5-メチル-7-[(R)-1-[(R)-1-ヒドロキシエチル]-4-フェニルブチル]-2-(3,4-ジメトキシベンジル)イミダゾ[5,1-f][1,2,4]トリアジン-4(3H)-オン 化学特性,用途語,生産方法
説明
The second messengers cAMP and cGMP are important mediators of signal transduction and hence a wide range of cellular processes including vasodilation and synaptic plasticity. Type 2 cyclic nucleotide phosphodiesterases (PDE2) isoforms inactivate cAMP and cGMP by hydrolyzing the phosphodiester bond. 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.
使用
The compound induced anxiety by inhibition of Phosphodiesterase-2 (PDE2), which regulates cGMP and cAMP signaling
Biochem/physiol Actions
BAY 60-7550 is an orally active, potent and selective cGMP-dependent phosphodiesterase PDE2 (PDE2A) inhibitor (human/bovine PDE2 IC50 = 4.7/2.0 nM; bovine PDE1 IC50 = 108 nM, human PDE5/5A/10A/4B IC50 = 240/580/704/940/1830 nM, human PDE3B/7B/8A/9A/11A IC50 >4 μM) with little activity (IC50 >10 μM) toward acetylcholinesterase, mAO-A/B, adenosine deaminase, and many receptor subtypes tested. Bay 60-7550 effectively upregulates cGMP and cAMP level in cultured rat and murine neurons (1 nM-1 μM) exposed to guanylyl cyclase (GC) or adenylyl cyclase (AC) stimulator (1 μM Bay 41-8543 or 2 μM forskolin), respectively, as well as exhibits learning and memory-improving efficacy in rats (0.6-3 mg/kg p.o.) and mice (0.3-1 mg/kg p.o.) in vivo.
5-メチル-7-[(R)-1-[(R)-1-ヒドロキシエチル]-4-フェニルブチル]-2-(3,4-ジメトキシベンジル)イミダゾ[5,1-f][1,2,4]トリアジン-4(3H)-オン 上流と下流の製品情報
原材料
準備製品