Alvameline (Lu 25-109) (Synonyms: Lu 25-109) |
| رقم الكتالوجGC30996 |
Alvameline (Lu 25-109) (Lu25-109) هو ناهض جزئي M1 ومضاد M2 / M3.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120241-31-8
Sample solution is provided at 25 µL, 10mM.
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Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
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].
Alvameline competitively and effectively antagonizes carbachol-induced contractions and contractions induced by electrical field stimulation in human detrusor muscle. Alvameline produces a concentration-dependent rightward shift of the concentration-response curves for carbachol in both human and pig detrusor, the pKb values being 6.2 and 5.8. Contractions induced by electrical field stimulation in human detrusor are almost completely inhibited by 100 μM alvameline. In contrast, electrical field stimulation-induced contractions in pig detrusor are less sensitive to alvameline, resulting in a final inhibition of 32% with the highest concentration used (100 μM)[2]. Alvameline has been shown to improve cognitivefunction following traumatic brain injury in rats. Alvameline treated rats causes a 13% and 5% decrease in the medial septal nucleus, a 48 and 23% decrease in the vertical limb nucleus of the diagonal band, and a 51 and 28% decrease in the nucleus basalis magnocellularis, respectively[3].
[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. [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. [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.
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 120241-31-8 | SDF | |
| المرادفات | Lu 25-109 | ||
| Canonical SMILES | CN1CCC=C(C2=NN(CC)N=N2)C1 | ||
| Formula | C9H15N5 | M.Wt | 193.25 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.1746 mL | 25.8732 mL | 51.7464 mL |
| 5 mM | 1.0349 mL | 5.1746 mL | 10.3493 mL |
| 10 mM | 517.5 μL | 2.5873 mL | 5.1746 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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