Uses
SCH 79797 Dihydrochloride is a selective PAR1 antagonist.
Definition
ChEBI: N3-cyclopropyl-7-[(4-propan-2-ylphenyl)methyl]pyrrolo[3,2-f]quinazoline-1,3-diamine is a member of quinazolines.
Biological Activity
Potent, selective non-peptide PAR 1 receptor antagonist (IC 50 = 70 nM). Inhibits haTRAP-induced- but not g-thrombin-, ADP- or collagen-induced human platelet aggregation. Also selectively blocks PAR 1 agonist- or thrombin-induced increases in cytosolic Ca 2+ in vascular smooth muscle cells.
in vivo
SCH79797 (2.5-250 μg/kg; intravenous injection; male Sprague Dawley rats) treatment immediately before or during ischemia reduces myocardial necrosis following I/R in the intact rat heart in two rat models of myocardial ischemia/reperfusion (I/R) injury. This response is dose-dependent with the optimal dose being 25 μg/kg[4].
| Animal Model: | Male Sprague Dawley rats (8 weeks of age) with myocardial I/R injury[4] |
| Dosage: | 2.5 μg/kg, 10 μg/kg, 25 μg/kg, 50 μg/kg, 100 μg/kg, and 250 μg/kg |
| Administration: | Intravenous injection |
| Result: | Immediately before or during ischemia reduced myocardial necrosis following I/R in the intact rat heart. |
IC 50
PAR1: 70 nM (IC
50); PAR1: 35 nM (Ki)
![N3-cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine dihydrochloride Structure](https://www.chemicalbook.com/CAS/GIF/245520-69-8.gif)