Substances with analgesic activity among dermorphine analogues
Tatiana VoroninaLudmila GuzevatykhLudmila AndreevaTatiana EmelyanovaSergey SeredeninNikolay Myasoedov.Nikolay Myasoedov
State Zakusov Institute of Pharmacology RAMS.Institute of Molecular Genetics RAS.
摘要：<正> The synthesis and study of the structure - activity relationship were carried out in 43 fragments and analogues of dermorphine （aDM） by consecutive replacement individual amino acids residues. The optimal structures for analgesic,thermoregulatory and vasomotor activities were determined. Based on these findings new aDM were purposefully synthetised. including those stereochemically modified Pro in the 6 - th position. The aDM demonstrated a high analgesic activity （used tests as follows: tail flick; acetic acid caused writhing,hot plate,mechanical pressure of the tail,formaline test） The aDM caused no negative influence upon breath,exhibited alow narcogenic potential,and wide safety range.