Central and peripheral action of enkephalin analogues.
Chemical modifications of enkephalins led to analogues with strongly increased biological potency. Compounds such as H-Tyr-DLys(CHO)-Gly-Phe-L-homocysteinethiolactone (Hoe 825) additionally show a remarkable split between central and peripheral action, favouring the stimulation of gastrointestinal contractions. Hoe 825 could, therefore, be useful in the treatment of conditions where gut motility is lacking in humans, especially in adynamic ileus.
D000818:Animals; D004285:Dogs; D004745:Enkephalins / Q000138:chemical synthesis / Q000494:pharmacology*; D005769:Gastrointestinal Motility / Q000187:drug effects; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D007202:Indicators and Reagents; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D010146:Pain / Q000503:physiopathology; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D014828:Vocalization, Animal
D004745:Enkephalins; D007202:Indicators and Reagents