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形式
solid
质量水平
颜色
white
溶解性
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.11 mg/mL
DMSO: 10 mg/mL
H2O: insoluble
SMILES字符串
CCCOc1ccccc1C2=NC(=O)c3nn[nH]c3N2
InChI
1S/C13H13N5O2/c1-2-7-20-9-6-4-3-5-8(9)11-14-12-10(13(19)15-11)16-18-17-12/h3-6H,2,7H2,1H3,(H2,14,15,16,17,18,19)
InChI key
REZGGXNDEMKIQB-UHFFFAOYSA-N
基因信息
human ... PDE2A(5138) , PDE4A(5141) , PDE4B(5142) , PDE4D(5144)
应用
扎普司特已被用于通过生发泡破裂(GVBD)检测测定其对卵母细胞减数分裂的影响,并用于通过免疫组织化学测试其对视网膜细胞的抑制作用。
生化/生理作用
扎普司特对磷酸二酯酶10和11(PDE10和PDE11)没有实质性的抑制作用。它还具有血管舒张作用。
cGMP 特异性磷酸二酯酶 V 和 VI (PDE5/6) 选择性抑制剂和 G 蛋白偶联受体 35 (GPR35) 激动剂。
警示用语:
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
Resumption of meiosis induced by meiosis-activating sterol has a different signal transduction pathway than spontaneous resumption of meiosis in denuded mouse oocytes cultured in vitro
Biology of Reproduction, 65(6), 1751-1758 (2001)
Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35
Febs Letters, 580(21), 5003-5008 (2006)
Cell death & disease, 4, e488-e488 (2013-02-09)
For most neurodegenerative diseases the precise duration of an individual cell's death is unknown, which is an obstacle when counteractive measures are being considered. To address this, we used the rd1 mouse model for retinal neurodegeneration, characterized by phosphodiesterase-6 (PDE6)
The Journal of neuroscience : the official journal of the Society for Neuroscience, 19(7), 2489-2499 (1999-03-23)
High-frequency stimulation (HFS) of corticostriatal glutamatergic fibers induces long-term depression (LTD) of excitatory synaptic potentials recorded from striatal spiny neurons. This form of LTD can be mimicked by zaprinast, a selective inhibitor of cGMP phosphodiesterases (PDEs). Biochemical analysis shows that
Selective pulmonary vasodilation induced by aerosolized zaprinast
Anesthesiology, 88(2), 410-416 (1998)
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