Idalopirdine
Idalopirdine (Lu AE58054 ) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
For research use only. We do not sell to patients.
- CAS No.: 467459-31-0
- Formula: C20H19F5N2O
- Molecular Weight:398.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT6 Receptor |
5-HT6 Receptor 0.83 nM (Ki) |
Idalopirdine (1 or 2 mg/kg, i.v) can dose-dependently increase the gamma power during nPO electrical stimulation, enhance effect of donepezil on cortical gamma oscillations but no alteration of sleep-wake patterns in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats[1]
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Dosage:5 mg/kg
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Administration:intraperitoneal injection, daily, 28 days
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Result:Significantly reduced the amount of calories consumed by animals in a palatable diet and significantly reduced plasma levels of glucose, triglycerides and cholesterol.
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Animal Model:Male Sprague-Dawley rats[2]
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Dosage:1 or 2 mg/kg
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Administration:i.v.
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Result:No significant increase in the gamma power at 1 mg/kg and significantly increased the gamma power at 2 mg/kg.
Significantly enhanced and/or prolonged effect of low-dose donepezil (0.3 mg/kg) on gamma power during 60-minute nPO stimulation after donepezil administration.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 467459-31-0
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Molecular Weight 398.37
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Formula C20H19F5N2O
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SMILES
FC1=CC(NC=C2CCNCC3=CC(OCC(F)(C(F)F)F)=CC=C3)=C2C=C1
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Synonyms
Lu AE58054
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Magdalena Kotańska, et al. Idalopirdine, a selective 5-HT6 receptor antagonist, reduces food intake and body weight in a model of excessive eating. Metab Brain Dis. 2018 Jun;33(3):733-740. [Content Brief]
[2]. Maria Amat-Foraster, et al. The 5-HT6 receptor antagonist idalopirdine potentiates the effects of donepezil on gamma oscillations in the frontal cortex of anesthetized and awake rats without affecting sleep-wake architecture. Neuropharmacology. 2017 Feb;113(Pt A):45-5 [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Idalopirdine Related Classifications
HY-14338 Related Classifications
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