AGN 192836

AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Cardiovascular Disease

EC50: 8.7 nM (α2A), 41 nM (α2B), 6.6 nM (α2C)[1] Ki: 1.7 nM (α2A), 82 nM (α2B), 19 nM (α2C)[1]

Binding assays demonstrates that AGN 192836 is 1200-fold selective for the α2A-receptor relative to the α1-receptor, 50-fold selective for the α2A-receptor relative to the α2B-receptor, and 10-fold selective for the α2Areceptor relative to the α2C-receptor[1].

AGN 192836 is equally efficacious when compared to brimonidine for the reduction of intraocular pressure upon topical administration to the rabbit and more efficacious than brimonidine for the reduction of blood pressure upon intravenous administration to monkey[1].

Rabbit: A single drop of either brimonidine or AGN 192836 (0.001%) is applied unilaterally to rabbit eyes, and the intraocular pressure is monitored for 6 h post-administration[1].

[1]. Stephen M, et al. Synthesis and Evaluation of 2-(Arylamino)imidazoles as α2-Adrenergic Agonists. J. Med. Chem., 1997, 40 (1), pp 18–23

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