Abstract
A series of 4,4-disubstituted cyclohexylamine NK(1) antagonists containing a lactam ring is described. The compounds are brain penetrant and activity is demonstrated in a ferret emesis model.
MeSH terms
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Amides / chemistry
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Animals
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Antiemetics / chemical synthesis*
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Antiemetics / chemistry
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Antiemetics / pharmacology*
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Gerbillinae
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Humans
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Inhibitory Concentration 50
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Lactams / chemical synthesis
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Lactams / chemistry*
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Lactams / pharmacology*
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Methylation
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Molecular Structure
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Receptors, Neurokinin-1 / metabolism
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Structure-Activity Relationship
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Tachykinins / antagonists & inhibitors*
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Tachykinins / metabolism
Substances
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Amides
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Antiemetics
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Lactams
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Receptors, Neurokinin-1
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Tachykinins