Dopamine D4R antagonist-1
Dopamine D4R antagonist-1 is a blood-brain barrier-permeable antagonist of dopamine D4 receptor. Dopamine D4R antagonist-1 functionally inhibits dopamine D4 receptor, exhibits only weak activity against dopamine D3 receptor, and shows no activity against dopamine D1 and D2 receptors.
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- No. CAS: 1379510-21-0
- Fòrmula: C20H23N3O
- Peso molecular:321.42
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Dopamine D4 receptor |
In Vitro
(R)-dopamine D4R antagonist-1 (compound 1) potently inhibits and binds to human D4 receptors with an IC50 of 180 nM and Ki of 70 nM, while showing no activity against human D1 and D2 receptors, weak activity against human D3 receptors, and the racemic and (S)-enantiomer forms are significantly less active or inactive[1].
Dopamine D4R antagonist-1 exhibits moderate predicted hepatic clearance in rat and human hepatic microsomes, low free fraction in human plasma and high free fraction in rat plasma, and inhibits multiple human CYP enzymes with varying potencies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Plasma Concentration | Brain Concentration | CLhepatic |
|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 1935 nM | 3558 nM | 65.1 mL/min/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Showed non-significant linear trend of reversing cocaine-induced hyperlocomotion at 3 mg/kg.
Showed non-significant linear trend of reversing cocaine-induced hyperlocomotion at 10 mg/kg.
Chemical Information
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No. CAS 1379510-21-0
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Peso molecular 321.42
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Fòrmula C20H23N3O
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SMILES
C(C=1NC=2C(N1)=CC=CC2)N3C[C@@H](CCC4=CC=CC=C4)OCC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dopamine D4R antagonist-1 Related Classifications
HY-130203 Related Classifications
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