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.
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- CAS 番号: 2881017-49-6
- 分子式: C13H16FNO
- 分子量:221.27
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保管条件:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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 |
化学情報
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CAS 番号 2881017-49-6
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性状 Oil
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分子量 221.27
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分子式 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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別名
GM-1020
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (278 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Blixeprodil 関連分類
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