- 作者: Lenard R. Forte;朱樂華
- 作者服務機構: 美國密蘇里州密蘇里大學藥理學科; 國立陽明醫拿院生化學科
- 中文摘要: 本項研究是比較天然的牛副甲激素、合成性牛副甲激素片段(1-34)及合成性人副甲激素片段(1-34)對於腎臟皮質部 腺甘酸環化?的激進作用。從有效激進腺甘酸環化?的激素濃度來看,合成性人副甲激素片段只有天然的牛副甲激素1/30到 1/5的效應。從它們對環化?激進的最高程度來比較,合成性人副甲激素片段僅及天然的牛副甲激素效應的一半。多量的合成 性人副甲激素片段也可阻止合成性牛副甲激素片段的效應。因此,合成性人副甲激素片段可當作天然的及合成性牛副甲激素 的部份致活劑及部份對抗劑。由此結果,我們認?人副甲激素片段(1-34)能與腎?皮質部之副甲激素接受器作用而引起激 進腺甘酸環化?的效應。但它對於該接受器的親合力與激進環化?的效能,皆較天然的牛副甲激素或合成性牛副甲激素片段 (1-34)的能力?低。
- 英文摘要: This study compared the biological properties of both native bPTH and synthetic bPTH(l-34) with a synthetic hPTH(l-34) molecule for activation of the renal cortical adenyl cyclase. We found that hPTH(l-34) was about 1/5 to 1/30 as potent as the bPTH molecule. In addition, hPTH(l-34) exhibited the property of a partial agonist in that this peptide activated the renal cortical adenyl cyclase to less than one-half the level that could be achieved by bPTH. Furthermore, the hPTH(l-34) at high concentration (67μg/ml) acted as a competitive antagonist of bPTH (1-34). We conclude that hPTH(l-34) interacts with PTH receptor in the renal plasma membrane but exhibits both reduced affinity for the receptor and reduced efficacy with regard to activation of adenyl cyclase when compared to either native bPTH or synthetic bPTH(l-34).
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