Morphine-like activity of some N-substituted amides of met-enkephalin.
Opioid activity of a homologous series of met-enkephalin alkylamides was analysed. In guinea pig ileum test, the hexylamide derivative was most active, whereas the isopropylamide derivative was most potent in analgesia test. The results suggest that structural changes of this type at the C-terminus of the pentapeptide improve the opioid activity.
Raghubir
R
R
Patnaik
G K
GK
Dhotre
B J
BJ
Mathur
K B
KB
Dhar
M M
MM
Dhawan
B N
BN
D000577:Amides; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004744:Enkephalin, Methionine / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D009020:Morphine / Q000494:pharmacology
D000577:Amides; D004744:Enkephalin, Methionine; D009020:Morphine