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Home   »   Product Pathways  »  Histamine Receptor  »  GSK189254A

Products are for research use only. Not for human use. We do not sell to patients.

CS-6206 GSK189254A

(GSK-189254A;GSK 189254A)
Structure Price and Availability of    GSK189254A
United States
Size Price Stock
1mg $150 In-stock Inquiry
5mg $350 In-stock
10mg $500 In-stock
50mg $1500 In-stock
100mg $2100 In-stock
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 Distributor In Japan:  フナコシ株式会社    電話番号:81-3-5684-1620   
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GSK189254A  M.Wt:  351.44
GSK189254A  Formula: C21H25N3O2
GSK189254A  Solubility: ≤6 mg/mL in DMSO
GSK189254A  Purity: >98%
GSK189254A  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 720690-73-3

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GSK189254A (GSK189254) 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. pKi&Target: 9.59-9.90 (H3, human), 8.51-9.17 (H3, rat)[1] InVitro: GSK189254 has high affinity for both recombinant H3 receptors expressed in HEK-293-MSR-II cells and native H3 receptors expressed in the cerebral cortex of several species. GSK189254 generally exhibits higher affinity for human and pig H3 receptors compared with rat,mouse, and dog H3 receptors. [3H]GSK189254 binds in rat and human brain areas, including cortex and hippocampus. GSK189254 may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer’s disease and other cognitive disorders [1]. InVivo: GSK189254 (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. GSK189254 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 GSK189254 increases W and decreases slow wave and paradoxical sleep to a similar degree to modafinil, while it reduces narcoleptic episodes in Ox-/-mice[2].

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