Description
MDL29951actsasanagoNISTatGPR17,inhibitingmaturationofprimaryoligodendrocytesandpotentiallypromotingmyelinrepairinmodelsofmultiplesclerosis.MDL29951alsoinhibitsNMDAreceptorsattheglycinesiteaswellasfructose1,6-bisphosphatase.Thiscompounddisplaysneuromodulatory,anticonvulsant,andantinociceptiveactivities.Invivo,MDL29951inhibitsformalin-inducedlicking.Inanimalmodelsofseizures,thiscompoundincreasesthresholdsforthedevelopmentofchemically-inducedseizures.
References
HennenS,WangH,PetersL,etal.DecodingsignalingandfunctionoftheorphanGprotein-coupledreceptorGPR17withasmall-moleculeagonist.SciSignal.2013Oct22;6(298):ra93.PMID:24150254.
WrightSW,CarloAA,DanleyDE,etal.3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylicacid:anallostericinhibitoroffructose-1,6-bisphosphataseattheAMPsite.BioorgMedChemLett.2003Jun16;13(12):2055-8.PMID:12781194.
MillanMJ,SeguinL.Chemically-diverseligandsattheglycineBsitecoupledtoN-methyl-D-aspartate(NMDA)receptorsselectivelyblockthelatephaseofformalin-inducedpaininmice.NeurosciLett.1994Aug29;178(1):139-43.PMID:7816323.
BaronBM,HarrisonBL,McDonaldIA,etal.Potentindole-andquinoline-containingN-methyl-D-aspartateantagonistsactingatthestrychnine-insensitiveglycinebindingsite.JPharmacolExpTher.1992Sep;262(3):947-56.PMID:1388205.