Cayman Snx-2112; Purity- Greater Than Or Equal To 98%; Size- 1 Mg

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 (1 µM) enhances the binding of the CB₁ full agonist CP 55,940 to CHO cells expressing human recombinant CB₁ (hCB₁), as well as the activity of 2-arachidonoyl glycerol (2-AG; Item No. ), arachidonoyl ethanolamide (AEA; Item No. ), and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB₁. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

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