Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H8N6O |
Molecular Weight | 228.2101 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=CN2C(=O)C(=CN=C12)C3=NN=NN3
InChI
InChIKey=HIANJWSAHKJQTH-UHFFFAOYSA-N
InChI=1S/C10H8N6O/c1-6-3-2-4-16-9(6)11-5-7(10(16)17)8-12-14-15-13-8/h2-5H,1H3,(H,12,13,14,15)
Molecular Formula | C10H8N6O |
Molecular Weight | 228.2101 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Pemirolast is a mast cell stabilizer that acts as an antiallergic agent, it is approved in Japan for the treatment of bronchial asthma and of allergic rhinitis. Pemirolast strongly inhibits extracellular Ca2+ influx and the release of intracellular Ca2+, an important factor in the release of chemical mediators, by inhibiting inositol-phospholipid metabolism in mast cells. It also inhibits the release of arachidonic acid. Furthermore contribution of increasing effect on c-AMP based on inhibiting phosphodiesterase is suggested. Main pharmacological effects is an inhibition of release of chemical mediators, e.g. histamine, LTB4, LTC4, LTD4, PGD2, TXB2 and PAF from human lung tissues, abraded fragments of the nasal mucosa, and peripheral leukocytes, rat peritoneal exudate cells, and rat and guniea pig lung tissues.
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.283 μg/mL |
0.2 mg/kg single, oral dose: 0.2 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
PEMIROLAST plasma | Canis lupus population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
|
4.7 ng/mL |
2 drop 4 times / day steady-state, ocular dose: 2 drop route of administration: Ocular experiment type: STEADY-STATE co-administered: |
PEMIROLAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.315 μg × h/mL |
0.2 mg/kg single, oral dose: 0.2 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
PEMIROLAST plasma | Canis lupus population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.5 h |
2 drop 4 times / day steady-state, ocular dose: 2 drop route of administration: Ocular experiment type: STEADY-STATE co-administered: |
PEMIROLAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
34% |
0.2 mg/kg single, oral dose: 0.2 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
PEMIROLAST plasma | Canis lupus population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
0.1 % 2 times / day steady, ophthalmic Recommended Dose: 0.1 %, 2 times / day Route: ophthalmic Route: steady Dose: 0.1 %, 2 times / day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: allergic conjunctivitis Age Group: adult Sex: M+F Population Size: 39 Sources: |
Disc. AE: Eye allergy... AEs leading to discontinuation/dose reduction: Eye allergy (1 patient) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Eye allergy | 1 patient Disc. AE |
0.1 % 2 times / day steady, ophthalmic Recommended Dose: 0.1 %, 2 times / day Route: ophthalmic Route: steady Dose: 0.1 %, 2 times / day Sources: |
unhealthy, adult n = 39 Health Status: unhealthy Condition: allergic conjunctivitis Age Group: adult Sex: M+F Population Size: 39 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/16498570/ Page: 7.0 |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Effects of topical anti-inflammatory and antiallergic eyedrops on prostaglandin E2-induced aqueous flare elevation in pigmented rabbits. | 2002 Jul |
|
Comparison of 0.1% bromfenac sodium and 0.1% pemirolast potassium for the treatment of allergic conjunctivitis. | 2004 Nov-Dec |
|
Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
|
Increasing effect by simultaneous use of levocabastine and pemirolast on experimental allergic conjunctivitis in rats. | 2005 Mar |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT03119714
reatment with pemirolast 200 mg bid for 14-16 days
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8130655
It was investigated the effect of pemirolast on the release of leukotriene C4 (LTC4) and eosinophil cationic protein (ECP) from human eosinophils. Pemirolast (10(-6) to 10(-3) M) inhibited A23187-induced LTC4 release from the eosinophils in a dose-dependent fashion with 77% inhibition at 10(-3) M. Pemirolast (10(-5) to 10(-3) M) inhibited A23187-induced ECP release from the eosinophils in a dose-dependent fashion with 42% inhibition at 10(-3) M. Pemirolast (10(-4) and 10(-3) M) also inhibited PAF-induced and FMLP-induced ECP release from the eosinophils. It was concluded that pemirolast prevented the activation of human eosinophils to inhibit LTC4 and ECP release.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 16:42:31 UTC 2023
by
admin
on
Sat Dec 16 16:42:31 UTC 2023
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Record UNII |
2C09NV773M
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Record Status |
Validated (UNII)
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Record Version |
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-
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000175630
Created by
admin on Sat Dec 16 16:42:31 UTC 2023 , Edited by admin on Sat Dec 16 16:42:31 UTC 2023
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NDF-RT |
N0000175628
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admin on Sat Dec 16 16:42:31 UTC 2023 , Edited by admin on Sat Dec 16 16:42:31 UTC 2023
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NCI_THESAURUS |
C29714
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admin on Sat Dec 16 16:42:31 UTC 2023 , Edited by admin on Sat Dec 16 16:42:31 UTC 2023
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Code System | Code | Type | Description | ||
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19551
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C055139
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DB00885
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SUB09656MIG
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69372-19-6
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PEMIROLAST
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100000082476
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57697
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6449
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Pemirolast
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2C09NV773M
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m8457
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7329
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7291
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DTXSID1048338
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C66334
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2074
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CHEMBL1201198
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