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Details

Stereochemistry ACHIRAL
Molecular Formula C13H12N2O2
Molecular Weight 228.2466
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of OZAGREL

SMILES

OC(=O)\C=C\C1=CC=C(CN2C=CN=C2)C=C1

InChI

InChIKey=SHZKQBHERIJWAO-AATRIKPKSA-N
InChI=1S/C13H12N2O2/c16-13(17)6-5-11-1-3-12(4-2-11)9-15-8-7-14-10-15/h1-8,10H,9H2,(H,16,17)/b6-5+

HIDE SMILES / InChI
Molecular Formula C13H12N2O2
Molecular Weight 228.2466
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description

Ozagrel is a thromboxane A2 synthesis inhibitor used for the treatment of cerebral vasospasm and asthma due to its antiplatelet and anti-inflammation properties.

CNS Activity

Originator

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Thromboxane-A synthase
21
Target ID: P24557|||Q8IUN1|||Q9HD82
Gene ID: 6916.0
Gene Symbol: TBXAS1
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 11.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8583
DOMENAN

Approved Use

Unknown
Primary
Approved
8583
XANBON

Approved Use

Cerebral vasospasm and ischaemia following surgical management of subarachnoid haemorrhage.
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
97 ng/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25
1 μg/kg/min single, intravenous
dose: 1 μg/kg/min
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1657.3 ng/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25
15 μg/kg/min single, intravenous
dose: 15 μg/kg/min
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
576.5 ng/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=26
5 mg single, intravenous
dose: 5 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1928.8 ng/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2020 ng/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1940 ng/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
281 ng × h/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25
1 μg/kg/min single, intravenous
dose: 1 μg/kg/min
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4659.2 ng × h/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25
15 μg/kg/min single, intravenous
dose: 15 μg/kg/min
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
197.4 ng × h/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=26
5 mg single, intravenous
dose: 5 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3913.2 ng × h/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3360 ng × h/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3500 ng × h/mL
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.79 h
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25
1 μg/kg/min single, intravenous
dose: 1 μg/kg/min
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.66 h
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25
15 μg/kg/min single, intravenous
dose: 15 μg/kg/min
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.09 h
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=26
5 mg single, intravenous
dose: 5 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.45 h
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.74 h
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.76 h
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OZAGREL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
46%
OTHER GOV'T
https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19
OZAGREL serum
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
800 mg 1 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9792572/
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/9792572/
Sources:
https://pubmed.ncbi.nlm.nih.gov/9792572/
PubMed

PubMed

TitleDatePubMed
Thromboxane synthase mutations in an increased bone density disorder (Ghosal syndrome).
2008-03
Effect of sodium ozagrel on the activity of rat CYP2D6.
2007-11-14
Heparin-protamine complexes cause pulmonary hypertension in goats.
1995-10
Thromboxane A2 and development of genetic hypertension in the Lyon rat strain.
1990-12
Patents

Patents

20050009896
4
CN102429903 A
4
CN102626388 B
4
CN102633723 A
4
JPS57131769A
4
US20090247600 A1
4

Sample Use Guides

In Vivo Use Guide
1 tablet (200 mg of the active ingredient) at a time, twice a day after breakfast and before bedtime (for asthma). Intravenous infusion of 80mg, twice a day, solute in 500ml normal saline or 5% glucose solution (cerebral vasospasm).
Route of Administration: Other
In Vitro Use Guide
The influence of ozagrel on platelets aggregation was investigated. Platelet aggregation which was induced by ADP (5 uM) was inhibited by ozagrel. This inhibition was dependent on the concentration of the drug and was significant at 10(−6)–10(−3) M.
Substance Class Chemical
Created
by admin
on Wed Apr 02 09:19:44 GMT 2025
Edited
by admin
on Wed Apr 02 09:19:44 GMT 2025
Record UNII
L256JB984D
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
OZAGREL
INN   MART.   MI   WHO-DD  
INN  
Official Name English
KCT-0809
Preferred Name English
(E)-P-(IMIDAZOL-1-YLMETHYL)CINNAMIC ACID
Common Name English
OZAGREL [MI]
Common Name English
Ozagrel [WHO-DD]
Common Name English
ozagrel [INN]
Common Name English
OZAGREL [MART.]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C471
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
NCI_THESAURUS C1327
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
Code System Code Type Description
FDA UNII
L256JB984D
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
SMS_ID
100000082757
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
INN
5918
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
ChEMBL
CHEMBL11662
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
CAS
82571-53-7
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
EPA CompTox
DTXSID6048547
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
PUBCHEM
5282440
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
MESH
C034364
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
WIKIPEDIA
Ozagrel
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
DRUG CENTRAL
2043
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
MERCK INDEX
m8349
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY Merck Index
EVMPD
SUB09581MIG
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
DRUG BANK
DB12017
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
NCI_THESAURUS
C66288
Created by admin on Wed Apr 02 09:19:44 GMT 2025 , Edited by admin on Wed Apr 02 09:19:44 GMT 2025
PRIMARY
Related Record Type Details
THROMBOXANE-A SYNTHASE
TARGET -> INHIBITOR
IC50
Structure of OZAGREL HYDROCHLORIDE MONOHYDRATE
SALT/SOLVATE -> PARENT
Structure of OZAGREL HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of OZAGREL
ACTIVE MOIETY
NIH
NCATS
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