NNC-112
NNC-112 is a dopamine D1 receptor antagonist with a Ki of 0.18 nM for rat D1R and a Ki of 18 nM for 5-HT2. NNC-112 competitively inhibits [3H]SCH 23390 binding and blocks dopamine-stimulated adenylate cyclase. NNC-112 blocks D1 receptor-mediated rotational behavior in 6-OHDA-lesioned rats. NNC-112 can serve as a C11-labeled radioligand ([11C] NNC 112) for positron emission tomography imaging. NNC-112 can be used for research on schizophrenia and 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: 125341-24-4
- 分子式: C19H18ClNO2
- 分子量:327.81
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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
IC50 & Target
[2]|
D1 Receptor 0.18 nM (Ki) |
5-HT2A Receptor 18 nM (Ki) |
体外実験
NNC-112 (20 min) exhibits low affinity for rat striatal dopamine D2 receptors, with a KI of 898 nM[2].
NNC-112 exhibits moderate affinity for 5-HT2 receptors with a KI of 18 nM[2].
NNC-112 (15 min) is a potent competitive inhibitor of dopamine-stimulated adenylate cyclase in rat striatal tissue, with a KI of 2.8 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
NNC-112 (s.c.; 0.5 h before the agonist) selectively antagonizes D1 receptor-mediated rotational behavior in 6-OHDA (HY-B1081A)-lesioned rats with an ED50 of 0.08 mg/kg, without affecting D2-mediated rotation[2].
Pretreatment with NNC-112 (2-2.5 mg/kg; i.v.) produces 77% blockade of [11C]NNC 112 binding in the rat renal cortex, indicating that the PET signal is predominantly driven by specific D1-like receptor binding[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats[4]
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Dosage:2 mg/kg; 2.5 mg/kg
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Administration:i.v.; single pretreatment bolus
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Result:Reached an average of 0.083% injected dose per mL of tissue at 35 min in the left renal cortex, corresponding to a blocking percentage of 77%.
化学情報
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CAS 番号 125341-24-4
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分子量 327.81
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分子式 C19H18ClNO2
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SMILES
CN1C[C@@H](C=2C(=CC(Cl)=C(O)C2)CC1)C3=C4C(=CC=C3)C=CO4
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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)
NNC-112 関連分類
HY-165450 関連分類
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