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[ D ‐Ala 2 , Phe ( p ‐NO 2 ) 4 , Leu 5 ]Enkephalin Amide and N α ‐[ D ‐Ala 2 , Leu 5 ]‐Enkephalyl‐N ε ‐Acetyl‐Lysine Amide: Synthesis and Biological Properties of Prospective Enkephalin Cooperative‐Affinity and Photoaffinity Labels. Preliminary communication

1979; Wiley; Volume: 62; Issue: 2 Linguagem: Inglês

10.1002/hlca.19790620219

1522-2675

José V. Castell, Alex N. Eberlé, Verena Marly Kriwaczek, Aung Tun‐Kyi, Peter W. Schiller, Kim Q., Peter Thanei, R. Schwyzer,

Chemical Synthesis and Analysis

Abstract As a study preliminary to attempts at photoaffinity and cooperative affinity labelling of cells and cell membrane vesicles bearing opiate receptors, the title compounds were prepared and tested by rat brain membrane binding assays and by a modified guinea‐pig ileum bio‐assay. The potency of the two compounds in both systems was considerably greater than that of the standard peptide, [Leu 5 ]enkephalin, justifying further work with these and similar compounds.