Name | 1-(4'-AMINOPHENYL)-3,5-DIHYDRO-7,8-DIMETHOXY-4H-2,3-BENZODIAZEPIN-4-ONE |
Synonyms | CFM-2 1-(4'-AMINOPHENYL)-3,5-DIHYDRO-7,8-DIMETHOXY-4H-2,3-BENZODIAZEPIN-4-ONE 4H-2,3-Benzodiazepin-4-one,1-(4-aminophenyl)-3,5-dihydro-7,8-dimethoxy- |
CAS | 178616-26-7 |
Molecular Formula | C17H17N3O3 |
Molar Mass | 311.34 |
Appearance | Off-white solid. |
Storage Condition | Store at RT |
In vitro study | CFM-2 inhibits the extracellular signal regulated kinase (ERK1/2) pathway, CFM-2 reduced phosphorylation of cAMP-responsive element binding protein (CREB), suppressed expression of cyclin D1, upregulated the cell cycle regulators and tumor suppressor proteins p21 and p53 and decreased number of lung adenocarcinoma cells in G2 and S phases of the cell cycle. |
In vivo study | Pretreatment with CFM-2 delays the progression of seizure rank during repeated administration of pentylentetrazole. At the end of the period of repeated pentylentetrazole treatment (6 weeks) the mean seizure score was 0 in vehicle treated controls, 4.3 in animals treated with vehicle + pentylentetrazole, 2.2 in rats treated chronically with CFM-2 (20 μmol/kg; i.p.) + pentylentetrazole and 1.0 in rats treated repeatedly with CFM-2 (50 μmol/kg; i.p.) + pentylenetetrazole. CFM-2 is also able to antagonize the long-term increase in sensitivity of the convulsant effects of GABA function inhibitors in pentylentetrazole-kindled animals.Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 μg) and GYKI 52466 (50μg), significantly attenuated mechanical and thermal hypersensitivities on the ipsilateral hind paw at 2 and 24 h post-CFA injection. Neither CFM-2 nor GYKI 52466 affects the contralateral basal responses to thermal and mechanical stimuli. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.212 ml | 16.06 ml | 32.119 ml |
5 mM | 0.642 ml | 3.212 ml | 6.424 ml |
10 mM | 0.321 ml | 1.606 ml | 3.212 ml |
5 mM | 0.064 ml | 0.321 ml | 0.642 ml |
biological activity | CFM-2 is a potent, selective, non-competitive AMPAR antagonist. CFM-2 showed anticonvulsant activity in different animal models of convulsion. |