Abstract
A series of 1-adamantanecarboxamides was synthesized and examined for their potency as a selective 5-HT2 receptor antagonist. We found (S)-N-[1-[2-(4-fluorophenyl)ethyl]pyrrolidin-3-yl]-1-adamantane carboxamide hydrochloride hydrate (10-(S), Y-39241) to have a high affinity and selectivity for 5-HT2 receptors, and this potent anti-platelet effect of Y-39241 was confirmed both in vitro and in vivo.
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin / metabolism
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Adamantane / analogs & derivatives
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Adamantane / chemical synthesis*
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Adamantane / chemistry
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Adamantane / metabolism
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Adamantane / pharmacology*
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Animals
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Brain Chemistry
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Ketanserin / metabolism
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Male
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Molecular Structure
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Platelet Aggregation Inhibitors / chemical synthesis
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Platelet Aggregation Inhibitors / chemistry
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Platelet Aggregation Inhibitors / metabolism
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Platelet Aggregation Inhibitors / pharmacology
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / chemistry
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Pyrrolidines / metabolism
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Pyrrolidines / pharmacology*
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Rabbits
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Rats
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Rats, Wistar
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Receptors, Serotonin / metabolism*
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Receptors, Serotonin, 5-HT1
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / chemistry
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Serotonin Antagonists / metabolism
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Serotonin Antagonists / pharmacology*
Substances
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N-(1-(2-(4-fluorophenyl)ethyl)pyrrolidin-3-yl)-1-adamantane carboxamide
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Platelet Aggregation Inhibitors
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Pyrrolidines
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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Serotonin Antagonists
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Ketanserin
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Adamantane