Z3003
Zardaverine
powder, ≥98% (HPLC)
别名:
6-(4-Difluoromethoxy-3-methoxyphenyl)-3(2H)-pyridazinone
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关于此项目
经验公式（希尔记法）:
C12H10F2N2O3
化学文摘社编号:
分子量:
268.22
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
Zardaverine,
SMILES string
COc1cc(ccc1OC(F)F)C2=NNC(=O)C=C2
InChI key
HJMQDJPMQIHLPB-UHFFFAOYSA-N
InChI
1S/C12H10F2N2O3/c1-18-10-6-7(2-4-9(10)19-12(13)14)8-3-5-11(17)16-15-8/h2-6,12H,1H3,(H,16,17)
Quality Level
Gene Information
human ... PDE3A(5139), PDE3B(5140), PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144), PDE5A(8654), PDE7A(5150)
rat ... Pde2a(81743), Pde4a(25638)
Application
Zardaverine has been used as a phosphodiesterase inhibitor:
- to study its effects on human colonic epithelial cells
- to study its effects on junctional proteins in Sertoli cells
- to study its effects on phosphodiesterase 3 A (PDE3A) expression in various tumor cells
Biochem/physiol Actions
Selective inhibitor of phosphodiesterase III/IV (PDE3/4).
Zardaverine is a derivative of pyridazinone. It shows anti-tumor and anti-proliferative activity in varied cell lines. Zardaverine possesses broncho-dilatory activity and exhibits therapeutic effects against asthma.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
W Fischer et al.
Biochemical pharmacology, 45(12), 2399-2404 (1993-06-22)
Phosphodiesterase inhibitors were used as a tool to manipulate cellular nucleotide levels in vitro and in vivo. The lipopolysaccharide (LPS)-induced release of tumor necrosis factor alpha (TNF-alpha) from mouse peritoneal macrophages was inhibited by prostaglandin E2 with an IC50 of
D T Schmidt et al.
British journal of pharmacology, 131(8), 1607-1618 (2001-01-05)
Non-selective inhibitors of cyclic nucleotide phosphodiesterase (PDE) block allergen-induced contraction of passively sensitized human airways in vitro by a dual mechanism involving a direct relaxant effect on smooth muscle and inhibition of histamine and cysteinyl leukotriene (LT) release from airways.
K F Rabe et al.
The American journal of physiology, 266(5 Pt 1), L536-L543 (1994-05-01)
The effects of the nonselective phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine (IBMX) and the selective PDE inhibitors motapizone (type III), rolipram (type IV), zardaverine (type III/IV), and zaprinast (type V and I) on prostaglandin F2 alpha (PFG2 alpha)-induced tone in human pulmonary
A Hatzelmann et al.
British journal of pharmacology, 114(4), 821-831 (1995-02-01)
1. The effect of non-selective (3-isobutyl-1-methylxanthine, IBMX; theophylline) and type IV- or type III/IV-selective (rolipram, RP 73401; zardaverine, tolafentrine) phosphodiesterase (PDE) inhibitors on human eosinophil functions was investigated. 2. For this purpose human eosinophils were purified from blood of healthy
R T Schermuly et al.
American journal of respiratory and critical care medicine, 160(5 Pt 1), 1500-1506 (1999-11-11)
Inhalation of aerosolized prostaglandin I(2) (PGI(2)) causes selective pulmonary vasodilation, but the effect rapidly levels off after termination of nebulization. In experimental pulmonary hypertension in intact rabbits, provoked by continuous infusion of the stable thromboxane mimetic U46619, the impact of
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