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Glycine receptors and glycine transporters: targets for novel analgesics?


Zeilhofer, Hanns Ulrich; Acuña, Mario A; Gingras, Jacinthe; Yévenes, Gonzalo E (2018). Glycine receptors and glycine transporters: targets for novel analgesics? Cellular and Molecular Life Sciences, 75(3):447-465.

Abstract

Glycinergic neurotransmission has long been known for its role in spinal motor control. During the last two decades, additional functions have become increasingly recognized-among them is a critical contribution to spinal pain processing. Studies in rodent pain models provide proof-of-concept evidence that enhancing inhibitory glycinergic neurotransmission reduces chronic pain symptoms. Apparent strategies for pharmacological intervention include positive allosteric modulators of glycine receptors and modulators or inhibitors of the glial and neuronal glycine transporters GlyT1 and GlyT2. These prospects have led to drug discovery efforts in academia and in industry aiming at compounds that target glycinergic neurotransmission with high specificity. Available data show promising analgesic efficacy. Less is currently known about potential unwanted effects but the presence of glycinergic innervation in CNS areas outside the nociceptive system prompts for a careful evaluation not only of motor function, but also of potential respiratory impairment and addictive properties.

Abstract

Glycinergic neurotransmission has long been known for its role in spinal motor control. During the last two decades, additional functions have become increasingly recognized-among them is a critical contribution to spinal pain processing. Studies in rodent pain models provide proof-of-concept evidence that enhancing inhibitory glycinergic neurotransmission reduces chronic pain symptoms. Apparent strategies for pharmacological intervention include positive allosteric modulators of glycine receptors and modulators or inhibitors of the glial and neuronal glycine transporters GlyT1 and GlyT2. These prospects have led to drug discovery efforts in academia and in industry aiming at compounds that target glycinergic neurotransmission with high specificity. Available data show promising analgesic efficacy. Less is currently known about potential unwanted effects but the presence of glycinergic innervation in CNS areas outside the nociceptive system prompts for a careful evaluation not only of motor function, but also of potential respiratory impairment and addictive properties.

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Additional indexing

Item Type:Journal Article, refereed, further contribution
Communities & Collections:04 Faculty of Medicine > Institute of Pharmacology and Toxicology
07 Faculty of Science > Institute of Pharmacology and Toxicology
Dewey Decimal Classification:570 Life sciences; biology
610 Medicine & health
Scopus Subject Areas:Life Sciences > Molecular Medicine
Life Sciences > Molecular Biology
Life Sciences > Pharmacology
Life Sciences > Cellular and Molecular Neuroscience
Life Sciences > Cell Biology
Uncontrolled Keywords:Adverse effect, Analgesia, Central inhibition, Disinhibition, Drug discovery, Neuropathy, Pain, Therapeutic application
Language:English
Date:2018
Deposited On:25 Sep 2017 14:15
Last Modified:22 Nov 2023 08:08
Publisher:Springer
ISSN:1420-682X
OA Status:Closed
Publisher DOI:https://doi.org/10.1007/s00018-017-2622-x
PubMed ID:28791431
Project Information:
  • : FunderH2020
  • : Grant ID116064
  • : Project TitleITCC-P4 - ITCC Pediatric Preclinical POC Platform (ITCC-P4)
  • : FunderSNSF
  • : Grant ID31003AB_131093
  • : Project TitleControl of spinal pain processing by strychnine-sensitive glycine and GABAA receptors