U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

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
Structure of PAROGRELIL HYDROCHLORIDE

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

HIDE SMILES / InChI

Description

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 TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Unknown
Palliative
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
4 mg and/or 8 mg PAROGRELIL taken twice a day for 24 weeks
Route of Administration: Oral
In Vitro Use Guide
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.