Key result
The novel T-type calcium channel antagonist (S)-5 demonstrated potent and selective in vivo CNS efficacy without adverse cardiovascular effects.
The novel compound (S)-5 demonstrates potential as a CNS-active T-type calcium channel antagonist without cardiovascular toxicity in preclinical models.
Supports CNS T-type antagonist development; human trials required before clinical consideration.
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.
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Shipe et al. (2008) studied this question. The novel T-type calcium channel antagonist (S)-5 demonstrated potent and selective in vivo CNS efficacy without adverse cardiovascular effects.
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