GSK 189254A Chemical Properties

Boiling point:

545.0±50.0 °C(Predicted)

Density 

1.195±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:25.0(Max Conc. mg/mL);71.13(Max Conc. mM)

form 

A solid

pka

14.26±0.46(Predicted)

color 

White to off-white

GSK 189254A Usage And Synthesis

Description

GSK189254A is a histamine H3 receptor antagonist for the treatment of narcolepsy.It may also be useful for the treatment of dementia and neuropathic pain. Its pharmacological effect may be related to its effect on increasing the release neurotransmitter in the brain. Microdialysis studies demonstrated that GSK189254 increased the release of acetylcholine, noradrenaline, and dopamine in the anterior cingulate cortex and acetylcholine in the dorsal hippocampus. GSK189254 significantly improved performance of rats in diverse cognition paradigms, including passive avoidance, water maze, object recognition, and attentional set shift. These data suggest that GSK189254 may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer's disease and other cognitive disorders.

References

Medhurst, Andrew D., and A. I. J. Beresford. "GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models." Alzheimers & Dementia 321.3(2007):1032.
Plisson, Christophe, et al. "PET imaging of the CNS histamine H3 receptor using [11C] GSK189254A." Neuroimage 31.1(2006):T47-T47.
http://medkoo.com/products/10117

Uses

GSK189254A (GSK189254 free base) 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.

in vivo

IC 50

H₃ receptor

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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