Literature DB >> 8981054

The dermorphin peptide family.

P Melchiorri1, L Negri.   

Abstract

1. In 1980, the skin of certain frogs belonging to the genus Phyllomedusinae was found to contain two new peptides that proved to be selective mu-opioid agonists. Given the name dermorphins, these were the first members of a peptide family that in the past 15 years has grown to reach a total of seven naturally occurring peptides and nearly 30 synthetic analogs. 2. Dermorphin peptides are potent analgesics in rodents and primates, including man. Some dermorphins can enter the blood-brain barrier and produce central antinociception after peripheral administration. 3. The dermorphin family also includes mu 1-opioid receptor selective agonists that produce intense opioid analgesia, but stimulate pulmonary ventilation. 4. Experiments in rats and mice chronically exposed to dermorphins have shown that not only do they have higher antinociceptive efficacy and potency than morphine, but they are also less likely than morphine to produce tolerance, dependence and opiate side effects.

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Year:  1996        PMID: 8981054     DOI: 10.1016/0306-3623(95)02149-3

Source DB:  PubMed          Journal:  Gen Pharmacol        ISSN: 0306-3623


  12 in total

1.  Synthesis of 3,6-bis[H-Tyr/H-Dmt-NH(CH2)m,n]-2(1H)pyrazinone derivatives: function of alkyl chain length on opioid activity.

Authors:  Kimitaka Shiotani; Tingyou Li; Anna Miyazaki; Yuko Tsuda; Sharon D Bryant; Akihiro Ambo; Yusuke Sasaki; Lawrence H Lazarus; Yoshio Okada
Journal:  Bioorg Med Chem Lett       Date:  2006-09-01       Impact factor: 2.823

2.  Chemical space screening around Phe3 in opioid peptides: Modulating µ versus δ agonism by Suzuki-Miyaura cross-couplings.

Authors:  Tom Willemse; Emilie Eiselt; Karlijn Hollanders; Wim Schepens; Herman W T van Vlijmen; Nga N Chung; Véronique Blais; Brain Holleran; Jean-Michel Longpré; Peter W Schiller; Bert U W Maes; Philippe Sarret; Louis Gendron; Steven Ballet
Journal:  Bioorg Med Chem Lett       Date:  2018-05-12       Impact factor: 2.823

3.  Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).

Authors:  Gianfranco Balboni; Remo Guerrini; Severo Salvadori; Lucia Negri; Elisa Giannini; Sharon D Bryant; Yunden Jinsmaa; Lawrence H Lazarus
Journal:  J Med Chem       Date:  2005-12-29       Impact factor: 7.446

4.  Activity of mu- and delta-opioid agonists in vas deferens from mice deficient in MOR gene.

Authors:  R Maldonado; C Severini; H W Matthes; B L Kieffer; P Melchiorri; L Negri
Journal:  Br J Pharmacol       Date:  2001-04       Impact factor: 8.739

5.  Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.

Authors:  Kimitaka Shiotani; Tingyou Li; Anna Miyazaki; Yuko Tsuda; Toshio Yokoi; Akihiro Ambo; Yusuke Sasaki; Sharon D Bryant; Lawrence H Lazarus; Yoshio Okada
Journal:  Bioorg Med Chem Lett       Date:  2007-08-28       Impact factor: 2.823

6.  Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.

Authors:  Bhaswati Sinha; Zhengyu Cao; Thomas F Murray; Jane V Aldrich
Journal:  J Med Chem       Date:  2009-12-10       Impact factor: 7.446

7.  χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.

Authors:  Olivier Van der Poorten; Robin Van Den Hauwe; Emilie Eiselt; Cecilia Betti; Karel Guillemyn; Nga N Chung; François Hallé; Frédéric Bihel; Peter W Schiller; Dirk Tourwé; Philippe Sarret; Louis Gendron; Steven Ballet
Journal:  ACS Med Chem Lett       Date:  2017-10-04       Impact factor: 4.345

8.  Change in functional selectivity of morphine with the development of antinociceptive tolerance.

Authors:  T A Macey; E N Bobeck; K L Suchland; M M Morgan; S L Ingram
Journal:  Br J Pharmacol       Date:  2014-07-01       Impact factor: 8.739

9.  Behavioral pharmacology of the mixed-action delta-selective opioid receptor agonist BBI-11008: studies on acute, inflammatory and neuropathic pain, respiration, and drug self-administration.

Authors:  Glenn W Stevenson; Denise Giuvelis; James Cormier; Katherine Cone; Phillip Atherton; Rebecca Krivitsky; Emily Warner; Brooke St Laurent; Julio Dutra; Jean M Bidlack; Lajos Szabò; Robin Polt; Edward J Bilsky
Journal:  Psychopharmacology (Berl)       Date:  2020-01-07       Impact factor: 4.530

10.  In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist-neurokinin 1 receptor antagonist chimera.

Authors:  Karel Guillemyn; Patrycja Kleczkowska; Alexandre Novoa; Bart Vandormael; Isabelle Van den Eynde; Piotr Kosson; Muhammad Faheem Asim; Peter W Schiller; Mariana Spetea; Andrzej W Lipkowski; Dirk Tourwé; Steven Ballet
Journal:  Mol Brain       Date:  2012-01-30       Impact factor: 4.041

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