In vitro activity: SUN11602, a novel synthetic aniline compound with basic fibroblast growth factor-like activity, can mimic the neuroprotective mechanisms of basic fibroblast growth factor. Basic fibroblast growth factor (FGF-2/bFGF) possesses neuroprotective activity and promotes cell proliferation. SUN11602 exhibited neuroprotective activities similar to those of FGF-2 without promoting cell proliferation. In primary cultures of hippocampal neurons, stimulation with SUN11602 or FGF-2 increased calbindin D-28k (CalB) gene expression and prevented glutamate-induced neuronal death. These effects were abolished by pretreatment with PD166866 (FGF receptor 1 [FGFR1] tyrosine kinase-specific inhibitor). This indicated that FGFR1 activation and increased CalB expression were involved in SUN11602-mediated neuroprotection. However, receptor-binding assays revealed that unlike FGF-2, SUN11602 did not alter the binding of (125)I-labeled FGF-2 to FGFR1.

Kinase Assay: SUN11602 is a novel aniline compound with basic fibroblast growth factor-like activity.

Cell Assay: Cerebrocortical neurons are pretreated with vehicle (Hanks’ Balanced Salt Solution), SUN11602, bFGF, or the other growth factors for 24 h prior to the onset of glutamate toxicity. Subsequently, 10 μL of the MTT solution (5 mg/mL) is added to each well (200 μL of culture medium) of the microplates. Neurons in each well are then dried for 24 h, and 200 μL of DMSO is poured into all of the wells in order to dissolve the reaction products thoroughly for the MTT assay.