Abstract
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.
MeSH terms
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Animals
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Blood Pressure / drug effects
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Calcium Channel Blockers / chemical synthesis*
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Calcium Channel Blockers / chemistry
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Calcium Channel Blockers / pharmacology*
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Calcium Channels, T-Type / metabolism*
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Dogs
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Dose-Response Relationship, Drug
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Drug Design*
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Haplorhini
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Heart Rate / drug effects
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Models, Animal
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Molecular Structure
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology*
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Pyrans / chemical synthesis*
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Pyrans / chemistry
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Pyrans / pharmacology*
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Rats
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Structure-Activity Relationship
Substances
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Calcium Channel Blockers
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Calcium Channels, T-Type
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Piperidines
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Pyrans