Endogenous expression of histamine H1 receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP
Endogenous expression of histamine H1 receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP
复制标题
C6 胶质瘤细胞中组胺 H1 受体的内源表达与磷酸肌醇水解功能耦合：环 AMP 的调节
DOI：
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发表时间：
1994
影响因子：
7.3
通讯作者：
S. Hill
中科院分区：
文献类型：
--
作者：
M. Peakman;S. Hill
1研究了组胺受体激动剂和拮抗剂对大鼠C6胶质瘤细胞磷脂水解的影响。2组胺H1受体刺激导致[3 H]-肌醇预标记细胞中总[3 H]-肌醇磷酸盐积累的浓度依赖性增加。激动剂效力的等级顺序为组胺（EC 50 = 24 μm）> Nα-甲基组胺（EC 50 = 31 μm）> 2-噻唑乙胺（EC 50 = 91 μm）。3对0.1 mm组胺的反应以浓度依赖性方式被H1-拮抗剂美托咪胺（表观Kd = 1 nm）和（+）-扑尔敏（表观Kd = 4 nm）拮抗。此外，（−）−氯苯那敏的效力比其（+）-立体异构体低两个数量级以上。4用forskolin（10 μm，EC 50 = 0.3 μm），isoprenaline（1 μm，EC 50 = 4 nm）或rolipram（0.5 μm）增加细胞内cAMP的积累，分别显著降低组胺介导的（0.1 μm）磷酸肌醇反应37%，43%和26%。相比之下，1，9-二脱氧毛喉素没有增加环AMP的积累，对磷酸肌醇对组胺的反应没有影响。这些数据表明C6神经胶质瘤细胞中存在功能性偶联的内源性组胺H1受体。此外，结果还表明，H1受体介导的磷脂水解被这些细胞中环AMP水平的升高所抑制。
1 The effects of histamine receptor agonists and antagonists on phospholipid hydrolysis in rat‐derived C6 glioma cells have been investigated. 2 Histamine H1 receptor‐stimulation caused a concentration‐dependent increase in the accumulation of total [3H]‐inositol phosphates in cells prelabelled with [3H]‐myo‐inositol. The rank order of agonist potencies was histamine (EC50 = 24 μm) > Nα‐methylhistamine (EC50 = 31 μm) > 2‐thiazolylethylamine (EC50 = 91 μm). 3 The response to 0.1 mm histamine was antagonized in a concentration‐dependent manner by the H1‐antagonists, mepyramine (apparent Kd = 1 nm) and (+)‐chlorpheniramine (apparent Kd = 4 nm). In addition, (−)−chlorpheniramine was more than two orders of magnitude less potent than its (+)‐stereoisomer. 4 Elevation of intracellular cyclic AMP accumulation with forskolin (10 μm, EC50 = 0.3 μm), isoprenaline (1 μm, EC50 = 4 nm) or rolipram (0.5 μm), significantly reduced the histamine‐mediated (0.1 μm) inositol phosphate response by 37%, 43% and 26% respectively. In contrast, 1,9‐dideoxyforskolin did not increase cyclic AMP accumulation and had no effect on the phosphoinositide response to histamine. 5 These data indicate the presence of functionally coupled, endogenous histamine H1 receptors in C6 glioma cells. Furthermore, the results also indicate that H1 receptor‐mediated phospholipid hydrolysis is inhibited by the elevation of cyclic AMP levels in these cells.
两种神经母细胞瘤中激动剂诱导的毒蕈碱受体丧失与刺激的磷酸肌醇周转脱敏之间的关系：方法学考虑。
影响因子：
3.5
作者：
A. K. Thompson;S. Fisher
通讯作者：
S. Fisher
乙酰胆碱刺激 C62B 神经胶质瘤细胞中花生四烯酸的选择性释放和再酯化以及磷酸肌醇和甘油磷酸肌醇的积累。
DOI：
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发表时间：
1987
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
DeGeorge,JJ;Ousley,AH;McCarthy,KD;Lapetina,EG;Morell,P
通讯作者：
Morell,P