Alvameline
Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
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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: 120241-31-8
- 分子式: C9H15N5
- 分子量:193.25
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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mAChR3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
296 nM
Compound: Alvameline
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Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
体外実験
Alvameline is metabolized by human liver microsomes to Lu 31-126 mainly by CYP2D6; to Lu 29-297 and Lu 25-077 mainly by CYP1A2, CYP2A6, CYP2C19, and CYP3A4; and to Lu 32-181 by CYP1A2 and possibly by CYP2C19. One metabolite, Lu 32-181, could be reduced back to alvameline, a reaction not inhibited by the applied cytochrome P-450 inhibitors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
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 120241-31-8
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分子量 193.25
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分子式 C9H15N5
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SMILES
CN1CCC=C(C2=NN(CC)N=N2)C1
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別名
Lu 25-109
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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
Animal Administration[2]
Rats: Treatment with alvameline is initiated 24 h following TBI and rats are injected (sc) once daily for the first 15 days after injury or sham injury. Injured rats are injected daily with either saline or 15 μmol/kg of alvameline. Sham-injured rats are injected (sc) daily with either saline or 15 μmol/kg of alvameline-T[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
[1]. Jensen KG, et al. In vitro metabolism of the M1-muscarinic agonist 5-(2-ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine by human hepatic cytochromes P-450 determined at pH 7.4 and 8.5. Drug Metab Dispos. 1999 Jan;27(1):125-32. [Content Brief]
[2]. Waldeck K, et al. Actions of the new antimuscarinic compound Alvameline on isolated human and pig detrusor. Neurourol Urodyn. 2002;21(1):92-8. [Content Brief]
[3]. Pike BR, et al. Chronic administration of a partial muscarinic M1 receptor agonist attenuates decreases in forebrain choline acetyltransferase immunoreactivity following experimental brain trauma. Exp Neurol. 1997 Sep;147(1):55-65. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Alvameline 関連分類
HY-101586 関連分類
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