对中枢受体具有高度选择性的胆囊收缩素环类似物的合成。

Synthesis of cyclic analogues of cholecystokinin highly selective for central receptors.

作者信息

Rodriguez M, Amblard M, Galas M C, Lignon M F, Aumelas A, Martinez J

机构信息

CNRS-INSERM Center for Pharmacology and Endocrinology, Montpellier, France.

出版信息

Int J Pept Protein Res. 1990 May;35(5):441-51. doi: 10.1111/j.1399-3011.1990.tb00071.x.

DOI:10.1111/j.1399-3011.1990.tb00071.x

PMID:2376470

Abstract

Cyclic CCK analogues in which positions 28 and 31 have been replaced by lysine residues and whose side chains are bridged by a succinic moiety, were synthesized. They were tested for their ability to inhibit the binding of 125I-BH-CCK-8 to isolated rat pancreatic acini and to guinea pig brain membranes. These cyclic CCK-analogues were compared to the potent CCK analogue Boc-[Nle28,31]-CCK-7 and to Boc-Trp-Leu-Asp-Phe-NH2, analogue of CCK-4. These cyclic compounds appeared to be highly selective for central CCK receptors.

摘要

合成了环状CCK类似物，其中第28位和31位已被赖氨酸残基取代，其侧链由琥珀酸部分桥接。测试了它们抑制125I-BH-CCK-8与分离的大鼠胰腺腺泡和豚鼠脑膜结合的能力。将这些环状CCK类似物与强效CCK类似物Boc-[Nle28,31]-CCK-7以及CCK-4的类似物Boc-Trp-Leu-Asp-Phe-NH2进行比较。这些环状化合物似乎对中枢CCK受体具有高度选择性。