SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 reduced the binding of guanosine 5' -3-o -(sulfur) triphosphate to the membrane containing hCB, inhibited BaF3/CB2 cell migration, inhibited leukocyte migration in mouse delayed hypersensitivity models, and inhibited antigen-induced pulmonary eosinophilia in mouse allergy models.

CB1 (human):200nM(EC50), CB2 (BaF3 cells):34nM, CB2 (human):2nM(EC50)

SCH 336（亦称Sch.336）对Sf9细胞膜上的人CB2受体与[3H]CP55,940的竞争性结合表现出Ki值为1.8 nM的高亲和力。该化合物能够降低含有人CB2受体的膜上GTPγS的结合，EC50值为2 nM。然而，其在含CB1受体的膜上的效力降低，EC50值达到200 nM [1]。此外，SCH 336还能抑制BaF3/CB2细胞向100 nM 2-AG移动，IC50值为34 nM [1]。

在体内研究中，通过腹膜内给药(i.p.)，剂量为0.02-2.0 mg/kg时，SCH 336显著抑制白细胞迁移[1]。