Glycine Receptors and Glycine Transporters: Targets for Novel Analgesics?

Overview

Journal Cell Mol Life Sci

Publisher Springer

Specialty Biology

Date 2017 Aug 10

PMID 28791431

Citations 39

Authors

Hanns Ulrich Zeilhofer

Mario A Acuna

Jacinthe Gingras

Gonzalo E Yevenes

Affiliations

Soon will be listed here.

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.

Citing Articles

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Allosteric modulation and direct activation of glycine receptors by a tricyclic sulfonamide.

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