Design, Synthesis, and Evaluation of a Novel 4-Aminomethyl-4-fluoropiperidine as a T-Type Ca2+ Channel Antagonist
WD Shipe, JC Barrow, ZQ Yang… - Journal of medicinal …, 2008 - ACS Publications
WD Shipe, JC Barrow, ZQ Yang, CW Lindsley, FV Yang, KAS Schlegel, Y Shu, KE Rittle…
Journal of medicinal chemistry, 2008•ACS PublicationsThe novel T-type antagonist (S)-5 has been prepared and evaluated in in vitro and in vivo
assays for T-type calcium ion channel activity. Structural modification of the piperidine leads
1 and 2 afforded the fluorinated piperidine (S)-5, a potent and selective antagonist that
displayed in vivo CNS efficacy without adverse cardiovascular effects.
assays for T-type calcium ion channel activity. Structural modification of the piperidine leads
1 and 2 afforded the fluorinated piperidine (S)-5, a potent and selective antagonist that
displayed in vivo CNS efficacy without adverse cardiovascular effects.
The novel T-type antagonist (S)-5 has been prepared and evaluated in in vitro and in vivo assays for T-type calcium ion channel activity. Structural modification of the piperidine leads 1 and 2 afforded the fluorinated piperidine (S)-5, a potent and selective antagonist that displayed in vivo CNS efficacy without adverse cardiovascular effects.
ACS Publications