NSD 1034
NSD 1034 is a potent inhibitor of aromatic L-amino acid decarboxylase (AADC) and tyrosine aminotransferase (TAT), with IC50 values of 0.32 μM and 80 μM, respectively. NSD 1034 increases dopamine synthesis and release by inhibiting AADC and TAT, and stimulating tyrosine hydroxylase in dopaminergic neurons via calcium influx in a classical dopamine receptor-independent manner. NSD 1034 is used in studies of Parkinson's disease and sleep disorders.
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- CAS. Nr.: 555-62-4
- Formel: C8H12N2O
- Molecular Weight:152.19
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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
Beschreibung
IC50 & Target
[1]|
AADC 0.32 μM (IC50) |
TAT 80 μM (IC50) |
In Vitro
NSD 1034 (80 μM) inhibits male Wistar rat liver tyrosine aminotransferase in vitro with an IC50 of 80 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NSD 1034 (12.5-200 mg/kg; s.c.; single dose; treatment for 10-60 min) dose- and time-dependently increases DOPA accumulation in the striatum, cerebral hemispheres, and limbic areas, as well as 5-HTP accumulation in all tested brain regions in a rat model[1].
NSD 1034 (2-400 mg/kg; s.c.; single dose; treatment for 2-4 h) reduces p-tyramine concentrations and bidirectionally modulates m-tyramine concentrations in the striatum in an albino Swiss mouse model[3].
NSD 1034 (100 mg/kg; s.c.; single dose; during electrophysiological recording) does not alter the firing frequency of dopaminergic neurons in the substantia nigra in anesthetized rat models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 220-400 g)[1]
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Dosage:12.5 mg/kg, 25 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 107 mg/kg, 268 mg/kg
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Administration:s.c.; single dose; 10, 20, 30, 45, 60 min
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Result:Promote DOPA accumulation in the striatum and inhibit AADC activity.
Increased DOPA accumulation in the striatum, cerebral hemispheres, and limbic regions, and increased 5-HTP accumulation in all brain regions examined, in a dose- and time-dependent manner.
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Animal Model:albino Swiss mice (male, 18-22 g body weight)[3]
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Dosage:2, 20, 400 mg/kg
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Administration:s.c.; single dose; 2 or 4 h
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Result:Significantly reduced the concentration of p-tyramine in the mouse striatum at all tested doses (2, 20, 400 mg/kg).
Mildly increased the concentration of m-tyramine at lower doses (2 and 20 mg/kg), but significantly reduced the concentration of m-tyramine at the high dose (400 mg/kg).
Chemical Information
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CAS. Nr. 555-62-4
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Molecular Weight 152.19
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Formel C8H12N2O
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SMILES
OC1=CC=CC(CN(C)N)=C1
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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
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
NSD 1034 Related Classifications
HY-187668 Related Classifications
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