PGT-β小鼠松果体瘤细胞中β2-肾上腺素能受体的药理学特性
Pharmacological characterization of beta2-adrenoceptor in PGT-beta mouse pineal gland tumour cells.
作者信息
Suh B C, Chae H D, Chung J H, Kim K T
机构信息
Department of Life Science and Basic Science Research Institute, Pohang University of Science and Technology, Republic of Korea.
出版信息
Br J Pharmacol. 1999 Jan;126(2):399-406. doi: 10.1038/sj.bjp.0702248.
Abstract
- The adrenoceptor in a mouse pineal gland tumour cell line (PGT-beta) was identified and characterized using pharmacological and physiological approaches. 2. Adrenaline and noradrenaline, adrenoceptor agonists, stimulated cyclic AMP generation in a concentration-dependent manner, but had no effect on inositol 1,4,5-trisphosphate production. Adrenaline was a more potent activator of cyclic AMP generation than noradrenaline, with half maximal-effective concentrations (EC50) seen at 175+/-22 nM and 18+/-2 microM for adrenaline and noradrenaline, respectively. 3. The addition of forskolin synergistically stimulated the adrenaline-mediated cyclic AMP generation in a concentration-dependent manner. 4. The pA2 value for the specific beta2-adrenoceptor antagonist ICI-118,551 (8.7+/-0.4) as an antagonist of the adrenaline-stimulated cyclic AMP generation were 3 units higher than the value for the betaI-adrenoceptor antagonist atenolol (5.6+/-0.3). 5. Treatment of the cells with adrenaline and forskolin evoked a 3 fold increase in the activity of serotonin N-acetyltransferase with the peak occurring 6 h after stimulation. 6. These results suggest the presence of beta2-adrenoceptors in mouse pineal cells and a functional relationship between the adenylyl cyclase system and the regulation of N-acetyltransferase expression.
摘要
- 采用药理学和生理学方法对小鼠松果体肿瘤细胞系（PGT-β）中的肾上腺素能受体进行了鉴定和特性分析。2. 肾上腺素能受体激动剂肾上腺素和去甲肾上腺素以浓度依赖方式刺激环磷酸腺苷（cAMP）生成，但对肌醇1,4,5-三磷酸的产生无影响。肾上腺素比去甲肾上腺素更有效地激活cAMP生成，肾上腺素和去甲肾上腺素的半数最大有效浓度（EC50）分别为175±22 nM和18±2 μM。3. 加入福斯高林以浓度依赖方式协同刺激肾上腺素介导的cAMP生成。4. 特异性β2肾上腺素能受体拮抗剂ICI-118,551作为肾上腺素刺激的cAMP生成拮抗剂的pA2值（8.7±0.4）比β1肾上腺素能受体拮抗剂阿替洛尔的值（5.6±0.3）高3个单位。5. 用肾上腺素和福斯高林处理细胞使血清素N-乙酰基转移酶活性增加3倍，刺激后6小时达到峰值。6. 这些结果表明小鼠松果体细胞中存在β2肾上腺素能受体，且腺苷酸环化酶系统与N-乙酰基转移酶表达的调节之间存在功能关系。
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