An α2-AR agonist (Kis = 2.7

Brimonidine (tartrate) – 50 mg

Brand:
Cayman
CAS:
70359-46-5
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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.  

 

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Description

An α2-AR agonist (Kis = 2.7, 52, and 44 nM for α2A, α2B, and α2C-ARs, respectively, in CHO cells); selective for α2-ARs over α1-ARs (Ki = 1,800 nM in human brain); lowers intraocular pressure in DBA/2J mice to control levels at 0.1% applied topically to the eye; protects rat retinal ganglion cells against glutamate excitotoxicity in a rat model of retinal ischemia at 1 mg/kg per day

Formal name: 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-6-quinoxalinamine, 2R,3R-dihydroxybutanedioate

Synonyms:  AGN 190342LF|Alphagan P

Molecular weight: 442.2

CAS: 70359-46-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Ophthalmology

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