GSK189254

GSK189254 is a potent and highly selective histamine H3 receptor antagonist and inverse agonist developed by GSK. It exhibits subnanomolar affinity for the human H3 receptor (pKi = 9.59–9.90) and over 10,000-fold selectivity versus other histamine receptor subtypes[2][5]. In preclinical models, it increases the release of acetylcholine, noradrenaline (norepinephrine), and dopamine in key brain regions such as the anterior cingulate cortex and dorsal hippocampus[2]. Animal studies have demonstrated stimulant, nootropic (cognitive-enhancing), and analgesic effects[5]. The drug has been investigated for symptomatic treatment of dementia in Alzheimer's disease and other cognitive disorders as well as narcolepsy and neuropathic pain[2][4][5].

Other names

6-[(3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochlorideGSK189254AGSK-189254AGSK 189254AGSK189254 free baseGSK-189254 free baseGSK 189254 free base