CE-103
CE-103 is a selective, blood-brain barrier-permeable dopamine transporter (DAT) inhibitor with an IC50 of 14.73 μM. CE-103 blocks DAT-mediated dopamine reuptake and exhibits antagonistic activity against 5-HT1A. CE-103 reduces working memory errors in the radial arm maze test of rats, decreases the levels of complexes containing phosphorylated DAT (pDAT) and D1R in the hippocampus of rats, and increases the levels of complexes containing D2R and D3R simultaneously. CE-103 can be used in studies related to dopaminergic neurotransmission, working memory and cognitive function.
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- CAS 番号: 1879038-73-9
- 分子式: C17H15NOS2
- 分子量:313.44
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保管条件:
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]
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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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Help & FAQs
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生物活性
CE-103 inhibits hDAT-mediated dopamine reuptake in HEK293 cells with an IC50 of 14.73 μM, with weak activity on hNET and no activity on hSERT.
CE-103 (10 μM) acts as a dopamine transporter inhibitor, not a substrate, as it does not induce significant substrate efflux in HEK-DAT cells even under elevated intracellular sodium conditions[1].
CE-103 (10 μM) shows selective antagonist activity on the 5HT1A receptor (64.1% inhibition at 10 μM) with no significant activity on 17 other tested GPCR targets[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax (Plasma) |
|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 15 min |
CE-103 (10 mg/kg; i.p.; once daily for 10 consecutive days) reduces the levels of D1R and pDAT complexes in the hippocampus of trained rats, increases the levels of D2R and D3R complexes, and regulates the levels of DAT complexes. It exerts anxiolytic-like effects on rats in the elevated plus maze test without altering their motor ability, motor coordination, or depressive-like behavior[1].
CE-103 (10 mg/kg; i.p.; single administration) is detectable in rat plasma and cerebrospinal fluid, with a Tmax of 15 min in plasma and 30 min in cerebrospinal fluid[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, 12-14 weeks old)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Reduced working-memory errors from days 8 to 10 without affecting reference-memory errors.
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Animal Model:Sprague Dawley (male, 12-14 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Increased open-arm time without impairing locomotion, motor coordination or neurological behavior.
Reduced D1R- and pDAT-containing complexes, increased D2R- and D3R-containing complexes, and altered DAT-containing complex levels.
化学情報
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CAS 番号 1879038-73-9
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分子量 313.44
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分子式 C17H15NOS2
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SMILES
O=S(C(C1=CC=CC=C1)C2=CC=CC=C2)CC3=CN=CS3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CE-103 関連分類
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