Abstract
A series of arylsulfonamides containing guanidine incorporated in the structure of secondary amines (piperidine, piperazine) was synthesized on SynPhase Lanterns and evaluated for 5-HT(1A), 5-HT(2A), and 5-HT(7) receptors. The results demonstrated that N-alkyl-N'-dialkylguanidines displayed good 5-HT(7)/5-HT(1A) selectivity and may be regarded as promising structural core for development of 5-HT(7) ligands.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Guanidines / chemical synthesis
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Guanidines / chemistry*
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Guanidines / pharmacology
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Humans
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Ligands
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Rats
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Receptor, Serotonin, 5-HT1A / metabolism
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Receptor, Serotonin, 5-HT2A / metabolism
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Receptors, Serotonin / chemistry*
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Receptors, Serotonin / metabolism
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Serotonin 5-HT1 Receptor Antagonists
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Serotonin 5-HT2 Receptor Antagonists
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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
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology
Substances
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Guanidines
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Ligands
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Receptor, Serotonin, 5-HT2A
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Receptors, Serotonin
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Serotonin 5-HT1 Receptor Antagonists
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Serotonin 5-HT2 Receptor Antagonists
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Serotonin Antagonists
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Sulfonamides
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serotonin 7 receptor
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Receptor, Serotonin, 5-HT1A