| 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 |
MOL RATIO
1 MOL RATIO (average) |
| 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.
CNS Activity
Approval Year
Doses
AEs
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as victim
Tox targets
Sourcing
PubMed
Sample Use Guides
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.
