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:
Form:
solid
Quality level:
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
Cristina Cosi et al.
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
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
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)
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
Faerge I, et al.
Biology of Reproduction, 65(6), 1751-1758 (2001)
A Sahaboglu et al.
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)
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