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GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(–) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists.

GAT229 is a CB1 positive allosteric modulator (PAM) that effectively reduces intraocular pressure (IOP) in high IOP mouse models and enhances CB1 receptor-mediated IOP-lowering effects. A 0.2% GAT229 solution or 10 mg/kg of GAT229 alone significantly reduces IOP. GAT229 is promising for research related to glaucoma and elevated intraocular pressure[1].

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[1] Cairns EA, et al. The In Vivo Effects of the CB1-Positive Allosteric Modulator GAT229 on Intraocular Pressure in Ocular Normotensive and Hypertensive Mice. J Ocul Pharmacol Ther. 2017 Oct;33(8):582-590. DOI:10.1089/jop.2017.0037