Abstract
Investigation of halogen substitution in lead compound 1 has led to the identification of analogues which combine high affinity for 5-HT(1A) receptors and potent serotonin reuptake inhibitory activity. Several compounds show an improved selectivity over 5-HT(1B) and 5-HT(1D) receptors and a superior pharmacokinetic profile in the rat.
MeSH terms
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Animals
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Benzoxazines / chemical synthesis*
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Benzoxazines / pharmacology*
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Binding, Competitive / drug effects
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CHO Cells
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Callithrix
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Cell Line
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Cricetinae
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Cricetulus
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Guinea Pigs
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Humans
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Models, Molecular
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Piperazines / pharmacology
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Pyridines / pharmacology
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Radioligand Assay
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Rats
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Receptor, Serotonin, 5-HT1A / drug effects*
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Receptor, Serotonin, 5-HT1B / drug effects
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Receptor, Serotonin, 5-HT1D / drug effects
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Selective Serotonin Reuptake Inhibitors / chemical synthesis*
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / pharmacology*
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Synaptosomes / drug effects
Substances
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Benzoxazines
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Indicators and Reagents
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Piperazines
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Pyridines
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Receptor, Serotonin, 5-HT1B
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Receptor, Serotonin, 5-HT1D
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Serotonin Antagonists
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Serotonin Uptake Inhibitors
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Receptor, Serotonin, 5-HT1A
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N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide