胆囊收缩素受体配体的合成与受体结合亲和力：PD134308的2-和1-吲哚基衍生物
Synthesis and receptor binding affinity of cholecystokinin receptor ligands: 2-and 1-indolyl derivatives of PD134308.
作者信息
Araldi G, Donati D, Oliosi B, Ursini A, van Amsterdam F, Natalini B, Pellicciari R, Tarzia G
机构信息
Glaxo Wellcome S.p.A., Medicines Research Centre, Verona, Italy.
出版信息
Farmaco. 1996 Jul;51(7):471-6.
PMID:8765669
Abstract
The synthesis of two "dipeptoids" structurally related to the CCK-B antagonist CI-988 (PD134308) is described. The 2- and 1-indolyl derivatives 4a, b were prepared in order to define the role of the tryptophan moiety in this series of "dipeptoids". They were evaluated as competitors in the binding of [3H]-CCK8S on guinea pig brain CCK-B receptors.
摘要
描述了两种与CCK - B拮抗剂CI - 988（PD134308）结构相关的“二肽类化合物”的合成。制备了2 - 吲哚基和1 - 吲哚基衍生物4a、b，以确定色氨酸部分在这一系列“二肽类化合物”中的作用。它们被评估为[3H] - CCK8S与豚鼠脑CCK - B受体结合的竞争剂。
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