Abstract
Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT(2C) receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT(2) receptor subtypes of 1 order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT(2C) receptor agonists.
MeSH terms
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Animals
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Eating / drug effects*
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Indoles / chemical synthesis
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Indoles / pharmacology
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Injections, Subcutaneous
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Pyrazines / chemical synthesis
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Pyrazines / pharmacology
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Pyridines / chemical synthesis
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Pyridines / pharmacology
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Rats
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Rats, Wistar
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Serotonin 5-HT2 Receptor Agonists*
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Serotonin Receptor Agonists / chemical synthesis
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Serotonin Receptor Agonists / pharmacology*
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Structure-Activity Relationship
Substances
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Indoles
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Pyrazines
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Pyridines
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Serotonin 5-HT2 Receptor Agonists
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Serotonin Receptor Agonists