Milameline
Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [3H]CMD (IC50 = 20 nM), than [3H]QNB, (IC50 = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease.
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- CAS No.: 139886-32-1
- Formule: C8H14N2O
- Masse moléculaire:154.21
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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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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mAChR1 1.3 μM (IC50) |
mAChR2 1.1 μM (IC50) |
mAChR3 1.5 μM (IC50) |
mAChR4 1.9 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
0.021 μM
Compound: Milameline
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Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
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[PMID: 25765911] |
Milameline increases soluble APP (sAPP) secretion in CHO cells transfected with human M1 or M3 receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Milameline (0.02- > 0.1 mg/kg, p.o.) effectively reverses Scopolamine (HY-N0296)-induced working memory impairment in rats at low doses (0.02-0.1 mg/kg), but the effect is reduced at high doses (> 0.1 mg/kg)[1].
Milameline increases cerebral blood flow in rats, and its distribution in the brain is consistent with the areas where the cholinergic system is enriched[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 139886-32-1
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Masse moléculaire 154.21
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Formule C8H14N2O
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SMILES
CO/N=C/C1=CCCN(C)C1
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Synonyms
CI-979; RU35926
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Milameline Related Classifications
HY-135460 Related Classifications
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