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=CC=CC=C1CCCCCCCCC2=CC=CC=C2)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 |
---|---|---|
Cysteinyl leukotrienes induce P-selectin expression in human endothelial cells via a non-CysLT1 receptor-mediated mechanism. | 1997 May |
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Identification and characterization of two cysteinyl-leukotriene high affinity binding sites with receptor characteristics in human lung parenchyma. | 1998 Apr |
|
Pharmacology of leukotriene receptor antagonists. | 1998 Jun |
|
Inhibition of 5-lipoxygenase diminishes neurally evoked tachykinergic contraction of guinea pig isolated airway. | 1998 May |
|
Leukotriene C4 is a tight-binding inhibitor of microsomal glutathione transferase-1. Effects of leukotriene pathway modifiers. | 1999 Jan 22 |
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:43:29 GMT 2025
by
admin
on
Mon Mar 31 21:43:29 GMT 2025
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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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C0U5450C51
Created by
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60841
Created by
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385390-37-4
Created by
admin on Mon Mar 31 21:43:29 GMT 2025 , Edited by admin on Mon Mar 31 21:43:29 GMT 2025
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300000055008
Created by
admin on Mon Mar 31 21:43:29 GMT 2025 , Edited by admin on Mon Mar 31 21:43:29 GMT 2025
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SOLVATE->ANHYDROUS | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |