An α2A-AR antagonist
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BRL 44408 (maleate)

Item No. 29454

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole, 2Z-butenedioate
CAS Number
681806-46-2
Molecular Formula
C13H17N3 • C4H4O4
Formula Weight
331.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
CC1N(CC2=NCCN2)CC3=CC=CC=C31.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C13H17N3.C4H4O4/c1-10-12-5-3-2-4-11(12)8-16(10)9-13-14-6-7-15-13;5-3(6)1-2-4(7)8/h2-5,10H,6-9H2,1H3,(H,14,15);1-2H,(H,5,6)(H,7,8)/b;2-1-
InChi Key
DDIQGSUEJOOQQQ-BTJKTKAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $95

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    10 mg

    $168

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    25 mg

    $370

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    Product Description

    BRL 44408 is an antagonist of α2A-adrenergic receptors (α2A-ARs; Ki = 8.56 nM for the recombinant human receptors).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dwyer, J.M., Platt, B.J., Sukoff Rizzo, S.J., et al. Preclinical characterization of BRL 44408: Antidepressant- and analgesic-like activity through selective α2A-adrenoceptor antagonism. Int. J. Neuropsychopharmacol. 13(9), 1193-1205 (2010).