Z0878
敏喘宁
cGMP-specific phosphodiesterases V and VI inhibitor, solid
别名:
1,4-二氢-5-（2-丙氧苯基）-7H-1,2,3-三唑并 (4,5-d) 嘧啶-7-酮
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关于此项目
经验公式（希尔记法）:
C13H13N5O2
化学文摘社编号:
分子量:
271.27
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352202
EC Number:
253-655-1
MDL number:
产品名称
敏喘宁, solid
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
SMILES string
CCCOc1ccccc1C2=NC(=O)c3nn[nH]c3N2
form
solid
color
white
solubility
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.11 mg/mL, DMSO: 10 mg/mL, H2O: insoluble
Quality Level
Gene Information
human ... PDE2A(5138), PDE4A(5141), PDE4B(5142), PDE4D(5144)
Application
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。
Biochem/physiol Actions
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。
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
Selective pulmonary vasodilation induced by aerosolized zaprinast
Ichinose F, et al.
Anesthesiology, 88(2), 410-416 (1998)
Xinhua Zhang et al.
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
Barbara Picconi et al.
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
Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35
Taniguchi Y, et al.
Febs Letters, 580(21), 5003-5008 (2006)
P Calabresi et al.
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
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