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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Cyclic CCK analogues in which positions 28 and 31 have been replaced by lysine residues and whose side chains are bridged by a succinic moiety, were synthesized.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。

相似文献

1
Synthesis of cyclic analogues of cholecystokinin highly selective for central receptors.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。
Int J Pept Protein Res. 1990 May;35(5):441-51. doi: 10.1111/j.1399-3011.1990.tb00071.x.
2
Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds.胆囊收缩素C末端七肽假肽类似物的合成及生物活性。论肽键的重要性。
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Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.对中枢受体具有选择性的CCK8环状及相关线性类似物的合成与结合亲和力
J Med Chem. 1989 Jun;32(6):1184-90. doi: 10.1021/jm00126a007.
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Cyclic cholecystokinin analogues that are highly selective for rat and guinea pig central cholecystokinin receptors.对大鼠和豚鼠中枢胆囊收缩素受体具有高度选择性的环胆囊收缩素类似物。
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Cyclic cholecystokinin analogues with high selectivity for central receptors.对中枢受体具有高选择性的环胆囊收缩素类似物。
Proc Natl Acad Sci U S A. 1988 Mar;85(6):1968-72. doi: 10.1073/pnas.85.6.1968.
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Synthesis and biological evaluation of cholecystokinin analogs in which the Asp-Phe-NH2 moiety has been replaced by a 3-amino-7-phenylheptanoic acid or a 3-amino-6-(phenyloxy)hexanoic acid.天冬氨酸-苯丙氨酸-氨基部分已被3-氨基-7-苯基庚酸或3-氨基-6-(苯氧基)己酸取代的胆囊收缩素类似物的合成及生物学评价
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