Abstract
Bisaryl ethers have been identified with excellent 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 11, 27 and 38 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their potential as novel non-sedating anxiolytic and antidepressants is under investigation.
MeSH terms
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Administration, Oral
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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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Anti-Anxiety Agents / administration & dosage
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Anti-Anxiety Agents / chemical synthesis
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Anti-Anxiety Agents / chemistry
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Anti-Anxiety Agents / pharmacology
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Antidepressive Agents / administration & dosage
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Antidepressive Agents / chemical synthesis
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Antidepressive Agents / chemistry
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Antidepressive Agents / pharmacology
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Drug Design
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Humans
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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 / chemistry
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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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Anti-Anxiety Agents
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Antidepressive Agents
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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