Tetrapeptide CCK-A Agonists: Effect of Backbone N-Methylations on in vitro and in vivo CCK Activity

…, BR Bianchi, DG Witte, K Shiosaki, CW Lin

Index: Holladay; Kopecka; Miller; Bednarz; Nikkel; Bianchi; Witte; Shiosaki; Chun Wel Lin; Asin; Nadzan Journal of Medicinal Chemistry, 1994 , vol. 37, # 5 p. 630 - 635

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Citation Number: 22

Abstract

N-Methylation of backbone amide bonds was conducted on a tetrapeptide that had been identified previously (Shiosaki, K.; et al. J. Med. Chem. 1991, 34, 2387-2842) as a potent and selective CCK-A agonist. No-Methylation at the position corresponding to A~ p 3~(CCK- 33 numbering) was consistent with high affinity, efficacy, and selectivity for the CCK-A receptor. Combination of this (N-Me) Asp with the (N-Me) Phe modification also provided a ...