BRL 44408 (maleate)

BRL 44408 (maleate)

CAT N°: 29454
Price:

129.00 109.65

BRL 44408 is an antagonist of ?2A-adrenergic receptors (?2A-ARs; Ki = 8.56 nM for the recombinant human receptors).{45714} It is greater than 50-fold selective for ?2A-ARs over ?1-, ?2B-, ?2C-, ?1-, and ?2-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 ?2A-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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