Alvameline
Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
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- CAS No.: 120241-31-8
- Formule: C9H15N5
- Masse moléculaire:193.25
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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] |
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 120241-31-8
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Masse moléculaire 193.25
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Formule C9H15N5
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SMILES
CN1CCC=C(C2=NN(CC)N=N2)C1
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Synonyms
Lu 25-109
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Alvameline Related Classifications
HY-101586 Related Classifications
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