Literature DB >> 34826881

Strategies towards safer opioid analgesics-A review of old and upcoming targets.

Balazs R Varga1, John M Streicher2, Susruta Majumdar1.   

Abstract

Opioids continue to be of use for the treatment of pain. Most clinically used analgesics target the μ opioid receptor whose activation results in adverse effects like respiratory depression, addiction and abuse liability. Various approaches have been used by the field to separate receptor-mediated analgesic actions from adverse effects. These include biased agonism, opioids targeting multiple receptors, allosteric modulators, heteromers and splice variants of the μ receptor. This review will focus on the current status of the field and some upcoming targets of interest that may lead to a safer next generation of analgesics.
© 2021 The British Pharmacological Society.

Entities:  

Year:  2021        PMID: 34826881      PMCID: PMC9133275          DOI: 10.1111/bph.15760

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   9.473


  149 in total

1.  6'-Guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.

Authors:  Marie-Laure Rives; Mary Rossillo; Lee-Yuan Liu-Chen; Jonathan A Javitch
Journal:  J Biol Chem       Date:  2012-06-26       Impact factor: 5.157

2.  Absence of conditioned place preference or reinstatement with bivalent ligands containing mu-opioid receptor agonist and delta-opioid receptor antagonist pharmacophores.

Authors:  Natalie R Lenard; David J Daniels; Philip S Portoghese; Sandra C Roerig
Journal:  Eur J Pharmacol       Date:  2007-03-03       Impact factor: 4.432

3.  Biphalin, an enkephalin analog with unexpectedly high antinociceptive potency and low dependence liability in vivo, selectively antagonizes excitatory opioid receptor functions of sensory neurons in culture.

Authors:  K F Shen; S M Crain
Journal:  Brain Res       Date:  1995-12-01       Impact factor: 3.252

4.  Heat shock protein 90 inhibitors block the antinociceptive effects of opioids in mouse chemotherapy-induced neuropathy and cancer bone pain models.

Authors:  Carrie Stine; Deziree L Coleman; Austin T Flohrschutz; Austen L Thompson; Sanket Mishra; Brian S Blagg; Tally M Largent-Milnes; Wei Lei; John M Streicher
Journal:  Pain       Date:  2020-04-10       Impact factor: 6.961

5.  TRV130 partial agonism and capacity to induce anti-nociceptive tolerance revealed through reducing available μ-opioid receptor number.

Authors:  Samuel Singleton; Daniel T Baptista-Hon; Emily Edelsten; Kirsty S McCaughey; Ewan Camplisson; Tim G Hales
Journal:  Br J Pharmacol       Date:  2021-03-02       Impact factor: 8.739

6.  CNS penetration of the opioid glycopeptide MMP-2200: a microdialysis study.

Authors:  Omar S Mabrouk; Torsten Falk; Scott J Sherman; Robert T Kennedy; Robin Polt
Journal:  Neurosci Lett       Date:  2012-11-02       Impact factor: 3.046

7.  Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.

Authors:  Abdelfattah Faouzi; Rajendra Uprety; Ivone Gomes; Nicolas Massaly; Attila I Keresztes; Valerie Le Rouzic; Achla Gupta; Tiffany Zhang; Hye Jean Yoon; Michael Ansonoff; Abdullah Allaoa; Ying Xian Pan; John Pintar; Jose A Morón; John M Streicher; Lakshmi A Devi; Susruta Majumdar
Journal:  J Med Chem       Date:  2020-11-10       Impact factor: 7.446

8.  Inhibition of Hsp90 in the spinal cord enhances the antinociceptive effects of morphine by activating an ERK-RSK pathway.

Authors:  David I Duron; Wei Lei; Natalie K Barker; Carrie Stine; Sanket Mishra; Brian S J Blagg; Paul R Langlais; John M Streicher
Journal:  Sci Signal       Date:  2020-05-05       Impact factor: 8.192

9.  Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects.

Authors:  Ram Kandasamy; Todd M Hillhouse; Kathryn E Livingston; Kelsey E Kochan; Claire Meurice; Shainnel O Eans; Ming-Hua Li; Andrew D White; Bernard P Roques; Jay P McLaughlin; Susan L Ingram; Neil T Burford; Andrew Alt; John R Traynor
Journal:  Proc Natl Acad Sci U S A       Date:  2021-04-20       Impact factor: 11.205

10.  Development of a bioavailable μ opioid receptor (MOPr) agonist, δ opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.

Authors:  Henry I Mosberg; Larisa Yeomans; Jessica P Anand; Vanessa Porter; Katarzyna Sobczyk-Kojiro; John R Traynor; Emily M Jutkiewicz
Journal:  J Med Chem       Date:  2014-03-26       Impact factor: 7.446

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  3 in total

Review 1.  Quantitative Systems Pharmacology and Biased Agonism at Opioid Receptors: A Potential Avenue for Improved Analgesics.

Authors:  Andrea Bedini; Elisabetta Cuna; Monica Baiula; Santi Spampinato
Journal:  Int J Mol Sci       Date:  2022-05-04       Impact factor: 6.208

2.  Modulation of the MOP Receptor (μ Opioid Receptor) by Imidazo[1,2-a]imidazole-5,6-Diones: In Search of the Elucidation of the Mechanism of Action.

Authors:  Dominik Straszak; Agata Siwek; Monika Głuch-Lutwin; Barbara Mordyl; Marcin Kołaczkowski; Aldona Pietrzak; Mansur Rahnama-Hezavah; Bartłomiej Drop; Dariusz Matosiuk
Journal:  Molecules       Date:  2022-05-04       Impact factor: 4.927

Review 3.  Current and Future Therapeutic Options in Pain Management: Multi-mechanistic Opioids Involving Both MOR and NOP Receptor Activation.

Authors:  Flaminia Coluzzi; Laura Rullo; Maria Sole Scerpa; Loredana Maria Losapio; Monica Rocco; Domenico Billeci; Sanzio Candeletti; Patrizia Romualdi
Journal:  CNS Drugs       Date:  2022-05-26       Impact factor: 6.497

  3 in total

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