GSK189254A | H3R antagonist | Probechem Biochemicals

Chemical Structure : GSK189254A

CAS No.: 720690-73-3

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GSK189254A (GSK189254 free base)

货号: PC-27476Not For Human Use, Lab Use Only.

GSK189254A (GSK189254 free base) is a potent, selective histamine H3 receptor (H3R) antagonist with pKi of 9.59 -9.90 and 8.51-9.17 for human and rat H3R respectively.

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5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

GSK189254A (GSK189254 free base) is a potent, selective histamine H3 receptor (H3R) antagonist with pKi of 9.59 -9.90 and 8.51-9.17 for human and rat H3R respectively.
GSK189254A exhibits potent functional antagonism (pA(2) = 9.06 versus agonist-induced changes in cAMP) and inverse agonism [pIC(50) = 8.20 versus basal guanosine 5'-O-(3-[(35)S]thio)triphosphate binding] at the human recombinant H(3) receptor.
GSK189254 inhibits cortical ex vivo R-(-)-alpha-methyl[imidazole-2,5(n)-(3)H]histamine dihydrochloride ([(3)H]R-alpha-methylhistamine) binding (ED(50) = 0.17 mg/kg) and increases c-Fos immunoreactivity in prefrontal and somatosensory cortex (3 mg/kg).
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 (1 and 3 mg/kg p.o.), water maze (1 and 3 mg/kg p.o.), object recognition (0.3 and 1 mg/kg p.o.), and attentional set shift (1 mg/kg p.o.).

物理化学性质&存储条件

分子量	351.45
分子式	C21H25N3O2
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	6-[(3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide

参考文献

1. Giannoni P, et al. J Pharmacol Exp Ther. 2010 Jan;332(1):164-72.

2. Guo RX, et al. Br J Pharmacol. 2009 May;157(1):104-17.

3. Medhurst AD, et al. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45.

GSK189254A (GSK189254 free base)

生物&药学活性

物理化学性质&存储条件

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GSK189254A (GSK189254 free base)

生物&药学活性

物理化学性质&存储条件

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