GSK189254A hydrochloride
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 945493-87-8
- Formula: C21H26ClN3O2
- Molecular Weight:387.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK189254A hydrochloride
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Biological Activity
pKi: 9.59-9.90 (H3, human), 8.51-9.17 (H3, rat)[1]
GSK189254A hydrochloride 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. GSK189254A hydrochloride generally exhibits higher affinity for human and pig H3 receptors compared with rat,mouse, and dog H3 receptors. [3H] GSK189254A hydrochloride binds in rat and human brain areas, including cortex and hippocampus. GSK189254A hydrochloride may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer’s disease and other cognitive disorders [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 945493-87-8
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Molecular Weight 387.90
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Formula C21H26ClN3O2
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SMILES
O=C(NC)C(C=N1)=CC=C1OC2=CC(CC3)=C(C=C2)CCN3C4CCC4.Cl
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Synonyms
GSK189254
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
The Histamine H4 Receptor Participates in the Neuropathic Pain-Relieving Activity of the Histamine H3 Receptor Antagonist GSK189254. [Abstract]2022 Nov 18;23(22):14314. PMID: 36430790 -
J Inflamm Res
Neural-Inflammation Mechanism of Spinal Palmitic Acid Promoting Atopic Dermatitis in Mice. [Abstract]2025 Jun 17:18:7907-7919. PMID: 40546406
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK189254A hydrochloride Related Classifications
HY-12200 Related Classifications
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