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. Nr.: 150151-15-8
- Formel: C29H34F2N2O
- Molecular Weight:464.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
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. Further protocols information, click here.
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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.
Chemical Information
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CAS. Nr. 150151-15-8
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Molecular Weight 464.59
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LR1143 Related Classifications
HY-124186 Related Classifications
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