An antagonist of α2A-ARs (Ki = 8.56 nM for the recombinant human receptors); >50-fold selective for α2A-ARs over α1-

BRL 44408 (maleate) – 5 mg

Brand:
Cayman
CAS:
681806-46-2
Storage:
-20
UN-No:
Non-Hazardous - /

BRL 44408 is an antagonist of α2A-adrenergic receptors (α2A-ARs; Ki = 8.56 nM for the recombinant human receptors).{45714} It is greater than 50-fold selective for α2A-ARs over α1-, α2B-, α2C-, β1-, and β2-ARs, as well as 19 other neurotransmitter receptors, transporters, and enzymes in a panel at 1 µM. BRL 44408 inhibits forskolin-stimulated cAMP accumulation with an IC50 value of 92.3 nM in CHO cells expressing the recombinant human α2A-AR. It increases norepinephrine and dopamine levels by 200 and 100%, respectively, in rat medial prefrontal cortex when administered at a dose of 10 mg/kg. BRL 44408 (10 and 30 mg/kg) decreases the time rats spend immobile in the forced swim test, indicating antidepressant-like activity, and reduces para-phenylquinone-induced abdominal stretching, indicating analgesic activity, in rats.  

 

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Description

An antagonist of α2A-ARs (Ki = 8.56 nM for the recombinant human receptors); >50-fold selective for α2A-ARs over α1-, α2B-, α2C-, β1-, and β2-ARs, as well as 19 other neurotransmitter receptors, transporters, and enzymes in a panel at 1 µM; inhibits forskolin-stimulated cAMP accumulation (IC50 = 92.3 nM in CHO cells expressing the recombinant human α2A-AR); increases norepinephrine and dopamine levels by 200 and 100%, respectively, in rat medial prefrontal cortex at 10 mg/kg; decreases the time rats spend immobile in the forced swim test, indicating antidepressant-like activity at 10 and 30 mg/kg; reduces para-phenylquinone-induced abdominal stretching, indicating analgesic activity, in rats at 10 and 30 mg/kg

Formal name: 2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole, 2Z-butenedioate

Synonyms: 

Molecular weight: 331.4

CAS: 681806-46-2

Purity: ≥98%

Formulation: A crystalline solid

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