Enkephalin tetra-and pentapeptide analogues containing acetyl group in the 2-position.Synthesis and investigation of biological activity in vivo and in vitro

摘要

Enkephalins-endogenous opioid pentapeptides,natural ligands of the opioid receptor have attracted considerable attention since their discovery in 1975,most notably,with respect to the appearance of the new principal approach in analgesic design.The general scheme for searching of new enkephalin analogues presented in full in includes the detailed study of conformational properties of natural enkephalin resulting in the assumption of the biologically active conformation of enkephalin.Besides,structural similarity between endogenous and exogenous opiates found almost immediately after the opening of enkephalins gives a unique possibility for one more approach for designing new analogues of enkephalins.