GSK189254A

GSK189254A (GSK189254)是一个新颖高效有选择性的H3受体拮抗剂，对人类和大鼠H3的pK_i值分别为9.59-9.90 and 8.51-9.17。GSK189254 has high affinity for both recombinant H3 receptors expressed in HEK-293-MSR-II cells and native H3 receptors expressed in the cerebral cortex of several species. GSK189254 generally exhibits higher affinity for human and pig H3 receptors compared with rat,mouse, and dog H3 receptors. [³H]GSK189254 binds in rat and human brain areas, including cortex and hippocampus. GSK189254 may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer’s disease and other cognitive disorders