Abstract
Following the program started at Johnson & Johnson Pharmaceutical Research & Development searching for 5-HT(2A/2C) antagonists, we now report on the synthesis of 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,4-c]-[2]benzazepine and 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,2-c]-[2]benzazepine. A new method for the synthesis of pyridobenzazepines is described as well. The affinities for several receptors as well as the mCPP antagonistic activity of the compounds synthesised are described.
MeSH terms
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Animals
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Anti-Anxiety Agents / administration & dosage
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Anti-Anxiety Agents / chemical synthesis*
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Anti-Anxiety Agents / pharmacology
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Benzazepines / administration & dosage
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Benzazepines / chemical synthesis*
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Benzazepines / pharmacology
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Cyclization
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Humans
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Injections, Subcutaneous
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Male
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Radioligand Assay
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Rats
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Rats, Wistar
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Receptors, Histamine H1 / drug effects
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Receptors, Serotonin / drug effects*
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Serotonin Antagonists / administration & dosage
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / pharmacology
Substances
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Anti-Anxiety Agents
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Benzazepines
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Receptors, Histamine H1
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Receptors, Serotonin
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Serotonin Antagonists