Abstract
The 5-HT2C receptor has been implicated in the regulation of appetite. As such, small molecule agonists to this receptor may serve as novel therapies to combat obesity. We describe here the identification, synthesis, and SAR of a 5-HT2C agonist from a unique pyrimidine-diazabicyclo[3.3.0]octane series. This compound displayed good potency at the 5-HT2C receptor, modest selectivity relative to other 5-HT2 receptors, and was efficacious in an acute feeding study in rats.
MeSH terms
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Amines / chemistry
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Animals
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Aza Compounds / chemical synthesis
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Aza Compounds / chemistry*
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Aza Compounds / pharmacology*
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Bridged Bicyclo Compounds / chemical synthesis
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Bridged Bicyclo Compounds / chemistry*
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Bridged Bicyclo Compounds / pharmacology*
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Molecular Structure
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology*
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Rats
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Receptor, Serotonin, 5-HT2C / metabolism*
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Serotonin 5-HT2 Receptor Agonists*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Amines
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Aza Compounds
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Bridged Bicyclo Compounds
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Pyrimidines
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Receptor, Serotonin, 5-HT2C
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Serotonin 5-HT2 Receptor Agonists