Savoxepine
Savoxepine (Cipazoxapine; CGP 19486A) is a dopamine antagonist with antipsychotic activity. Savoxepine preferentially blocks hippocampal dopamine D2 receptors and also inhibits dopamine-stimulated adenylate cyclase activity. Savoxepine shows strong interactions with α-adrenergic receptors, serotonin 5-HT2 receptors and histamine H1 receptors, and moderate interactions with α2-adrenergic receptors, histamine H2 receptors, serotonin 5-HT1 receptors and cholinergic muscarinic receptors. Savoxepine inhibits dopamine agonist-induced stereotyped behaviors in animals, induces catalepsy in animals, and antagonizes Apomorphine (HY-12723)-induced climbing behavior in mice. Savoxepine can be used in schizophrenia-related research.
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- CAS 番号: 79262-46-7
- 分子式: C25H26N2O
- 分子量:370.49
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
Rat D2 Receptor |
体外実験
Savoxepine (CGP 19486) preferentially binds to hippocampal D2 dopamine receptors, with an affinity for hippocampal D2 receptors that is 10-fold higher than that for striatal D2 receptors. It potently blocks D1 receptors by inhibiting dopamine-activated adenylate cyclase, while exerting equivalent presynaptic and postsynaptic antidopaminergic effects[1].
Savoxepine exhibits high binding affinity for α-adrenergic, 5-HT2 serotonin, and H1 histamine receptors, moderate binding affinity for α2-adrenergic, H2 histamine, 5-HT1, and muscarinic cholinergic receptors, and almost no binding activity for benzodiazepine, opioid, and β-adrenergic receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
Savoxepine (intraperitoneal injection) exhibits a higher blocking potency against hippocampal D2 dopamine receptors (ID50 = 0.04 mg/kg i.p.) than against striatal D2 dopamine receptors (ID50 = 0.7 mg/kg i.p.) in rats, and its inhibitory effect on hippocampal receptors lasts significantly longer; it potently antagonizes Apomorphine (HY-12723)-induced climbing behavior in mice, with an ID50 of 0.06 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 79262-46-7
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分子量 370.49
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分子式 C25H26N2O
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SMILES
N#CC1=CC=C2OC3=CC=CC=C3C(CCN(CC4)CC5CCCC5)=C4C2=C1
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別名
Cipazoxapine; CGP 19486A
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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
[1]. Möller HJ, et al. Efficacy and tolerability of a new antipsychotic compound (savoxepine): results of a pilot-study. Pharmacopsychiatry. 1989 Jan;22(1):38-41. [Content Brief]
[2]. Bischoff S, et al. Blockade of hippocampal dopamine (DA) receptors: a tool for antipsychotics with low extrapyramidal side effects. Progress in neuro-psychopharmacology & biological psychiatry. 1988;12(4):455-67. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Savoxepine 関連分類
HY-W747310 関連分類
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Keywords
- Savoxepine
- 79262-46-7
- Cipazoxapine
- CGP 19486A
- Dopamine Receptor
- Adenylate Cyclase
- histamine H2 receptors
- cholinergic muscarinic receptors
- serotonin 5-HT2 receptors
- hippocampal dopamine D2 receptors
- dopamine D1 receptors
- striatal dopamine D2 receptors
- histamine H1 receptors
- alpha2-adrenoceptors
- alpha-adrenergic receptors
- serotonin 5-HT1 receptors
- Inhibitor
- inhibitor
- inhibit