by histamine in cultured non-pigmented epithelial (NPE) cells from human ciliary body. Agonists specific for the H-1 histamine receptor subtype were 20- to 200-fold more potent than the H-2-specific agonists tested, and 5-16% as potent as histamine in inositol phosphates stimulation. An H-1 antagonist was 10,000-fold more potent than an H-2 antagonist in blocking histamine stimulation of inositol phosphates. H-1 agonists also mimicked and H-1 antagonists inhibited the elevation of intracellular Ca2+ by histamine. The first phase of the Ca2+ response to histamine was largely independent of extracellular Ca2+ while the second phase required extracellular Ca2+. Dose-response curves for histamine elevation of intracellular Ca2+ (EC50 = 10-mu-M, maximum at 100-mu-M)and inositol phosphates (EC50 = 2-mu-M, maximum at 100-mu-M) were similar. These data support the characterization of the NPE histamine receptor as an H-1 receptor linked to elevation of inositol phosphates and intracellular Ca2+.