VU6066098
VU6066098 is a blood-brain barrier penetrant, orally active inhibitor of metabotropic glutamate receptor subtype 2 (mGlu2), with IC50 values of 77 nM and 111 nM against human and rat targets, respectively. VU6066098 induces antidepressant-like activity, inhibits psychosis-like hyperlocomotion, enhances recognition memory and associative learning, and reverses cognitive deficits caused by blast-related traumatic brain injury. VU6066098 can be used in research on major depressive disorder, schizophrenia, Alzheimer's disease, and traumatic brain injury.
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- No. CAS: 3055537-47-5
- Fòrmula: C19H15F2N3O
- Peso molecular:339.34
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
VU6066098 potently and selectively inhibits human mGlu2 receptors in an mGlu2/GIRK assay with an IC50 of 77 nM, while showing no significant activity against most other human mGlu receptor subtypes[1].
VU6066098 inhibits human mGlu2 receptor activity in a cAMP assay with an IC50 of 114 nM[1].
VU6066098 potently inhibits rat mGlu2 receptors with an IC50 of 111 nM, while showing no significant activity against most other rat mGlu receptor subtypes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
VU6066098 (5.6-56.6 mg/kg; p.o.; single dose) exhibits antipsychotic-like activity in rats with an oral minimum effective dose of 30 mg/kg, reversing amphetamine-induced hyperlocomotion in a dose-dependent manner[1].
VU6066098 (1-10 mg/kg; p.o.; single dose) enhances long-term recognition memory in rats with an oral minimum effective dose of 3 mg/kg, producing a robust improvement in recognition index[1].
VU6066098 (0.1-1 mg/kg; p.o.; single dose) enhances associative learning and long-term memory in rats with an oral minimum effective dose of 0.3 mg/kg, increasing percent freezing behavior in contextual fear conditioning[1].
VU6066098 (10 mg/kg; i.p.; daily; 2 days) reverses cognitive deficits in a rat blast-related TBI model when administered at 10 mg/kg i.p. for 2 days, with effects lasting up to 30 days post-dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Reduced immobility time in a dose-dependent manner, with significant effects at all tested doses compared to vehicle.
Reached total brain levels of 230 nM (2.1-fold the rat mGlu2 IC50) and free brain levels of 3.1 nM (0.03-fold the rat mGlu2 IC50) at 1 mg/kg p.o.
Reached total brain levels of 4.9 μM (43.9-fold the rat mGlu2 IC50) and free brain levels of 67 nM (0.59-fold the rat mGlu2 IC50) at 10 mg/kg p.o., with efficacy comparable to 10 mg/kg s.c. ketamine.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:5.6 mg/kg; 10 mg/kg; 30 mg/kg; 56.6 mg/kg
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Administration:p.o.; single dose
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Result:Reversed amphetamine-induced hyperlocomotion in a dose-dependent manner, with significant effects at 30 mg/kg and 56.6 mg/kg p.o.
Produced total brain levels of 12.9 μM and free brain levels of 174 nM (1.55-fold the rat mGlu2 IC50) at 30 mg/kg p.o.
Reached total brain levels of 14.9 μM and free brain levels of 202 nM (1.79-fold the rat mGlu2 IC50) at 56.6 mg/kg p.o., with efficacy magnitude comparable to the positive control VU0467154.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Enhanced recognition memory in a dose-dependent manner, with significant increases in recognition index observed at 3 mg/kg and 10 mg/kg p.o.
Produced total brain levels of 1.2 μM (10.5-fold the rat mGlu2 IC50) and free brain levels of 15.9 nM (0.14-fold the rat mGlu2 IC50) at 3 mg/kg p.o.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
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Administration:p.o.; single dose
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Result:Enhanced acquisition of contextual fear conditioning in a dose-dependent manner, with significant increases in percent freezing observed at 0.3 mg/kg and 1 mg/kg p.o.
Produced total brain levels of 46 nM (0.41-fold the rat mGlu2 IC50) and free brain levels of 0.62 nM (0.005-fold the rat mGlu2 IC50) at 0.3 mg/kg p.o.
Reached total brain levels of 318 nM (2.83-fold the rat mGlu2 IC50) and free brain levels of 4.29 nM (0.038-fold the rat mGlu2 IC50) at 1 mg/kg p.o.
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Animal Model:unspecified[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 2 days
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Result:Reversed blast-induced deficits in novel object recognition for both short-term and long-term memory, with significant improvements in discrimination index compared to vehicle-treated blast-exposed rats.
Sustained the memory-enhancing effect for at least 30 days after the last dose administration.
Chemical Information
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No. CAS 3055537-47-5
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Peso molecular 339.34
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Fòrmula C19H15F2N3O
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SMILES
FC1=CC(F)=CC=C1C2=CC3=C(CNC3=O)C(C4=CC(C)=NN4C)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU6066098 Related Classifications
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