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Comparative Study
. 1982 Jul-Aug;3(4):697-700.
doi: 10.1016/0196-9781(82)90173-5.

Double-enkephalins--synthesis, activity on guinea-pig ileum, and analgesic effect

Comparative Study

Double-enkephalins--synthesis, activity on guinea-pig ileum, and analgesic effect

A W Lipkowski et al. Peptides. 1982 Jul-Aug.

Abstract

We have synthesized enkephalin analogues in which C-terminal methionine or leucine residues are replaced by a second active fragment of the enkephalin analogue. Synthesis of two compounds is described: in one, two fragments of a D-Ala2-enkephalin analogue are connected by a -NH-NH-bridge, and in the other, three methylene groups are incorporated between the amino groups. The first compound is a very potent inhibitor of electrically induced contractions of guinea-pig ileum and produces a strong analgesia when administered intraperitoneally in mice. The second compound is less active on the ileum and fails to produce analgesia after systemic injection. The double-enkephalins may interact with mu-receptors.

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