GSK-189254
Template:Short description Template:Drugbox
GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes.[1] Animal studies have shown it to possess not only stimulant and nootropic effects,[2] but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord.[3] GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia,[4] as well as possible use in the treatment of conditions such as narcolepsy,[5] or neuropathic pain which do not respond well to conventional analgesic drugs.[6]
References
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