Abstract
Structure activity studies on [4-(phenylsulfonyl)phenyl]methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4-methoxyphenyl(S)-sufinyl]phenyl]-1-pi perazineacetonitrile, 1, an M2 selective muscarinic antagonist. Affinity at the cloned human M2 receptor was 2.7 nM; the M1/M2 selectivity is 40-fold.
MeSH terms
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Acetylcholine / metabolism
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Administration, Oral
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Alkaloids / chemistry
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Alkaloids / pharmacology
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Animals
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Benzene Derivatives / chemical synthesis*
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Benzene Derivatives / chemistry
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Benzene Derivatives / pharmacology
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Corpus Striatum / drug effects
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Corpus Striatum / metabolism
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Dibenzazepines / chemistry
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Dibenzazepines / pharmacology
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Drug Design
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Furans
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Humans
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Muscarinic Antagonists / chemical synthesis*
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Muscarinic Antagonists / chemistry
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Muscarinic Antagonists / pharmacology
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Naphthalenes
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Piperidines
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Pyridines / chemistry
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Pyridines / pharmacology
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Rats
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Receptor, Muscarinic M2
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Receptors, Muscarinic / drug effects*
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Receptors, Muscarinic / physiology
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Recombinant Proteins / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Alkaloids
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Benzene Derivatives
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Dibenzazepines
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Furans
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Muscarinic Antagonists
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Naphthalenes
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Piperidines
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Pyridines
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Receptor, Muscarinic M2
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Receptors, Muscarinic
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Recombinant Proteins
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BIBN 99
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diphenyl sulfoxide
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himbacine
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Acetylcholine