title: New approaches to target glycinergic neurotransmission for the treatment of chronic pain.
abstract: Inhibitory glycinergic neurotransmission in the spinal cord dorsal horn plays an important role in regulating nociceptive signalling by inhibiting neuronal excitation. Blocking glycinergic transmission in the dorsal horn causes normally innocuous stimuli to become painful (allodynia) and increases sensitivity to noxious stimuli (hyperalgesia). Loss of inhibitory signalling is thought to contribute to the development of pathological pain. Management of neuropathic pain with current therapeutics is challenging and there is a great need for more effective treatments. Preclinical studies using drugs that increase glycinergic signalling by potentiating glycine receptor activity or inhibiting transporter activity suggest that targeting this system is a good therapeutic strategy. The spatially restricted expression of glycine receptors and transporters is an advantage for targeting specific pathologies such as pain. However, until recently there have been few pharmacological modulators identified and most of which do not specifically target glycinergic signalling. This mini-review provides an overview of recent advances in the development of therapeutics and novel approaches that aim to increase glycinergic neurotransmission for the treatment of persistent pain.
authors.affiliation: Discipline of Pharmacology, School of Medical Sciences, Rm. W300, Blackburn D06, The University of Sydney, Sydney NSW 2006, Australia. Electronic address: wendy.imlach@sydney.edu.au.
authors.forename: Wendy L
authors.initials: WL
authors.lastname: Imlach
mesh_terms: D000818:Animals; D059350:Chronic Pain / Q000188:drug therapy* / Q000378:metabolism; D018684:Glycine Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D006801:Humans; D026901:Membrane Transport Proteins / Q000378:metabolism; D018009:Receptors, Glycine / Q000378:metabolism; D009435:Synaptic Transmission / Q000187:drug effects*
chemical_list: D018684:Glycine Agents; D026901:Membrane Transport Proteins; D018009:Receptors, Glycine
keywords: Dorsal horn; Glycine receptors; Glycine transporters; Inhibitory neurotransmission; Pain