頁籤選單縮合
題 名 | Effect of (-)-cis-3-[2-Hydroxy-4-(1,1-dimethyl-heptyl)phenyl]-trans-4-(3-hydroxypropyl)cyclohexanol (CP55,940) on Intracellular Ca[fec7] Levels in Human Osteosarcoma Cells |
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作 者 | Lu,Yih-chau; Su,Warren; Jiann,Bang-ping; Chang,Hong-tai; Huang,Jong-khing; Jan,Chung-ren; | 書刊名 | 中國生理學雜誌 |
卷 期 | 45:3 2002.09[民91.09] |
頁 次 | 頁95-100 |
分類號 | 418.4 |
關鍵詞 | CP55,940; [Ca[fec7]]i; MG63 cells; Osteoblast; Thapsigargin; |
語 文 | 英文(English) |
英文摘要 | The study was undertaken to explore the effect of CPP, 940 ((-)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hydroxypropyl)cyclohexanol), a drug commonly used as a CB1/CB2 cannabinoid receptor agonist, on intracellular free □ levels (□) in MG63 human osteoblast-like epithelial cells. □ was measured in suspended cells by using the fluorescent dye fura-2 as an indicator. At concentrations between 2-20 μM, CP55,940 increased □ in a concentration-dependent manner with an E□ of 8 μM. The □ signal comprised an initial rise, a slow decay, and a sustained phase. CP55940 (10 <M)-induced □ signal was not altered by 5 μM of two cannabinoid receptor antagonists (AM-251, N-(piperidin-1-yl)-5-(4-iodophenyl)-4-m3thyl-N-morphoinyl-1H-pyrazole-3-carboxamide). Extracellular □ removal decreased the maximum value of the □ signals by 50%. CP55,940 induced quench of fura-2 fluorescence by M□ (50μM), suggesting the presence of C□ influx across the plasma membrane. CP55, 940 (10 μM)-induced □ increase in □ –free medium was inhibited by 84% by pretreatment with 1μM thapsigargin, an endoplasmic reticulum □ pump inhibitor. Conversely, pretreatment with 10 μM CP55,940 in □ –free medium abolished thapsigargin-induced □ increase. At 1 μM, nifedipine, verapamil, and diltiazem did not alter CP55, 940 (10 μM)-induced □ increase. CP55,940 (20 μM)-induced □ release was not affected when phospholipase C was inhibited by 2 μM U73122 (1-(6-)(17β-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione). CP55,940 (20 μM) did not induce acute cell death after incubation for 30 min as assayed by trypan blue exclusion. Collectively, CP55,940 induced significant □ increases in osteoblasts by releasing store □ from thapsigargin-sensitive stores and by causing □ entry. The CP55, 940’s action appears to be independent of stimulation of CB1 cannabinoid receptors. |
本系統中英文摘要資訊取自各篇刊載內容。