Abstract
A series of novel 4,4-disubstituted cyclohexylamines as NK(1) receptor antagonists is described: modifications to the amine moiety retain NK(1) receptor binding affinity whilst disrupting I(Kr) affinity.
MeSH terms
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Amines / chemistry
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Animals
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Benzopyrans / chemistry
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Binding Sites
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CHO Cells
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Cation Transport Proteins*
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Clone Cells
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Cricetinae
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Cyclohexylamines / chemical synthesis*
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Cyclohexylamines / pharmacokinetics
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Cyclohexylamines / pharmacology*
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Ether-A-Go-Go Potassium Channels
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Gerbillinae
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Inhibitory Concentration 50
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Models, Molecular
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Molecular Conformation
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Neurokinin-1 Receptor Antagonists*
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Piperidines / chemistry
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Potassium Channels / drug effects
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Potassium Channels / metabolism
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Potassium Channels, Voltage-Gated*
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Radioligand Assay
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Receptors, Neurokinin-1 / chemistry
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Receptors, Neurokinin-1 / drug effects
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Structure-Activity Relationship
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Time Factors
Substances
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Amines
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Benzopyrans
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Cation Transport Proteins
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Cyclohexylamines
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Ether-A-Go-Go Potassium Channels
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KCNH6 protein, human
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Neurokinin-1 Receptor Antagonists
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Piperidines
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Potassium Channels
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Potassium Channels, Voltage-Gated
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Receptors, Neurokinin-1
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L 706000