150151-15-8
Chemical Structure
LR1143
- CAS No.: 150151-15-8
- Formula:C29H34F2N2O
- Molecular Weight:464.59
IUPAC Name: 1-(2-(bis(4-fluorophenyl)methoxy)ethyl)-4-(3-phenylpropyl)-1,4-diazepane
InChIKey: DUNNQMCSUALPMK-UHFFFAOYSA-N
SMILES: FC1=CC=C(C=C1)C(OCCN2CCN(CCC2)CCCC3=CC=CC=C3)C4=CC=C(C=C4)F
Biological Activity: 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[1].
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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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- [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]
Keywords
