LR1143
LR1143 is a dopamine transporter (DAT) and 5-HT uptake inhibitor, with IC50 values of 3.4 nM and 112 nM in rats, respectively. LR1143 binds to DAT labeled with the dopamine reuptake inhibitor GBR 12935 (HY-12242A), with an IC50 of 4.4 nM. LR1143 shows lower selectivity for DAT than for serotonin reuptake sites. LR1143 can be used in studies related to cocaine abuse.
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- CAS 番号: 150151-15-8
- 分子式: C29H34F2N2O
- 分子量:464.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
LR1143 exhibits high affinity for rat striatal DAT (IC50=4.4 nM) and inhibits [3H]DA reuptake in rat caudate nucleus (IC50=3.4 nM), with 33-fold selectivity for DA reuptake sites over 5HT reuptake sites (IC50=112 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:rat striatal
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Concentration:IC50 assay
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Incubation Time:18-24 h (DAT binding), 15 min ([3H]DA reuptake), 30 min ([3H]5HT reuptake)
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Result:Exhibited high affinity for rat striatal DAT with an IC50 of 4.4 nM, inhibits [3H]DA reuptake in the rat caudate nucleus with an IC50 of 3.4 nM, and demonstrates 33-fold selectivity for DA reuptake sites over 5HT reuptake sites, which have an IC50 of 112 nM.
化学情報
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CAS 番号 150151-15-8
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分子量 464.59
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分子式 C29H34F2N2O
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SMILES
FC1=CC=C(C=C1)C(OCCN2CCN(CCC2)CCCC3=CC=CC=C3)C4=CC=C(C=C4)F
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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
[1]. Matecka D, et al. Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909). J Med Chem. 1996;39(24):4704-4716. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)