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.
For research use only. We do not sell to patients.
- CAS No.: 3055537-47-5
- Formula: C19H15F2N3O
- Molecular Weight:339.34
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
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.
-
Animal Model:Sprague-Dawley (male)[1]
-
Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
-
Administration:p.o.; single dose
-
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.
-
Animal Model:Sprague-Dawley (male)[1]
-
Dosage:5.6 mg/kg; 10 mg/kg; 30 mg/kg; 56.6 mg/kg
-
Administration:p.o.; single dose
-
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.
-
Animal Model:Sprague-Dawley (male)[1]
-
Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
-
Administration:p.o.; single dose
-
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.
-
Animal Model:Sprague-Dawley (male)[1]
-
Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
-
Administration:p.o.; single dose
-
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.
-
Animal Model:unspecified[1]
-
Dosage:10 mg/kg
-
Administration:i.p.; daily; 2 days
-
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
-
CAS No. 3055537-47-5
-
Molecular Weight 339.34
-
Formula C19H15F2N3O
-
SMILES
FC1=CC(F)=CC=C1C2=CC3=C(CNC3=O)C(C4=CC(C)=NN4C)=C2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
VU6066098 Related Classifications
HY-184596 Related Classifications
Powered by Bioz