Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers


著者: Lubos Remen†, Olivier Bezençon*†, Lloyd Simons‡, Rick Gaston‡, Dennis Downing‡, John Gatfield†, Catherine Roch†, Melanie Kessler†, Johannes Mosbacher†, Thomas Pfeifer†, Corinna Grisostomi†, Markus Rey†, Eric A. Ertel†, and Richard Moon†


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.

お問い合わせ

お問い合わせ

Sophion Bioscience A/S
Baltorpvej 154, 2750 Ballerup, Denmark
Telephone: +45 44 60 88 00

〒367-0035　埼玉県本庄市西富田1011
インキュベーション・オン・キャンパス本庄早稲田V203号室
TEL : 0495-71-8811 Fax : 0495-71-8812

inquiry[at]sophion.co.jp
※上記の"[at]"を"@"に置き換えて下さい。

You need to fill in all required fields.