- 作者: 陶寶綠; 張立人; 李賢鎧; 羅浩
- 作者服務機構: 國防醫學院藥理學科; 加州大學舊金山分校藥理學科
- 中文摘要:
鴉片類藥物的作用,目前認為是經由與鴉片受體結合後所產生,但是,關於鴉片受體的分子大小、結構等,尚不很
清楚。有許多學者以不同的方法將鴉片受體由細胞膜上溶解下來,經過純化後,所得的分子量由23,000到750,000,可
謂差異性非常大。本實驗乃應用高輻射能去活化的技術,以不同劑量(0.5~10 Mrad)的鈷60輻射能,照射經處理所得的
鼠腦胞膜,使受體失去不同程度之活性,此種活性喪失的速率乃與標的物分子量的大小有關。因此,可由此法來決定細
胞膜上鴉片受體,在不同離子(方程式無法摘錄)或核?酸〔Gpp(NH)p〕的影響下,其功能單位的分子大小。
結果發現,在(方程式無法摘錄),Gpp(NH)p同時存在下,所得的鴉片受體分子量為313,000 ± 13,500
;只有Na存在或Na與Gpp(NH)p同時存在下為165,000 ± 8,500;只有Gpp(NH)p存在下為217,000 ± 6,600;只有
存在下為286,000 ± 60,900。本文提出可能的模式,解釋上述分子量變化之情況。 - 英文摘要: Opioids, like other drugs, are thought to initiate their effects by associating with their specific re-ceptors. However, very little is known about the opioid receptor as a molecular entity. The binding com-ponents have been solubilized in detergent and purified by different approaches, but the molecular size ofsoluble opioid receptor complexes reported by different groups varied from 23,000 to 750,000. In thisstudy, the technique of radiation inactivation by gamma rays was used to investigate the apparent size ofthe opioid receptor in rat brain membranes under different conditions. The molecular sizes of opioid re-ceptor complexes were estimated as 313,000 ± 13,500 in the presence of (方程式無法摘錄) enkephalin,NaCl and Gpp(NH)p; as 165,000 ± 8,500 in the presence of NaCI only, or of both NaCl and Gpp(NH)p; as217,000 ± 6,600 in the presence of Gpp(NH)p only; and as 286,000 ± 60,900 in the presence of MgC1 only.A simple model has been proposed to explain these different apparent target sizes of opioid receptorsobtained under different conditions.
- 中文關鍵字: opioid receptors; sizes; radiation inactivation; target analysis
- 英文關鍵字: --