LY 367265
LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder.
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- CAS 番号: 210751-39-6
- 分子式: C24H25FN4O2S
- 分子量:452.54
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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5-HT2A Receptor 0.81 nM (Ki) |
5-HT1B Receptor 490 nM (Ki) |
5-HT1D Receptor 81 nM (Ki) |
化学情報
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CAS 番号 210751-39-6
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分子量 452.54
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分子式 C24H25FN4O2S
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SMILES
O=S1(N(CCN2CC=C(CC2)C3=CNC4=C3C=CC(F)=C4)C5=CC=CC6=C5N1CCC6)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)