Abstract
A series of benzamides was synthesized as selective agonists for the 5-HT1A receptor. It was found that (S)-N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarb oxamide(7-(S)) has potent and selective agonistic activity for the 5-HT1A receptor (5-HT1A; Ki 0.49 nmol/L, D2; IC50 = >1000 nmol/L, 5-HT2; Ki = 240 nmol/L).
MeSH terms
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Amides / chemical synthesis*
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Amides / pharmacology
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Animals
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Binding, Competitive / drug effects
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In Vitro Techniques
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Neurons / drug effects
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Neurons / metabolism
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / pharmacology
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Raphe Nuclei / cytology
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Raphe Nuclei / drug effects
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Raphe Nuclei / metabolism
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Rats
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Receptor, Serotonin, 5-HT2A
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Receptors, Dopamine D2 / drug effects
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Receptors, Dopamine D2 / metabolism
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Receptors, Serotonin / drug effects*
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Receptors, Serotonin / metabolism
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists / chemical synthesis*
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Serotonin Receptor Agonists / pharmacology
Substances
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Amides
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Pyrrolidines
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Receptor, Serotonin, 5-HT2A
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Receptors, Dopamine D2
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists