| Identification | Back Directory | [Name]
5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine | [CAS]
1184971-51-4 | [Synonyms]
5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine | [Molecular Formula]
C11H10BrN5 | [MOL File]
1184971-51-4.mol | [Molecular Weight]
292.14 |
| Hazard Information | Back Directory | [Description]
Brimonidine-d4 is intended for use as an internal standard for the quantification of brimonidine 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).1 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.2 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.3 Formulations containing brimonidine have been used in the treatment of open-angle glaucoma and ocular hypertension. | [storage]
Store at -20°C | [References]
1. Munk, S.A., Harcourt, D.A., Arasasingham, P.N., et al. Synthesis and evaluation of 2-(arylamino)imidazoles as α2-adrenergic agonists J. Med. Chem. 40(1),18-23(1997).
2. Sawada, K., Hiraoka, M., and Ohguro, H. Effect of antiglaucoma medicine on intraocular pressure in DBA/2J mice Ophthalmic Res. 55(4),205-211(2016).
3. Lee, D., Kim, K.Y., Noh, Y.H., et al. Brimonidine blocks glutamate excitotoxicity-induced oxidative stress and preserves mitochondrial transcription factor A in ischemic retinal injury PLoS One 7(10),e47098(2012). |
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