Chemical Structure : GSK207040
CAS No.:
720690-77-7
GSK207040
(GSK-207040)
Catalog No.: PC-27475Not For Human Use, Lab Use Only.
GSK207040 is a potent, selective histamine H3 receptor (H3R) antagonist with pKi of 9.67 and 9.08 for human and rat H3 receptors respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
GSK207040 is a potent, selective histamine H3 receptor (H3R) antagonist with pKi of 9.67 and 9.08 for human and rat H3 receptors respectively.
GSK207040 is a potent functional antagonist (pA(2)=9.26) versus H(3) agonist-induced changes in cAMP) and exhibits inverse agonist properties (pIC50=9.20 versus basal GTPgammaS binding).
GSK207040 potently inhibited cortical ex vivo [(3)H]-R-alpha-methylhistamine binding (ED(50)=0.03 mg/kg).
GSK207040 (0.1, 0.3 and 1mg/kg p.o.) significantly reversed amnesia induced by the cholinergic antagonist scopolamine in a passive avoidance paradigm.
Physicochemical Properties
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M.Wt
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352.44
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Formula
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C20H24N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-2-pyrazinecarboxamide
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References
1. Medhurst AD, et al. Biochem Pharmacol. 2007 Apr 15;73(8):1182-94.
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