Synthesis of O1.5-(beta-D-galactopyranosyl) [DMet2, Hyp5] enkephalin amide, a new highly potent analgesic enkephalin-related glycosyl peptide.
A new series of O-glycosyl enkephalins has been prepared, following a convergent strategy, with high chemical yields. The galactosyl analogue, O1.5-(beta-D-galactopyranosyl) [DMet2, Hyp5] enkephalin amide proved to be one of the most potent in vivo opioid agonists synthesized up to now.
Torres
J L
JL
Peptide Research Section, Centre d'Investigació i Desenvolupament, C.S.I.C., Barcelona, Spain.
Haro
I
I
Valencia
G
G
Reig
F
F
García-Antón
J M
JM
D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D004745:Enkephalins / Q000138:chemical synthesis* / Q000494:pharmacology; D006031:Glycosylation; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D000700:Analgesics; D004745:Enkephalins; C060124:enkephalinamide, Met(2)-Hyp(5)galactopyranosyl-