2‐Phenylethyl ester and 2‐phenylethyl amide derivative analogues of the C‐terminal hepta‐ and octapeptide of cholecystokinin

Wiley - Tập 32 Số 5 - Trang 384-395 - 1988
Pierre Fulcrand1, Marc Rodriguez1, Marie‐Christine Galas1, Marie-Françoise Lignon1, Jeanine Laur1, André Aumelas1, Jean Martínez1
1CNRS-INSERM Centre for Pharmacology and Endocrinology, Montpellier, France

Tóm tắt

Syntheses of analogues of the C‐terminal octa‐ and heptapeptide of cholecystokinin are described. These analogues were obtained by replacing the C‐terminal phenylalanine residue by 2‐phenylethyl alcohol or by 2‐phenylethylamine derivatives and by replacing the tryptophan residue by a d‐tryptophan. The CCK‐derivatives were tested for their ability to inhibit binding of labeled CCK‐8 to rat pancreatic acini and to guinea pig brain membranes, and for their action on stimulation of amylase release from rat pancreatic acini. Some of these derivatives appeared to exhibit only part of the CCK‐activity on amylase release, the d‐Trp analogues behaving as CCK‐antagonists.

Từ khóa


Tài liệu tham khảo

10.1021/jm00161a012

10.1111/j.1399-3011.1986.tb03288.x

Lignon M.F., 1987, J. Biol. Chem., 262, 7226, 10.1016/S0021-9258(18)48227-0

Galas M.C., 1988, Gastrin and Cholecystokinin, Chemistry, Physiology and Pharmacology, G176

10.1152/ajpcell.1982.242.3.C250

10.1073/pnas.77.4.2079

Pelaprat D., Life Sci., 37, 2483, 10.1016/0024-3205(85)90605-8

Castro B. Dormoy J.R. Dourtoglou B.Evin G. Selve C.&Ziegler C.(1976)Synthesis 751.

10.1016/S0021-9258(19)83812-7

10.1152/ajpendo.1978.235.6.E743

10.1016/0009-8981(69)90071-0

Thông tin
Thông tin xuất bản

Wiley

Tập 32 Số 5

384-395

Thông tin tác giả