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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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
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container_end_page 404
container_issue 3
container_start_page 400
container_title Journal of medicinal chemistry
container_volume 42
creator Negri, Lucia
Lattanzi, Roberta
Tabacco, Fabio
Orrù, Luigi
Severini, Cinzia
Scolaro, Barbara
Rocchi, Raniero
description 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.
doi_str_mv 10.1021/jm9810699
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subjects 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
title Dermorphin and Deltorphin Glycosylated Analogues:  Synthesis and Antinociceptive Activity after Systemic Administration
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