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Merck

Z3003

Zardaverine

powder, ≥98% (HPLC)

Synonym(s):

6-(4-Difluoromethoxy-3-methoxyphenyl)-3(2H)-pyridazinone

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About This Item

Empirical Formula (Hill Notation):
C12H10F2N2O3
CAS Number:
101975-10-4
Molecular Weight:
268.22
UNSPSC Code:
12352202
PubChem Substance ID:
24278784
NACRES:
NA.77
MDL number:
MFCD00867059

Key Documents

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Product Name

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

200

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Certificates of Analysis (COA)

Lot/Batch Number
SLCR4833
SLCD6156
SLCC9883
SLCC0064
SLBZ8251

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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
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
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)
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