μ-Opioid receptor 6-transmembrane isoform

A potential therapeutic target for new effective opioids

Marino Convertino, Alexander Samoshkin, Josee Gauthier, Michael S. Gold, William Maixner, Nikolay Dokholyan, Luda Diatchenko

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

The μ-opioid receptor (MOR) is the primary target for opioid analgesics. MOR induces analgesia through the inhibition of second messenger pathways and the modulation of ion channels activity. Nevertheless, cellular excitation has also been demonstrated, and proposed to mediate reduction of therapeutic efficacy and opioid-induced hyperalgesia upon prolonged exposure to opioids. In this mini-perspective, we review the recently identified, functional MOR isoform subclass, which consists of six transmembrane helices (6TM) and may play an important role in MOR signaling. There is evidence that 6TM MOR signals through very different cellular pathways and may mediate excitatory cellular effects rather than the classic inhibitory effects produced by the stimulation of the major (7TM) isoform. Therefore, the development of 6TM and 7TM MOR selective compounds represents a new and exciting opportunity to better understand the mechanisms of action and the pharmacodynamic properties of a new class of opioids.

Original languageEnglish (US)
Pages (from-to)61-67
Number of pages7
JournalProgress in Neuro-Psychopharmacology and Biological Psychiatry
Volume62
DOIs
StatePublished - Oct 1 2015

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Opioid Receptors
Opioid Analgesics
Protein Isoforms
Hyperalgesia
Second Messenger Systems
Therapeutics
Ion Channels
Analgesia

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Biological Psychiatry

Cite this

Convertino, Marino ; Samoshkin, Alexander ; Gauthier, Josee ; Gold, Michael S. ; Maixner, William ; Dokholyan, Nikolay ; Diatchenko, Luda. / μ-Opioid receptor 6-transmembrane isoform : A potential therapeutic target for new effective opioids. In: Progress in Neuro-Psychopharmacology and Biological Psychiatry. 2015 ; Vol. 62. pp. 61-67.
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μ-Opioid receptor 6-transmembrane isoform : A potential therapeutic target for new effective opioids. / Convertino, Marino; Samoshkin, Alexander; Gauthier, Josee; Gold, Michael S.; Maixner, William; Dokholyan, Nikolay; Diatchenko, Luda.

In: Progress in Neuro-Psychopharmacology and Biological Psychiatry, Vol. 62, 01.10.2015, p. 61-67.

Research output: Contribution to journalArticle

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AU - Convertino, Marino

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