cb1r allosteric modulator 1

CB1R Allosteric modulator 1 (compound 11) 是有效的 CB1R 变构调节剂。CB1R Allosteric modulator 1 显示出对 CB1Rs 正构配体 (NAM) 功能活性的负面影响。

CB1R Allosteric modulator 5 (compound 3) 是一种具有选择性和血脑屏障通透性的大麻素受体1型 (Cannabinoid receptor type 1) 变构调节剂，其 pIC0 值为 6.89。CB1R Allosteric modulator 5 能够减弱线索引发的可卡因寻求行为复发和由可卡因诱导的行为敏化，但不改变运动活动。

CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previous studies [1].

CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1].

GAT564 (Compound 15d) is a highly effective allosteric modulator of cannabinoid 1 receptor (CB1R), having EC50 values of 87 nM and 320 nM for cAMP and β-arrestin2, respectively. It significantly enhances the binding of orthosteric ligands to hCB1R. Moreover, GAT564 exhibits remarkable efficacy as a topical agent, resulting in a significant reduction of intraocular pressure (IOP) in an ocular normotensive murine model of glaucoma [1].