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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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5-HT6 Receptor |
5-HT6 Receptor 0.83 nM (Ki) |
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| 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.
Protocols
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
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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