Abstract
A 5-fluoro-tetrahydrocarbazole serotonin reuptake inhibitor (SRI) building block was combined with a variety of linkers and dopamine D2 receptor ligands in an attempt to identify potent D2 partial agonist/SRI molecules for treatment of schizophrenia. This approach has the potential to treat a broader range of symptoms compared to existing therapies. Selected compounds in this series demonstrate high affinity for both targets and D2 partial agonism in cell-based and in vivo assays.
MeSH terms
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Animals
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Carbazoles / chemical synthesis
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Carbazoles / chemistry*
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Carbazoles / pharmacology
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Disease Models, Animal
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Dopamine Agonists / chemical synthesis
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Dopamine Agonists / chemistry*
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Dopamine Agonists / pharmacology
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Rats
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Receptor, Serotonin, 5-HT1A / metabolism
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Receptors, Dopamine D2 / agonists*
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Receptors, Dopamine D2 / metabolism
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Schizophrenia / drug therapy*
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Selective Serotonin Reuptake Inhibitors / chemical synthesis
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Selective Serotonin Reuptake Inhibitors / chemistry*
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Selective Serotonin Reuptake Inhibitors / pharmacology
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Serotonin 5-HT1 Receptor Antagonists*
Substances
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Carbazoles
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Dopamine Agonists
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Receptors, Dopamine D2
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Serotonin 5-HT1 Receptor Antagonists
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Serotonin Uptake Inhibitors
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Receptor, Serotonin, 5-HT1A