Literature DB >> 28935293

Designing Safer Analgesics via μ-Opioid Receptor Pathways.

H C Stephen Chan1, Dillon McCarthy2, Jianing Li2, Krzysztof Palczewski3, Shuguang Yuan4.   

Abstract

Pain is both a major clinical and economic problem, affecting more people than diabetes, heart disease, and cancer combined. While a variety of prescribed or over-the-counter (OTC) medications are available for pain management, opioid medications, especially those acting on the μ-opioid receptor (μOR) and related pathways, have proven to be the most effective, despite some serious side effects including respiration depression, pruritus, dependence, and constipation. It is therefore imperative that both academia and industry develop novel μOR analgesics which retain their opioid analgesic properties but with fewer or no adverse effects. In this review we outline recent progress towards the discovery of safer opioid analgesics.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  GPCR; computational biology; drug discovery; opioid receptor; safer painkiller

Mesh：

Substances：

Year:  2017        PMID： 28935293      PMCID： PMC5690544          DOI： 10.1016/j.tips.2017.08.004

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN： 0165-6147            Impact factor:   14.819


  73 in total

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2.  β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists.

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4.  Stabilization of μ-opioid receptor facilitates its cellular translocation and signaling.

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7.  A2A Adenosine Receptor Partial Agonism Related to Structural Rearrangements in an Activation Microswitch.

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9.  Inhibition of mu-opioid receptor suppresses proliferation of hepatocellular carcinoma cells via CD147-p53-MAPK cascade signaling pathway.

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10.  Preclinical Assessment of the Analgesic Pharmacology of NKTR-181 in Rodents.

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