N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists |
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Authors: | Fujio M Kuroita T Sakai Y Nakagawa H Matsumoto Y |
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Institution: | Exploratory Research I, Drug Discovery Laboratories, Welfide Corporation, Iruma, Saitama, Japan. fujio@welfide.co.jp |
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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. |
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