LSN2814617
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research.
For research use only. We do not sell to patients.
- CAS No.: 1313498-17-7
- Formula: C18H20FN5O
- Molecular Weight:341.38
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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
Biological Activity
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rat mGluR5 42 ± 9 nM (IC50) |
human mGluR5 52 ± 21 nM (IC50) |
LSN2814617 (1nM-10 μM) fails to elicit responses alone in rat cortical neurons, and evokes a concentration-dependent increase in the [Ca2+]i response in AV12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LSN2814617 (0-10 mg/kg, Orally, once) significantly modulates amphetamine-induced locomotor hyperactivity[1].
LSN2814617 (0-3 mg/kg, Orally, once) markedly increase wakefulness[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Lister Hooded rats (180-250 g, four to eight per cage)[1]
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Dosage:0, 2.5, 5, and 10 mg/kg
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Administration:Orally, once, 60 min before amphetamine
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Result:Significantly modulated amphetamine hyperactivity, although a trend level decrease in hyperactivity was observed for the highest dose. At the end of the test session, from 75 to 120 min, the 10 mg/kg dose of LSN2814617 significantly increased amphetamine-induced hyperactivity.
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Animal Model:Adult male Wistar rats (approximately 270 g)[1]
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Dosage:0, 0.3, 1, and 3 mg/kg
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Administration:Orally, once
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Result:Displayed dose-dependently increase in wakefulness immediately following oral administration; Produced 234 ± 16 min of increased wake for over 7 h in the case of 3 mg/kg. Produced dose-dependent reductions in both NREM and REM sleep.
Chemical Information
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CAS No. 1313498-17-7
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Molecular Weight 341.38
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Formula C18H20FN5O
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SMILES
FC1=CC=C(C=C1)C2=NOC([C@@H]3CC4=NN=C(N4CC3)C(C)(C)C)=N2
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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