2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor 5-HT Receptor Adrenergic Receptor
  4. 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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NRA-0562

NRA-0562 Chemical Structure

CAS No. : 244276-65-1

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NRA-0562 Related Antibodies

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Description

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[1].[1].

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-HT2A Receptor

 

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 (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 Related Antibodies
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.
Molecular Weight

466.55

Formula

C25H24F2N4OS
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NRA-0562 Related Classifications

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Keywords:

NRA-0562244276-65-1NRA0562NRA 0562Dopamine Receptor5-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptorfunctional dopamine antagonistdopamine D1/D2/D3/D4 receptor5-HT?A receptorα?-adrenoceptormethamphetaminedopamine neuronFos-like immunoreactivityatypical indexratschizophreniaInhibitorinhibitorinhibit

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