Abstract
The stereoselective synthesis of N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl+ ++)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide (4) and its NK1 and NK2 receptor binding properties are reported. In addition the potent inhibitory effects in vivo on sar9-SP- and beta-Ala-NKA-induced airway bronchoconstriction in guinea pigs are demonstrated.
MeSH terms
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Administration, Oral
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Animals
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Anti-Asthmatic Agents / chemistry*
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Anti-Asthmatic Agents / metabolism
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Anti-Asthmatic Agents / pharmacology
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Aza Compounds / pharmacology*
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Benzamides / pharmacology*
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Bronchoconstriction / drug effects
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Drug Design
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Guinea Pigs
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Molecular Structure
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Neurokinin A / analogs & derivatives*
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Neurokinin A / pharmacology
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Neurokinin-1 Receptor Antagonists*
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Peptide Fragments / pharmacology
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Receptors, Neurokinin-2 / antagonists & inhibitors*
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Stereoisomerism
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Substance P / pharmacology
Substances
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Anti-Asthmatic Agents
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Aza Compounds
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Benzamides
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N-(1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl)-N-methyl-3,5,-bis-trifluoromethyl-benzamide
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Neurokinin-1 Receptor Antagonists
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Peptide Fragments
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Receptors, Neurokinin-2
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neurokinin A (4-10), beta-Ala(8)-
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Substance P
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Neurokinin A