| Identification | Back Directory | [Name]
GSK 189254 | [CAS]
945493-87-8 | [Synonyms]
GSK 189254
[3H]-GSK189254
GSK 189254 HCl
GSK 189254 hydrochloride
6-[(3-cyclobutyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)oxy]-N-methylpyridine-3-carboxamide:hydrochloride
6-[(3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride | [Molecular Formula]
C21H26ClN3O2 | [MDL Number]
MFCD16987635 | [MOL File]
945493-87-8.mol | [Molecular Weight]
387.903 |
| Hazard Information | Back Directory | [Uses]
GSK189254A hydrochloride is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively[1]. | [in vivo]
GSK189254A hydrochloride (0.3-3 mg/kg p.o.) increases the release of acetylcholine, noradrenaline, and dopamine in the anterior cingulate cortex and acetylcholine in the dorsal hippocampus. GSK189254A hydrochloride significantly improves performance of rats in diverse cognition paradigms, including passive avoidance, water maze, object recognition, and attentional set shift[1]. In Ox+/+ and Ox?/? mice, acute administration of GSK189254A hydrochloride increases W and decreases slow wave and paradoxical sleep to a similar degree to modafinil, while it reduces narcoleptic episodes in Ox?/? mice[2]. | [References]
[1] Medhurst AD, et al. GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. DOI:10.1124/jpet.107.120311
[2] Guo RX, et al. Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.Br J Pharmacol. 2009 May;157(1):104-17. DOI:10.1111/j.1476-5381.2009.00205.x |
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