ON THE SIGNIFICANCE OF THE C-TERMINAL PRIMARY AMIDE IN CHOLECYSTOKININ

Citation
M. Rolland et al., ON THE SIGNIFICANCE OF THE C-TERMINAL PRIMARY AMIDE IN CHOLECYSTOKININ, Bioorganic & medicinal chemistry letters, 3(5), 1993, pp. 851-854
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
3
Issue
5
Year of publication
1993
Pages
851 - 854
Database
ISI
SICI code
0960-894X(1993)3:5<851:OTSOTC>2.0.ZU;2-X
Abstract
We report on the synthesis of some analogs of the C-terminal heptapept ide of cholecystokinin in which the C-terminal primary amide has been deleted and the L-tryptophan replaced by a D-tryptophan. These analogs were evaluated in vitro for their ability (i) to recognize the CCK re ceptor on rat pancreatic acini and on guinea pig brain membranes; (ii) to stimulate amylase release from rat pancreatic acini. Although prev ious works suggested that the C-terminal primary amide is essential fo r exhibiting a full biological response on pancreatic acini, this stud y does not confirm this hypothesis.