神经降压素的构效关系研究：9、10和11位的分析
Structure-activity studies with neurotensin: analysis of positions 9, 10 and 11.
作者信息
Quirion R, Regoli D, Rioux F, St-Pierre S
出版信息
Br J Pharmacol. 1980 Aug;69(4):689-92. doi: 10.1111/j.1476-5381.1980.tb07923.x.
Abstract
1 The stimulant effects of neurotensin (NT) and NT analogues modified in positions 9, 10 or 11 were evaluated and compared in two pharmacological preparations: the rat stomach strip and the isolated spontaneously beating atria of guinea-pig. 2 The data derived from our structure-activity study suggest that Arg9 and Pro10 mainly contribute to the affinity of neurotensin for its cardiac and smooth muscle receptors. Tyr11 seems to be more closely involved in the process of receptor activation by NT. 3 The order of potency of some NT analogues modified in position 11 (e.g. [D-Phe11]-NT, [D-Tyr11]-NT) was strikingly different from that described in other systems (e.g. hypothermia test and specific mast cell binding). The importance of this observation is discussed.
摘要
- 在两种药理制剂中评估并比较了神经降压素（NT）及其在第9、10或11位修饰的类似物的兴奋作用：大鼠胃条和豚鼠离体自发搏动心房。2. 我们的构效关系研究得出的数据表明，精氨酸9和脯氨酸10主要影响神经降压素对其心脏和平滑肌受体的亲和力。酪氨酸11似乎更密切参与神经降压素激活受体的过程。3. 一些在第11位修饰的神经降压素类似物（如[D-苯丙氨酸11]-神经降压素、[D-酪氨酸11]-神经降压素）的效价顺序与其他系统（如体温过低试验和特异性肥大细胞结合）中描述的显著不同。讨论了这一观察结果的重要性。
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