Brimonidine (tartrate)

Brimonidine is an agonist of alpha2-adrenergic receptors (alpha2-ARs, Kis = 2.7, 52, and 44 nM for alpha2A, alpha2B, and alpha2C-ARs, respectively, in CHO cells). It is selective for alpha2-ARs over alpha1-ARs (Ki = 1,800 nM in human brain). Brimonidine lowers intraocular pressure in DBA/2J mice, a model of glaucoma, to control levels when applied topically to the eye as a 0.1% solution. It also inhibits glutamate release, prevents upregulation of NMDA receptors containing NR1 and NR2A subunits, and protects rat retinal ganglion cells against glutamate excitotoxicity in a rat model of retinal ischemia when administered at a dose of 1 mg/kg per day. Formulations containing brimonidine have been used in the treatment of open-angle glaucoma and ocular hypertension.Formal Name: 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-6-quinoxalinamine, 2R,3R-dihydroxybutanedioate. CAS Number: 70359-46-5. Synonyms: AGN 190342LF, Alphagan P. Molecular Formula: C11H10BrN5 . C4H6O6. Formula Weight: 442.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 1 mg/ml, PBS (pH 7.2): 3 mg/ml. lambdamax: 244, 320 nm. SMILES: BrC1=C(NC2=NCCN2)C=CC3=C1N=CC=N3.O[C@H]([C@@H](O)C(O)=O)C(O)=O. InChi Code: InChI=1S/C11H10BrN5.C4H6O6/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8,5-1(3(7)8)2(6)4(9)10/h1-4H,5-6H2,(H2,15,16,17),1-2,5-6H,(H,7,8)(H,9,10). InChi Key: QZHBYNSSDLTCRG-UHFFFAOYSA-N.