i2r

CR4056 (6-(1H-imidazol-1-yl)-2-phenylquinazoline) is a selective inhibitor of MAO-A with IC50 of 202.7 nM and a ligand of I2-imidazoline receptor with IC50 of 596 nM.

RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].

RX 801077 (2 BFI free base), a selective imidazoline I2 receptor (I2R) agonist with a K_i value of 70.1 nM, demonstrates anti-inflammatory and neuroprotective properties, making it a potential research candidate for traumatic brain injury (TBI).