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
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+
| Molecular Formula | C22H31N3O5 |
| Molecular Weight | 417.4986 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.cphi-online.com/cinepazide-maleate-prod079010.html
http://www.technology-x.net/CN54/201210324341.html
Curator's Comment: description was created based on several sources, including
http://www.cphi-online.com/cinepazide-maleate-prod079010.html
http://www.technology-x.net/CN54/201210324341.html
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
Sources: http://pg.jrj.com.cn/acc/Res%5CHK_RES%5CSTOCK%5C2011%5C9%5C28%5C5025ec90-2ed1-473d-bc50-4bc5affe1d83.pdf
Curator's Comment: 1969
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2363032 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27990002 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.7 μg/mL |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
CINEPAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
3.7 μg/mL |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
CINEPAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.07 h |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
CINEPAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.64 h |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
CINEPAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
200 mg 3 times / day multiple, oral Studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Agranulocytosis... AEs leading to discontinuation/dose reduction: Agranulocytosis (severe, 6 patients) Sources: |
320 mg 1 times / day multiple, intravenous Studied dose Dose: 320 mg, 1 times / day Route: intravenous Route: multiple Dose: 320 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Agranulocytosis | severe, 6 patients Disc. AE |
200 mg 3 times / day multiple, oral Studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Sample Use Guides
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/6322212
cinepazide in concentrations ranging from 10(-6) to 10(-5) M selectively potentiates the relaxing response mediated through purinergic P1-receptors.
| Substance Class |
Chemical
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67Y4P5C84X
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C04AX27
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QC04AX27
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C29707
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C91001
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CHEMBL1874750
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CINEPAZIDE
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C026896
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