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 β-O- and α-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.

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Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 1999-02, Vol.42 (3), p.400-404
Hauptverfasser:	Negri, Lucia, Lattanzi, Roberta, Tabacco, Fabio, Orrù, Luigi, Severini, Cinzia, Scolaro, Barbara, Rocchi, Raniero
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Analgesics Analgesics, Opioid - chemical synthesis Analgesics, Opioid - chemistry Analgesics, Opioid - pharmacology Animals Biological and medical sciences Glycosylation Guinea Pigs In Vitro Techniques Injections, Subcutaneous Male Medical sciences Mice Muscle, Smooth - drug effects Neuropharmacology Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Opioid Peptides Pharmacology. Drug treatments Receptors, Opioid - drug effects
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Beschreibung
Zusammenfassung:	In the present paper we describe the synthesis of some dermorphin and deltorphin analogues β-O- and α-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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm9810699