GSK207040 | H3R antagonist | Probechem Biochemicals

Chemical Structure : GSK207040

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GSK207040 (GSK-207040)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	352.44
分子式	C20H24N4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-2-pyrazinecarboxamide

参考文献

1. Medhurst AD, et al. Biochem Pharmacol. 2007 Apr 15;73(8):1182-94.

GSK207040 (GSK-207040)

生物&药学活性

物理化学性质&存储条件

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GSK207040 (GSK-207040)

生物&药学活性

物理化学性质&存储条件

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