Abstract
Bisarylmethoxyethers have been identified with nanomolar 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 1, 2, 8, 12, 14 and 18 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their therapeutic potential is currently under further investigation.
MeSH terms
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Aminopyridines / administration & dosage
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Aminopyridines / chemical synthesis*
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Aminopyridines / chemistry
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Aminopyridines / pharmacology*
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Animals
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Drug Design
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Indoles / administration & dosage
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology*
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Kinetics
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Molecular Structure
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Motor Activity / drug effects
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Rats
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Receptor, Serotonin, 5-HT2C
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Receptors, Serotonin / metabolism*
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Serotonin Antagonists / administration & dosage
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / chemistry
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Serotonin Antagonists / pharmacology*
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Structure-Activity Relationship
Substances
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Aminopyridines
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Indoles
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Receptor, Serotonin, 5-HT2C
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Receptors, Serotonin
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Serotonin Antagonists