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Cat. No.: HY-182504

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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
화학식: C₂₅H₂₄F₂N₄OS
분자량:466.55

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

NRA-0562 Chemical Structure

CAS No.: 244276-65-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
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Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

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-HT_2A Receptor

All Dopamine Receptor Isoforms :

All 5-HT Receptor Isoforms :

All Adrenergic Receptor Isoforms :

In Vitro

NRA-0562 exhibits high binding affinity for human cloned dopamine D₁, D₂, D₃, and D₄ receptors, with the highest affinity for D₄ receptors (K_i = 1.79 nM) and lowest for D₁ receptors (K_i = 7.09 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NRA‑0562 (0.1-1 mg/kg, i.v., sequentially administered every 2-3 minutes) dose-dependently reverses induced inhibition of rat A9 and A10 dopamine neuron firing activity,, with 3-fold greater potency for A10 (ED₅₀ = 0.3 mg/kg) than A9 (ED₅₀ = 0.9 mg/kg) neurons^[1].
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.

Animal Model:

Wistar (male, 300-400 g, electrophysiological studies, methamphetamine-induced dopamine neuron inhibition model)^[1]
Dosage:

0.1 ; 0.2 ; 0.7 ;1 mg/kg
Administration:

i.v.; sequentially every 2-3 minutes
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.

Animal Model:

Wistar (male, 280-320 g, immunohistochemical studies)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

i.p.
Result:

Increased Fos-like positive nuclei counts in the nucleus accumbens and dorsolateral striatum dose-dependently and significantly at all tested doses.

Chemical Information

CAS No. 244276-65-1
분자량 466.55
화학식 C₂₅H₂₄F₂N₄OS
SMILES

O=C(C1=NC(C2=CC=C(C=C2)F)=C(CCN3CCC(CC3)C4=CNC5=C4C=CC(F)=C5)S1)N
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Kawashima N, et al. Neuropharmacological profiles of a novel atypical antipsychotic, NRA0562, in rats. Eur J Pharmacol. 2001;423(1):27-33. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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NRA-0562

All Dopamine Receptor Isoforms

All 5-HT Receptor Isoforms

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

NRA-0562 Related Classifications

HY-182504 Related Classifications