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| | 5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine Basic information |
| Product Name: | 5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine | | Synonyms: | 5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine;5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl-4,4,5,5-d4)quinoxalin-6-amine | | CAS: | 1184971-51-4 | | MF: | C11H10BrN5 | | MW: | 292.14 | | EINECS: | | | Product Categories: | | | Mol File: | 1184971-51-4.mol |  |
| | 5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: soluble; Water: 1.5 mg/ml | | form | A solid |
| | 5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine Usage And Synthesis |
| 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. | | Uses | Brimonidine-d4 is the deuterium labeled Brimonidine. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist. | | 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). |
| | 5-bromo-N-(4,4,5,5-tetradeuterio-1H-imidazol-2-yl)quinoxalin-6-amine Preparation Products And Raw materials |
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