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
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
Sourcing
PubMed
Patents
Sample Use Guides
4 mg and/or 8 mg PAROGRELIL taken twice a day for 24 weeks
Route of Administration:
Oral
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.