Matches in SemOpenAlex for { <https://semopenalex.org/work/W2002203475> ?p ?o ?g. }
- W2002203475 endingPage "268" @default.
- W2002203475 startingPage "259" @default.
- W2002203475 abstract "202W92 (R-(−)-2,4-diamino-6-(fluromethyl)-5-(2,3,5-trichlorophenyl)pyrimidine) is a novel compound in the same chemical series as the antiepileptic drug lamotrigine and the neuroprotective sipatrigine. Here 202W92 was quantitatively assessed as a neuroprotective agent in focal cerebral ischaemia, and as an inhibitor of sodium and calcium channels and of synaptic transmission. In the rat permanent middle cerebral artery occlusion (MCAO) model of acute focal ischaemia, 202W92 reduced infarct volume by 75% in cortex and by 80% in basal ganglia, with ED50 approximately 2 mg/kg (single i.v. dose, 10 min post-occlusion). In whole-cell current recordings from single cells, 202W92 completely and reversibly inhibited voltage gated sodium channels (IC50 3×10−6 M) in rat freshly-isolated cortical neurons and in the GH3 pituitary cell line. 202W92 also inhibited a nifedipine-sensitive fraction (approximately 35%) of native high-voltage-activated (HVA) calcium current in rat cortical neurons (IC50 15×10−6 M) and weakly inhibited low-voltage-activated (LVA) calcium currents of the recombinant α1I-mediated T-type (IC50>100×10−6 M). The drug inhibited the amplitude and frequency of 4-aminopyridine-evoked glutamatergic excitatory post-synaptic currents (EPSCs). In conclusion, 202W92 is an effective neuroprotective agent when administered post-ischaemia and a potent sodium channel inhibitor in vitro." @default.
- W2002203475 created "2016-06-24" @default.
- W2002203475 creator A5014640825 @default.
- W2002203475 creator A5018828484 @default.
- W2002203475 creator A5034199990 @default.
- W2002203475 creator A5046136215 @default.
- W2002203475 creator A5054160570 @default.
- W2002203475 creator A5058705196 @default.
- W2002203475 creator A5066737809 @default.
- W2002203475 creator A5082221123 @default.
- W2002203475 creator A5082528797 @default.
- W2002203475 creator A5086123400 @default.
- W2002203475 date "2001-11-01" @default.
- W2002203475 modified "2023-10-14" @default.
- W2002203475 title "Neuroprotective actions in vivo and electrophysiological actions in vitro of 202W92" @default.
- W2002203475 cites W1501592147 @default.
- W2002203475 cites W1764026126 @default.
- W2002203475 cites W1963530961 @default.
- W2002203475 cites W1980636657 @default.
- W2002203475 cites W1997415998 @default.
- W2002203475 cites W1998622193 @default.
- W2002203475 cites W2002331174 @default.
- W2002203475 cites W2004595736 @default.
- W2002203475 cites W2011481607 @default.
- W2002203475 cites W2012864694 @default.
- W2002203475 cites W2021684176 @default.
- W2002203475 cites W2027554403 @default.
- W2002203475 cites W2030288942 @default.
- W2002203475 cites W2036925887 @default.
- W2002203475 cites W2037844026 @default.
- W2002203475 cites W2044715727 @default.
- W2002203475 cites W2045835005 @default.
- W2002203475 cites W2052006707 @default.
- W2002203475 cites W2059029867 @default.
- W2002203475 cites W2059623003 @default.
- W2002203475 cites W2062354609 @default.
- W2002203475 cites W2067935544 @default.
- W2002203475 cites W2072926617 @default.
- W2002203475 cites W2091280737 @default.
- W2002203475 cites W2093421851 @default.
- W2002203475 cites W2110095865 @default.
- W2002203475 cites W2125683177 @default.
- W2002203475 cites W2131705725 @default.
- W2002203475 cites W2142484144 @default.
- W2002203475 cites W2143033210 @default.
- W2002203475 cites W2144918294 @default.
- W2002203475 cites W2148448757 @default.
- W2002203475 cites W2149703467 @default.
- W2002203475 cites W2158009878 @default.
- W2002203475 cites W2167720740 @default.
- W2002203475 cites W2169079203 @default.
- W2002203475 cites W2949367276 @default.
- W2002203475 doi "https://doi.org/10.1016/s0006-8993(01)03029-3" @default.
- W2002203475 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11701138" @default.
- W2002203475 hasPublicationYear "2001" @default.
- W2002203475 type Work @default.
- W2002203475 sameAs 2002203475 @default.
- W2002203475 citedByCount "20" @default.
- W2002203475 countsByYear W20022034752013 @default.
- W2002203475 countsByYear W20022034752014 @default.
- W2002203475 countsByYear W20022034752015 @default.
- W2002203475 countsByYear W20022034752016 @default.
- W2002203475 countsByYear W20022034752017 @default.
- W2002203475 countsByYear W20022034752020 @default.
- W2002203475 countsByYear W20022034752022 @default.
- W2002203475 crossrefType "journal-article" @default.
- W2002203475 hasAuthorship W2002203475A5014640825 @default.
- W2002203475 hasAuthorship W2002203475A5018828484 @default.
- W2002203475 hasAuthorship W2002203475A5034199990 @default.
- W2002203475 hasAuthorship W2002203475A5046136215 @default.
- W2002203475 hasAuthorship W2002203475A5054160570 @default.
- W2002203475 hasAuthorship W2002203475A5058705196 @default.
- W2002203475 hasAuthorship W2002203475A5066737809 @default.
- W2002203475 hasAuthorship W2002203475A5082221123 @default.
- W2002203475 hasAuthorship W2002203475A5082528797 @default.
- W2002203475 hasAuthorship W2002203475A5086123400 @default.
- W2002203475 hasConcept C112592302 @default.
- W2002203475 hasConcept C126322002 @default.
- W2002203475 hasConcept C169760540 @default.
- W2002203475 hasConcept C170493617 @default.
- W2002203475 hasConcept C17077164 @default.
- W2002203475 hasConcept C178790620 @default.
- W2002203475 hasConcept C185592680 @default.
- W2002203475 hasConcept C18699975 @default.
- W2002203475 hasConcept C200170125 @default.
- W2002203475 hasConcept C25498285 @default.
- W2002203475 hasConcept C42219234 @default.
- W2002203475 hasConcept C50952357 @default.
- W2002203475 hasConcept C519063684 @default.
- W2002203475 hasConcept C537181965 @default.
- W2002203475 hasConcept C55493867 @default.
- W2002203475 hasConcept C71924100 @default.
- W2002203475 hasConcept C85520022 @default.
- W2002203475 hasConcept C86803240 @default.
- W2002203475 hasConcept C98274493 @default.
- W2002203475 hasConceptScore W2002203475C112592302 @default.
- W2002203475 hasConceptScore W2002203475C126322002 @default.
- W2002203475 hasConceptScore W2002203475C169760540 @default.