Abstract
5-HT1 receptor antagonists have been discovered with good selectivity over the 5-HT transporter. This is the first report of highly potent, selective ligands for the 5-HT1A/B/D receptors with low intrinsic activity, which represent a useful set of molecules for further understanding the roles of the 5-HT1 receptor subtypes and providing new approaches for the treatment of depression.
MeSH terms
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Animals
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Blood-Brain Barrier / metabolism
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Cerebral Cortex / metabolism
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Humans
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In Vitro Techniques
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Piperazines / chemical synthesis*
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Piperazines / pharmacokinetics
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Piperazines / pharmacology
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Quinolines / chemical synthesis*
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Quinolines / pharmacokinetics
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Quinolines / pharmacology
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Radioligand Assay
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Rats
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Recombinant Proteins / pharmacology
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Serotonin 5-HT1 Receptor Antagonists*
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Structure-Activity Relationship
Substances
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Piperazines
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Quinolines
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Recombinant Proteins
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Serotonin 5-HT1 Receptor Antagonists