Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H18BrClN4O2.ClH |
Molecular Weight | 486.19 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.ClC1=CC=C(CCCOC2=NNC(=O)C(Br)=C2NCC3=CN=CC=C3)C=C1
InChI
InChIKey=QWGUGDYWUADMGB-UHFFFAOYSA-N
InChI=1S/C19H18BrClN4O2.ClH/c20-16-17(23-12-14-3-1-9-22-11-14)19(25-24-18(16)26)27-10-2-4-13-5-7-15(21)8-6-13;/h1,3,5-9,11H,2,4,10,12H2,(H2,23,24,26);1H
Molecular Formula | C19H18BrClN4O2 |
Molecular Weight | 449.729 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.businesswire.com/news/home/20060313005348/en/Nissan-Chemical-Reports-Positive-Phase-IIb-StudyCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19616537
Sources: http://www.businesswire.com/news/home/20060313005348/en/Nissan-Chemical-Reports-Positive-Phase-IIb-Study
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19616537
NT-702 (parogrelil hydrochloride) is a novel phosphodiesterase 3 (PDE) inhibitor, and being developed for the treatment of intermittent claudication (IC) in patients with peripheral arterial disease. In Japan, Phase 2 studies are being conducted for intermittent claudication caused by arteriosclerosis obliterans, intermittent claudication caused by spinal canal stenosis, and asthma. In the USA, a Phase 2 study for intermittent claudication caused by arteriosclerosis obliterans has been successfully completed. Also was shown, that NT-702 has an anti-inflammatory effect as well as a bronchodilating effect and might be useful as a novel potent therapeutic agent with both a bronchodilating and an anti-inflammatory effect.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094125 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19616537 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | Unknown Approved UseUnknown |
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Palliative | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Optimal assessment of baseline treadmill walking performance in claudication clinical trials. | 2007 May |
|
NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase inhibitor, improves reduced walking distance and lowered hindlimb plantar surface temperature in a rat experimental intermittent claudication model. | 2007 Sep 1 |
|
NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase 3 inhibitor, suppress the asthmatic response in guinea pigs, with both bronchodilating and anti-inflammatory effects. | 2009 Sep 15 |
Patents
Sample Use Guides
4 mg and/or 8 mg PAROGRELIL taken twice a day for 24 weeks
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18558016
Was investigated the effects of NT-702 (PAROGRELIL) on arterioles isolated from rabbit lumbar spinal cords. NT-702 caused a dose-dependent dilation of the isolated spinal arterioles. The disruption of endothelium produced a significant reduction of higher concentrations(10(-7) and 10(-6) M), but not lower concentrations (less than 10(-8) M), of NT-702-induced vasodilation. The NT-702-induced vasodilation of the arterioles with endothelium was not affected by pretreatment with an inhibitor of nitric oxide, cyclooxygenase, or cytochrome P-450 monooxygenase. In contrast, catalase reduced significantly the higher concentrations of NT-702-induced vasodilation only.
Substance Class |
Chemical
Created
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Edited
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Record UNII |
65O9DMS368
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Record Status |
Validated (UNII)
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