BRL 44408 (maleate)

BRL 44408 is an antagonist of alpha2A-adrenergic receptors (alpha2A-ARs, Ki = 8.56 nM for the recombinant human receptors). It is greater than 50-fold selective for alpha2A-ARs over alpha1-, alpha2B-, alpha2C-, beta1-, and beta2-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 alpha2A-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.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: DMF: 30 mg/ml, DMSO: 30 mg/ml, PBS (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.