Design, Synthesis, and Evaluation of a Novel 4-Aminomethyl-4-fluoropiperidine as a T-Type Ca2+ Channel Antagonist

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.