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表单
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
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。
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。
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
储存分类代码
11 - Combustible Solids
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
历史批次信息供参考:
分析证书(COA)
Neuropharmacology, 60(7-8), 1227-1231 (2010-11-30)
G-protein coupled receptor 35 (GPR35) is a former "orphan receptor" expressed in brain and activated by either kynurenic acid or zaprinast. While zaprinast has been studied as a phosphodiesterase inhibitor, kynurenic acid (KYNA) is a tryptophan metabolite and has been
American journal of physiology. Endocrinology and metabolism, 302(2), E243-E253 (2011-10-27)
Testosterone (T) plays a permissive role in the development of benign prostatic hyperplasia (BPH), and phosphodiesterase 5 inhibitors (PDE5is) have been found to be effective for BPH and lower urinary tract symptoms (LUTS) in clinical trials. This study investigated the
Selective pulmonary vasodilation induced by aerosolized zaprinast
Anesthesiology, 88(2), 410-416 (1998)
Brain : a journal of neurology, 134(Pt 2), 375-387 (2010-12-25)
The aim of the present study was to evaluate the role of the nitric oxide/cyclic guanosine monophosphate pathway in corticostriatal long-term depression induction in a model of levodopa-induced dyskinesia in experimental parkinsonism. Moreover, we have also analysed the possibility of
Methods in molecular biology (Clifton, N.J.), 307, 141-154 (2005-07-01)
Of the 11 families of mammalian cyclic nucleotide phosphodiesterases (PDEs), 5 contain regulatory domains capable of binding cyclic guanosine 5'-monophosphate (cGMP). The best understood of the GAF-containing PDEs is the family of rod (PDE6R) and cone (PDE6C) photo receptor PDEs.
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