Z3003
Zardaverine
powder, ≥98% (HPLC)
別名:
6-(4-Difluoromethoxy-3-methoxyphenyl)-3(2H)-pyridazinone
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この商品について
実験式（ヒル表記法）:
C12H10F2N2O3
CAS番号:
分子量:
268.22
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
MDL number:
製品名
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.
保管分類
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
K F Rabe et al.
The American journal of physiology, 264(5 Pt 1), L458-L464 (1993-05-01)
The effects of the nonselective phosphodiesterase (PDE)-inhibitor 3-isobutyl-1-methylxanthine (IBMX) and the selective PDE inhibitors SKF 94120 (type III), rolipram (type IV), zardaverine (type III/IV), and zaprinast (type V) on inherent tone in human airways were investigated. Substantial relaxation was achieved
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
T Brunnée et al.
The European respiratory journal, 5(8), 982-985 (1992-09-01)
Zardaverine is a newly developed selective phosphodiesterase III and IV inhibitor. This study investigates the bronchodilatory properties of zardaverine, administered by inhalation. Twelve patients with reversible bronchial obstruction (increase in forced expiratory volume in one second (change FEV1 % predicted)
Bronchodilator and positive inotropic activity of pyridazine compound Zardaverine as a phosphodiesterase isozymes inhibitor
Asif M
Journal of Chemical and Pharmaceutical Sciences
, 3(1), 31-34 null
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