Tags: Drug.
GSK-189254 is a potent and selective H3-receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki 0.2nM) and selectivity of over 10000x for H3 over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord.
