Bioorganicheskaia khimiia 1994-07-01

[Synthesis and biological activity of new analogs of beta-casomorphine-5].

M M Sobirov, Sh Kh Khalikov, S S Saidov, M Z Kodirov, S V Zaĭtsev, O N Chichenkov, S D Varfolomeev

Index: Bioorg. Khim. 20(7) , 740-50, (1994)

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Abstract

Four new analogues of beta-cazomorphine-5 modified at the C-end with ethylenediamine- and glycine-containing derivatives were synthesized by the standard method of peptide chemistry (mixed anhydrides, carbodiimide, activated esters): H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-II (I) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-II (II) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-CO-CH3 (III) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-CO-CH2-CH2-COOH (IV) The level of affinity and the degree of selectivity of the peptides towards the mu- and delta-opioid receptors of the rat brain lyophilized membranes were studied by the radioreceptor method. All the new peptides displayed analgetic activity, largely depending upon their structure.