Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C26H34O5S.C2H8N2 |
Molecular Weight | 518.708 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NCCN.O[C@H]([C@H](SCCC(O)=O)C1=C(CCCCCCCCC2=CC=CC=C2)C=CC=C1)C(O)=O
InChI
InChIKey=GWUGCYFQFVTHBT-JIMLSGQQSA-N
InChI=1S/C26H34O5S.C2H8N2/c27-23(28)18-19-32-25(24(29)26(30)31)22-17-11-10-16-21(22)15-9-4-2-1-3-6-12-20-13-7-5-8-14-20;3-1-2-4/h5,7-8,10-11,13-14,16-17,24-25,29H,1-4,6,9,12,15,18-19H2,(H,27,28)(H,30,31);1-4H2/t24-,25-;/m1./s1
Molecular Formula | C2H8N2 |
Molecular Weight | 60.0983 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C26H34O5S |
Molecular Weight | 458.61 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Pobilukast is the Leukotriene D4 receptor antagonist. Pobilukast significantly attenuated the Salmonella enteritidis endotoxin-induced thrombocytopenia but had no effect on either the endotoxin-induced early leukopenia or late leukocytosis. Additionally, Pobilukast significantly reduced the endotoxin-induced hemoconcentration and improved survival to 30% at 48 hr. Pobilukast dose-dependently inhibited the immediate hemodynamic changes after leukotriene D4 (LTD4) injections. Pobilukast also attenuated the increase in vascular permeability and the prolonged decrease in CO, suggesting that the observed cardiac and vascular effects of LTs were mediated by stimulation of LT receptors. A shift toward the right of the dose-response curves to histamine with pobilukast compared to that with placebo in three subjects was demonstrated, whereas the active compound did not exhibit any protective effect against histamine in the remaining nine subjects. It was concluded that there is a leukotriene component to the bronchial responses to histamine in some, but not all, subjects. Pobilukast had been in phase II clinical trial for the treatment of asthma. However, this development was discontinued.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Identification and characterization of two cysteinyl-leukotriene high affinity binding sites with receptor characteristics in human lung parenchyma. | 1998 Apr |
|
Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. | 1999 Sep |
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 07:46:45 GMT 2023
by
admin
on
Sat Dec 16 07:46:45 GMT 2023
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Record UNII |
C0U5450C51
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Record Status |
Validated (UNII)
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Record Version |
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-
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C0U5450C51
Created by
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60841
Created by
admin on Sat Dec 16 07:46:45 GMT 2023 , Edited by admin on Sat Dec 16 07:46:45 GMT 2023
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385390-37-4
Created by
admin on Sat Dec 16 07:46:45 GMT 2023 , Edited by admin on Sat Dec 16 07:46:45 GMT 2023
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Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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PARENT -> SALT/SOLVATE |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |