NRA-0562
NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia..
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- CAS No.: 244276-65-1
- Formule: C25H24F2N4OS
- Masse moléculaire:466.55
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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Human D1 Receptor 7.09 nM (Ki) |
Human D2 Receptor 2.49 nM (Ki) |
Human D3 Receptor 3.48 nM (Ki) |
Human D4 Receptor 1.79 nM (Ki) |
α1-adrenergic receptor |
5-HT2A Receptor |
NRA-0562 exhibits high binding affinity for human cloned dopamine D1, D2, D3, and D4 receptors, with the highest affinity for D4 receptors (Ki = 1.79 nM) and lowest for D1 receptors (Ki = 7.09 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NRA-0562 (1-30 mg/kg; i.p.) dose-dependently increases Fos-like immunoreactivity in the rat nucleus accumbens and dorsolateral striatum, with a positive atypical index consistent with atypical antipsychotic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 300-400 g, electrophysiological studies, methamphetamine-induced dopamine neuron inhibition model)[1]
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Dosage:0.1 ; 0.2 ; 0.7 ;1 mg/kg
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Administration:i.v.; sequentially every 2-3 minutes
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Result:Reversed methamphetamine-induced inhibition of A9 and A10 dopamine neurons dose-dependently and significantly.
Achieved ED50 values of 0.3 mg/kg (A10) and 0.9 mg/kg (A9) for reversing dopamine neuron inhibition.
Showed no apparent effect on baseline firing rates of A9 or A10 dopamine neurons at 0.1-1 mg/kg.
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Animal Model:Wistar (male, 280-320 g, immunohistochemical studies)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.p.
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Result:Increased Fos-like positive nuclei counts in the nucleus accumbens and dorsolateral striatum dose-dependently and significantly at all tested doses.
Chemical Information
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CAS No. 244276-65-1
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Masse moléculaire 466.55
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Formule C25H24F2N4OS
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SMILES
O=C(C1=NC(C2=CC=C(C=C2)F)=C(CCN3CCC(CC3)C4=CNC5=C4C=CC(F)=C5)S1)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NRA-0562 Related Classifications
HY-182504 Related Classifications
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