173294-84-3
Chemical Structure
Dehydrosertindole
- CAS No.: 173294-84-3
- Formula:C24H24ClFN4O
- Molecular Weight:438.93
IUPAC Name: 1-(2-(4-(5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl)piperidin-1-yl)ethyl)-1,3-dihydro-2H-imidazol-2-one
InChIKey: UWVZAIBLBVMRAN-UHFFFAOYSA-N
SMILES: O=C1NC=CN1CCN2CCC(C3=CN(C4=CC=C(F)C=C4)C=5C=CC(Cl)=CC53)CC2
Biological Activity: Dehydrosertindole is a blood-brain barrier-permeable, orally active inhibitor of the dopamine D2 receptor. Dehydrosertindole occupies striatal dopamine D2 receptors to mediate receptor regulation. Dehydrosertindole is the active metabolite of Sertindole (HY-14543), which distributes rapidly in guinea pig myocardium and inhibits conditioned avoidance responses in rats. Dehydrosertindole can be used in research related to schizophrenia[1][2].
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Dehydrosertindole | Dehydrosertindole is a blood-brain barrier-permeable, orally active inhibitor of the dopamine D2 receptor. Dehydrosertindole occupies striatal dopamine D2 receptors to mediate receptor regulation. Dehydrosertindole is the active metabolite of Sertindole (HY-14543), which distributes rapidly in guinea pig myocardium and inhibits conditioned avoidance responses in rats. Dehydrosertindole can be used in research related to schizophrenia. | |||||||||||||||||||||
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- [1]. Bundgaard C, et al. Pharmacokinetics of sertindole and its metabolite dehydrosertindole in rats and characterization of their comparative pharmacodynamics based on in vivo D2 receptor occupancy and behavioural conditioned avoidance response. Biopharmaceutics & drug disposition. 2009 May;30(4):209-20. [Content Brief]
- [2]. Canal-Raffin M, et al. Myocardium distribution of sertindole and its metabolite dehydrosertindole in guinea-pigs. Biopharmaceutics & drug disposition. 2006 May;27(4):171-9. [Content Brief]
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