Structural Determinants of the Neuronal Glycine Transporter 2 for the Selective Inhibitors ALX1393 and ORG25543.
ALX1393
ORG25543
glycinergic neurotransmission
inhibitor binding
neuronal glycine transporter 2
pain
Journal
ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337
Informations de publication
Date de publication:
02 06 2021
02 06 2021
Historique:
pubmed:
19
5
2021
medline:
22
6
2021
entrez:
18
5
2021
Statut:
ppublish
Résumé
The neuronal glycine transporter GlyT2 modulates inhibitory glycinergic neurotransmission by controlling the extracellular concentration of synaptic glycine and the supply of neurotransmitter to the presynaptic terminal. Spinal cord glycinergic neurons present in the dorsal horn diminish their activity in pathological pain conditions and behave as gate keepers of the touch-pain circuitry. The pharmacological blockade of GlyT2 reduces the progression of the painful signal to rostral areas of the central nervous system by increasing glycine extracellular levels, so it has analgesic action.
Identifiants
pubmed: 34003005
doi: 10.1021/acschemneuro.0c00602
pmc: PMC8691691
doi:
Substances chimiques
4-benzyloxy-3,5-dimethoxy-N-(1-(dimethylaminocyclopently)methyl)benzamide
0
ALX 1393
0
Benzamides
0
Glycine Plasma Membrane Transport Proteins
0
Serine
452VLY9402
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1860-1872Références
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