Blixeprodil
Based on 1 Customer Validation
Blixeprodil (GM-1020) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil can be used in the research of depression.
For research use only. We do not sell to patients.
- Purity : 95.0%
- CAS No.: 2881017-49-6
- Formula: C13H16FNO
- Molecular Weight:221.27
-
Storage:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All iGluR Isoforms
More
Biological Activity
Description
In Vitro
Blixeprodil (GM-1020) binds to NMDA receptors in rat brain homogenates with a Ki value of 3.25 µM[1].
Blixeprodil inhibits the functional activities of both NR1/NR2A and NR1/NR2B NMDA receptors in Xenopus laevis oocytes with similar potency, with IC50 values of 3.70 µM and 4.16 µM, respectively[1].
Blixeprodil inhibits NR1/2A NMDA receptor-mediated currents in HEK293 cells with an IC50 of 1.192 µM, and blocks the receptor in a voltage-dependent manner;
Blixeprodil binds to the human μ-opioid receptor in transfected HEK cells, with a Ki value of 19 µM[1].
Blixeprodil exhibits selective binding to NMDA receptors across a broad panel of off-targets, with weak binding affinity for the serotonin transporter (Ki = 6.2 µM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Blixeprodil (0.75-9 mg/kg; i.p.; weekly; 5 weeks) reverses CMS-induced depressive-like phenotypes in rats at doses ≥1.5 mg/kg i.p., with effects durable for up to 15 days after the final weekly dose[1].
Blixeprodil (1.5-9 mg/kg; i.p.; single dose; 1-10 mg/kg; p.o.; single dose) restores CMS-induced anhedonia in rats for up to 14 days post-dose[1].
Blixeprodil (1-32 mg/kg; s.c.; single dose) produces motor impairment in rats and mice only at doses ≥ 10 mg/kg s.c., with a 12-fold separation between efficacious plasma exposures for antidepressant-like effects and those causing ataxia in rats[1].
Blixeprodil (1-10 mg/kg; s.c.; single dose) produces dose-dependent changes in rat cortical EEG indicative of NMDA receptor target engagement[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Wistar-Kyoto (adult male)[1]
-
Dosage:1.5 mg/kg (i.p.); 9 mg/kg (i.p.)
1 mg/kg (p.o.); 3.2 mg/kg (p.o.); 10 mg/kg (p.o.) -
Administration:i.p.; single dose; p.o.; single dose
-
Result:Restored sucrose intake to near unstressed levels for 14 days post-dose at single i.p. doses of 1.5 and 9 mg/kg, with effects returning to stressed baseline levels by 21 days.
Produced dose-dependent increases in sucrose intake via oral administration.
Restored sucrose intake to unstressed levels 24 hours post-dose at 10 mg/kg oral dose.
Reached peak plasma concentration of 257 ng/mL at 10 mg/kg oral minimum efficacious dose.
-
Animal Model:Wistar-Han (adult male)[1]
-
Dosage:0.75 mg/kg; 1.5 mg/kg; 3 mg/kg; 9 mg/kg
-
Administration:i.p.; weekly; 5 weeks
-
Result:Reversed CMS-induced deficits in sucrose intake within the first week of treatment at doses of 1.5, 3, and 9 mg/kg, with effects durable through 15 days after the final dose.
Failed to produce effects at 0.75 mg/kg dose.
Reversed CMS-induced anxiety (reduced % time in open arms in EPM) at 48 hours post-dose at 1.5 mg/kg dose.
Reversed CMS-induced memory impairment (reduced NOR recognition index) at 72 hours post-dose at 1.5 mg/kg dose.
Reached peak plasma concentration of 151 ng/mL at 1.5 mg/kg minimum efficacious dose.
-
Animal Model:Sprague-Dawley (adult male)[1]
-
Dosage:1 mg/kg; 3.2 mg/kg; 10 mg/kg; 32 mg/kg
-
Administration:s.c.; single dose
-
Result:Produced significant, dose-dependent reductions in immobility time.
Achieved maximal efficacy at 3.2 mg/kg, with efficacy comparable to positive control desipramine.
-
Animal Model:Sprague-Dawley (adult male); C57BL6/J (adult male)[1]
-
Dosage:Rats: 3.2 mg/kg; 10 mg/kg; 32 mg/kg
Mice: 1 mg/kg; 3.2 mg/kg; 10 mg/kg; 32 mg/kg -
Administration:s.c.; single dose
-
Result:Increased spontaneous locomotor activity (sLMA) only at 32 mg/kg in rats.
Decreased rotarod latency at 10 and 32 mg/kg in rats, with an ED50 for ataxia of 17.4 mg/kg (interpolated plasma concentration = 1,876 ng/mL), ~12-fold higher than the plasma concentration at the CMS minimum efficacious dose (151 ng/mL).
Left sLMA unaffected at all doses in mice.
Decreased rotarod latency only at 10 and 32 mg/kg in mice, with an ED50 for ataxia of 37.4 mg/kg.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2881017-49-6
-
Appearance Oil
-
Molecular Weight 221.27
-
Formula C13H16FNO
-
Color Colorless to light yellow
-
SMILES
CN[C@]1(C2=CC=C(C=C2)F)C(CCCC1)=O
-
Synonyms
GM-1020
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (451.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
-
Data Sheet (282 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.5194 mL | 22.5968 mL | 45.1937 mL | 112.9841 mL |
| 5 mM | 0.9039 mL | 4.5194 mL | 9.0387 mL | 22.5968 mL | |
| 10 mM | 0.4519 mL | 2.2597 mL | 4.5194 mL | 11.2984 mL | |
| 15 mM | 0.3013 mL | 1.5065 mL | 3.0129 mL | 7.5323 mL | |
| 20 mM | 0.2260 mL | 1.1298 mL | 2.2597 mL | 5.6492 mL | |
| 25 mM | 0.1808 mL | 0.9039 mL | 1.8077 mL | 4.5194 mL | |
| 30 mM | 0.1506 mL | 0.7532 mL | 1.5065 mL | 3.7661 mL | |
| 40 mM | 0.1130 mL | 0.5649 mL | 1.1298 mL | 2.8246 mL | |
| 50 mM | 0.0904 mL | 0.4519 mL | 0.9039 mL | 2.2597 mL | |
| 60 mM | 0.0753 mL | 0.3766 mL | 0.7532 mL | 1.8831 mL | |
| 80 mM | 0.0565 mL | 0.2825 mL | 0.5649 mL | 1.4123 mL | |
| 100 mM | 0.0452 mL | 0.2260 mL | 0.4519 mL | 1.1298 mL |
Blixeprodil Related Classifications
HY-172419 Related Classifications
Powered by Bioz