CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives

…, C Durieux, P Boudeau, A Bohme…

文献索引：Corringer; Weng; Ducos; Durieux; Boudeau; Bohme; Roques Journal of Medicinal Chemistry, 1993 , vol. 36, # 1 p. 166 - 172

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被引用次数: 31

摘要

Boc-[(N-Me) Nle31, 1Nal-NH2331CCK,(2)(KI= 2.8 nM), BOC-[P~~~~,~ N~~-NH~~~ ICC& (15)(KI= 14 nM), and Boc-[P~~~~,~ N~~-N (CH~)~ WCK,(17)(KI= 39 nM) displayed good affinities for brain CCK-B receptors and had good selectivity ratios. These pseudopeptides, in which the presence of unnatural and hydrophobic residues is expected to improve their penetration of the central nervous system, were shown to be very resistant to brain ...