Verbinding 7P CAS:1890208-58-8

Verbinding 7p werd ontwikkeld als één in een reeks verbindingen met als doel dubbelwerkende tromboxaanreceptorantagonisten/synthaseremmers te identificeren . In feite vertoont verbinding 7p selectiviteit voor prostaglandine I2-synthase (PTGIS, CYP8A1) dan tromboxaansynthase (CYP5A1).

De regeneratie van axonen na letsel in het centrale zenuwstelsel wordt gedeeltelijk belemmerd omdat er een leeftijdsafhankelijke afname van het intrinsieke groeipotentieel van axonen optreedt., en een van de strategieën om axongroei in beschadigde neuronen te stimuleren omvat farmacologische manipulatie van betrokken signaalroutes.

Here we report phenotypic cell-based screen of chemical libraries and structure-activity-guided optimization that resulted in the identification of compound 7p which promotes neurite outgrowth of cultured primary neurons derived from the hippocampus, cerebral cortex, and retina.

In an animal model of optic nerve injury, compound 7p was shown to induce growth of GAP-43 positive axons, indicating that the in vitro neurite outgrowth activity of compound 7p translates into stimulation of axon regeneration in vivo. Further optimization of compound 7p and elucidation of the mechanisms by which it elicits axon regeneration in vivo will provide a rational basis for future efforts to enhance treatment strategies.

1. Repare the danage head nerve.
2.We report phenotypic cell-based screen of chemical libraries and structure-activity-guided optimization that resulted in the identification of compound 7p which promotes neurite outgrowth of cultured primary neurons derived from the hippocampus, cerebral cortex, and retina. in an animal model of optic nerve injury, compound 7p was shown to induce growth of gap-43 positive axons, indicating that the in vitro neurite outgrowth activity of compound 7p translates into stimulation of axon regeneration in vivo.