Formulation: A solid
Formal Name: 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl-4,4,5,5-d4)quinoxalin-6-amine
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C11H6BrD4N5
Formula Weight: 296,2
Shelf life (days): 730
CAS Number: 1184971-51-4
Notes: Brimonidine-d4 is intended for use as an internal standard for the quantification of brimonidine (Item No. 15426) by GC- or LC-MS. Brimonidine is an agonist of α2-adrenergic receptors (α2-ARs; Kis = 2.7, 52, and 44 nM for α2A, α2B, and α2C-ARs, respectively, in CHO cells).{42418} It is selective for α2-ARs over α1-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.{42419} 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.{25329} Formulations containing brimonidine have been used in the treatment of open-angle glaucoma and ocular hypertension.