An α2A-AR antagonist
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $95

    Add

    10 mg

    $168

    Add

    25 mg

    $370

    Add
    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).