胃肠道神经降压素受体：11位芳香羟基对肽效力的贡献。
Gastrointestinal neurotensin receptors: contribution of the aromatic hydroxyl group in position 11 to peptide potency.
作者信息
Donoso M V, Huidobro-Toro J P, St Pierre S
出版信息
Br J Pharmacol. 1986 Mar;87(3):483-5. doi: 10.1111/j.1476-5381.1986.tb10189.x.
Abstract
Neurotensin structural analogues on tyrosine11 were tested in vitro to determine their ability to contract the fundus or relax the intestine. The rank order of potency was: neurotensin greater than [Phe11]-neurotensin greater than [D-Tyr11]-neurotensin greater than [D-Phe11]-neurotensin. All peptides behaved as full agonists. It is concluded that tyrosine11 is part of the neurotensin pharmacophore; the hydroxyl group increases the affinity not the intrinsic activity of the peptide at the receptor.
摘要
对酪氨酸11位上的神经降压素结构类似物进行了体外测试，以确定它们使胃底收缩或使肠道舒张的能力。效价顺序为：神经降压素＞[苯丙氨酸11] - 神经降压素＞[D - 酪氨酸11] - 神经降压素＞[D - 苯丙氨酸11] - 神经降压素。所有肽均表现为完全激动剂。结论是，酪氨酸11是神经降压素药效基团的一部分；羟基增加了该肽在受体处的亲和力而非内在活性。
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