| Literature DB >> 27579577 |
Lubos Remen1, Olivier Bezençon1, Lloyd Simons2, Rick Gaston2, Dennis Downing2, John Gatfield1, Catherine Roch1, Melanie Kessler1, Johannes Mosbacher1, Thomas Pfeifer1, Corinna Grisostomi1, Markus Rey1, Eric A Ertel1, Richard Moon1.
Abstract
A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. An optimized derivative, compound 6c, was advanced to in vivo studies, where it demonstrated efficacy in the WAG/Rij rat model of generalized nonconvulsive, absence-like epilepsy. Compound 6c was not efficacious in the basolateral amygdala kindling rat model of temporal lobe epilepsy, and it led to prolongation of the PR interval in ECG recordings in rodents.Entities:
Mesh：
Substances：
Year: 2016 PMID： 27579577 DOI： 10.1021/acs.jmedchem.6b00756
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446