Pelanserin
Pelanserin (Compound 1) is an orally active antihypertensive agent. Pelanserin is a potent 5-HT2 receptor antagonist. Pelanserin has the ability to block the activity of α-adrenergic receptor, with its ED50 being 0.03 μg/mL. Pelanserin has vasodilatory activity, with its ED100 being 5 μg. Pelanserin exhibits antihypertensive activity in hypertensive rats and renal hypertensive dog breeds. Pelanserin can be used for research on hypertension.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2208-51-7
- 分子式: C21H24N4O2
- 分子量:364.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | Inhibition |
-8.83 %
Compound: PELANSERIN
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
化学情報
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CAS 番号 2208-51-7
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分子量 364.44
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分子式 C21H24N4O2
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SMILES
O=C1NC2=C(C(N1CCCN3CCN(CC3)C4=CC=CC=C4)=O)C=CC=C2
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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.
プロトコル
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
純度とドキュメンテーション
参考文献
[1]. Havera HJ, Vidrio H. Derivatives of 1,3-disubstituted 2,4(1H,3H)-quinazolinediones as possible peripheral vasodilators or antihypertensive agents. J Med Chem. 1979 Dec;22(12):1548-50 [Content Brief]
[2]. Villalobos-Molina R, et al. The 5-HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro. Eur J Pharmacol. 1995 Apr 24;277(2-3):181-5. [Content Brief]
[3]. Flores-Murrieta FJ, et al. Pharmacokinetics and antihypertensive effect of oral pelanserin in renal hypertensive dogs. Arzneimittelforschung. 1992 Sep;42(9):1105-8. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Pelanserin 関連分類
HY-180379 関連分類
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