BAY-60-7550是有效的PDE2抑制剂，IC | 50 |值为2.0 nM（牛）和4.7 nM（人）。对PDE2的选择性是PDE1的50倍，对PDE5的选择性是PDE3B，PDE4B，PDE7B，PDE8A，PDE9A，PDE10A和PDE11A的100倍以上。以3 mg / kg的剂量，BAY-60-7550可通过增加cGMP信号传导拮抗小鼠氧化应激诱导的焦虑样行为。BAY-60-7550的剂量为1 mg / kg时，可提高大鼠在对象定位任务中的性能，从而增强cAMP / cGMP介导的对象和空间 BAY-60-7550 is a potent PDE2 inhibitor with IC|50|values of 2.0 nM (bovine) and 4.7 nM (human). It is 50-fold more selective for PDE2 compared to PDE1 and greater than 100-fold selective compared to PDE5 PDE3B, PDE4B, PDE7B, PDE8A, PDE9A, PDE10A, and PDE11A. At 3 mg/kg BAY-60-7550 antagonizes oxidative stress-induced anxiety-like behavioral effects in mice by increasing cGMP signaling. At 1 mg/kg BAY-60-7550 improves the performance of rats in an object location task, enhancing cAMP/cGMP-mediated object and spatial memory consolidation. cAMP and cGMP are important mediators of signal transduction and hence a wide range of cellular processes including synaptic plasticity and vasodilation. Type 2 cyclic nucleotide phosphodiesterases (PDE2) isoforms inactivate cAMP and cGMP by hydrolyzing the phosphodiester bond.
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BAY-60-7550
CAS number：439083-90-6 molecular formula：C27H32N4O4
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| Chinese alias | 2-(3,4-二甲氧基苄基)-7-{1-[(1-羟乙基]-4-苯基丁基} -5-甲基咪唑并三嗪酮 | ||
| English alias | SCHEMBL19205847 | 2-(3,4-Dimethoxy-benzyl)-7-[(R)-1-((R)-1-hydroxy-ethyl)-4-phenyl-butyl]-5-methyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one | HMS2089F14 | BDBM50166893 | SCHEMBL18380627 | BAY-607550 | BAY-60-7550 | Bay60-7550 | UNII-ZRN7LZK9TQ | 2-(3,4-dimet | ||
| CAS number | 439083-90-6 | molecular formula | C27H32N4O4 |
| molecular weight | 476.57 g/mol | Exact mass | - |
| PSA | 98.000 Ų | logp | 4.200 |
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