Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
In the present paper we describe the synthesis of some dermorphin and deltorphin analogues beta-O- and alpha-C-glycosylated on the C-terminal amino acid residue and report their opioid receptor affinity and selectivity as well as their analgesic potency after subcutaneous injection in mice.
Negri
L
L
Institute of Medical Pharmacology, University "La Sapienza" of Rome, P.le Aldo Moro, 5, I-00185 Rome, Italy.
Lattanzi
R
R
Tabacco
F
F
Orrù
L
L
Severini
C
C
Scolaro
B
B
Rocchi
R
R
D000595:Amino Acid Sequence; D000701:Analgesics, Opioid / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D006031:Glycosylation; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007279:Injections, Subcutaneous; D008297:Male; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018847:Opioid Peptides; D011957:Receptors, Opioid / Q000187:drug effects