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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- CAS. Nr.: 173294-84-3
- Formel: C24H24ClFN4O
- Molecular Weight:438.93
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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
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D2 Receptor 165 ng/mL (Kd) |
Dehydrosertindole (1-8 mg/kg; i.p.; single dose; daily for 8 days), a metabolite of Sertindole (HY-14543), readily distributes to guinea-pig myocardium[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 175-230 g for receptor binding studies, ~200 g at start of CAR training)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Yielded a potency estimate of 165 ng/mL for D2 receptor occupancy at the effect site.
Yielded a potency estimate of 424 ng/mL for CAR suppression at the effect site.
Exhibited a sigmoidicity factor (n) of 1.3 for D2 occupancy.
Exhibited a sigmoidicity factor (n) of 2.7 for CAR behaviour.
Showed a temporal delay between plasma concentrations and effects resolved using effect compartment models with ke0 = 0.67 h-1 for D2 occupancy and ke0 = 1.10 h-1 for CAR behaviour.
Chemical Information
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CAS. Nr. 173294-84-3
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Molecular Weight 438.93
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Formel C24H24ClFN4O
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SMILES
O=C1NC=CN1CCN2CCC(C3=CN(C4=CC=C(F)C=C4)C=5C=CC(Cl)=CC53)CC2
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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.
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Dehydrosertindole Related Classifications
HY-118477 Related Classifications
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