Blixeprodil
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.
- CAS No.: 2881017-49-6
- Formula: C13H16FNO
- Molecular Weight:221.27
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Storage:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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.
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.
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Animal Model:Wistar-Kyoto (adult male)[1]
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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
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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.
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Animal Model:Wistar-Han (adult male)[1]
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Dosage:0.75 mg/kg; 1.5 mg/kg; 3 mg/kg; 9 mg/kg
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Administration:i.p.; weekly; 5 weeks
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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.
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Animal Model:Sprague-Dawley (adult male)[1]
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Dosage:1 mg/kg; 3.2 mg/kg; 10 mg/kg; 32 mg/kg
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Administration:s.c.; single dose
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Result:Produced significant, dose-dependent reductions in immobility time.
Achieved maximal efficacy at 3.2 mg/kg, with efficacy comparable to positive control desipramine.
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Animal Model:Sprague-Dawley (adult male); C57BL6/J (adult male)[1]
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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
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2881017-49-6
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Appearance Oil
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Molecular Weight 221.27
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Formula C13H16FNO
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Color Colorless to light yellow
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SMILES
CN[C@]1(C2=CC=C(C=C2)F)C(CCCC1)=O
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Synonyms
GM-1020
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (278 KB)
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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)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Blixeprodil Related Classifications
HY-172419 Related Classifications
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