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Details

Stereochemistry ACHIRAL
Molecular Formula C22H31N3O5
Molecular Weight 417.4986
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of CINEPAZIDE

SMILES

COC1=CC(=CC(OC)=C1OC)\C=C\C(=O)N2CCN(CC(=O)N3CCCC3)CC2

InChI

InChIKey=RCUDFXMNPQNBDU-VOTSOKGWSA-N
InChI=1S/C22H31N3O5/c1-28-18-14-17(15-19(29-2)22(18)30-3)6-7-20(26)25-12-10-23(11-13-25)16-21(27)24-8-4-5-9-24/h6-7,14-15H,4-5,8-13,16H2,1-3H3/b7-6+

HIDE SMILES / InChI

Molecular Formula C22H31N3O5
Molecular Weight 417.4986
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description

Cinepazide or cinepazide maleate (Kelinao or Anjieli in China) is a vasodilator used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases. As a calcium channel blocker, cinepazide can stop calcium from entering vascular smooth muscle cells and relax smooth muscles of cerebral vessels, coronary arteries and peripheral vessels so as to relieve vasospasm, reduce vascular resistance, improve flexibility of red blood cells, increase blood circulation in cerebral vessels and improve microcirculation and brain metabolism. Cinepazide could also increase the number of cAMP by inhibiting cAMP phosphodiesterase and reduce oxygen consumption. In April 2002, cinepazide of Beijing Hwellso Pharmaceutical Co., Ltd was approved to enter the market with two dosage forms of oral formulation and injection under the trade name of Kelinao. Currently, Kelinao is the only domestic brand for the treatment of cardiovascular diseases. And in 2009, cinepazide was included in the national medicare drug list. Cinepazide maleate, after wide application, has gained the recognition of Chinese doctors and patients for the treatment of cerebral arteriosclerosis, transient ischemic attack, cerebral thrombosis, cerebral embolism, cerebral hemorrhage sequel and post-traumatic brain syndrome. Besides, due to its efficacy in cardiovascular diseases and peripheral vascular diseases, cinepazide maleate has become a leading product in cerebrovascular drug market.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
3.7 μg/mL
200 mg single, oral
CINEPAZIDE plasma
Homo sapiens
3.7 μg/mL
400 mg single, oral
CINEPAZIDE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
1.07 h
200 mg single, oral
CINEPAZIDE plasma
Homo sapiens
1.64 h
400 mg single, oral
CINEPAZIDE plasma
Homo sapiens

Doses

AEs

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
2ml:80mg/Ampoule
Route of Administration: Intravenous
In Vitro Use Guide
cinepazide in concentrations ranging from 10(-6) to 10(-5) M selectively potentiates the relaxing response mediated through purinergic P1-receptors.
Substance Class Chemical
Record UNII
67Y4P5C84X
Record Status Validated (UNII)
Record Version