Amino acids and peptides. XIX. Preparation of enkephalin-poly(ethylene glycol) hybrid and evaluation of its analgesic activity.
The poly(ethylene glycol) hybrid of Leu-enkephalin (Tyr-Gly-Gly-Phe-Leu) was prepared and its analgesic activity was examined. Poly(ethylene glycol) #4000 was converted to amino-poly(ethylene glycol) and coupled with the N alpha-protected pentapeptide, followed by trifluoroacetic acid treatment to give the hybrid. The hybrid was soluble in water or various organic solvents. The analgesic activity of Leu-enkephalin was markedly potentiated by hybrid formation with poly(ethylene glycol).
Kawasaki
K
K
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
Maeda
M
M
Yamashiro
Y
Y
Mayumi
T
T
Takahashi
M
M
Kaneto
H
H
D000595:Amino Acid Sequence; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D004743:Enkephalin, Leucine / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D008969:Molecular Sequence Data
D000700:Analgesics; D004743:Enkephalin, Leucine