871792-56-2Relevant academic research and scientific papers
(Biphenyl-4-yl)methylammonium chlorides: Potent anticonvulsants that modulate Na+ currents
Lee, Hyosung,Park, Ki Duk,Yang, Xiao-Fang,Dustrude, Erik T.,Wilson, Sarah M.,Khanna, Rajesh,Kohn, Harold
, p. 5931 - 5939 (2013)
We have reported that compounds containing a biaryl linked unit (Ar-X-Ar′) modulated Na+ currents by promoting slow inactivation and fast inactivation processes and by inducing frequency (use)-dependent inhibition of Na+ currents. These electrophysiological properties have been associated with the mode of action of several antiepileptic drugs. In this study, we demonstrate that the readily accessible (biphenyl-4-yl)methylammonium chlorides (compound class B) exhibited a broad range of anticonvulsant activities in animal models, and in the maximal electroshock seizure test the activity of (3′-trifluoromethoxybiphenyl-4- yl)methylammonium chloride (8) exceeded that of phenobarbital and phenytoin upon oral administration to rats. Electrophysiological studies of 8 using mouse catecholamine A-differentiated cells and rat embryonic cortical neurons confirmed that 8 promoted slow and fast inactivation in both cell types but did not affect the frequency (use)-dependent block of Na+ currents.
