Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C15H16N4O2 |
| Molecular Weight | 284.3131 |
| Optical Activity | ( + ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(CNC(=O)C1=CC=CN=C1)NC(=O)C2=CC=CN=C2
InChI
InChIKey=KTXBOOWDLPUROC-UHFFFAOYSA-N
InChI=1S/C15H16N4O2/c1-11(19-15(21)13-5-3-7-17-10-13)8-18-14(20)12-4-2-6-16-9-12/h2-7,9-11H,8H2,1H3,(H,18,20)(H,19,21)
Nicaraven is a hydroxyl radical scavenger with antivasospastic and neuroprotective effects. Chugai (the Japanese subsidiary of Roche) is developing nicaraven (Antevas), a water-soluble antioxidant, for the potential treatment of disorders caused by acute cerebrovascular diseases. A registration application was filed in April 1995, and in April 2002, nicaraven was still awaiting registration in Japan. By August 2002, Chugai had filed an NDA in Japan for the additional indication of subarachnoidal bleeding.
Approval Year
Sample Use Guides
4 g nicaraven infused intravenously for 6-8 hours once a day
Route of Administration:
Intravenous
The antiplatelet activities in vitro of nicaraven were examined. The concentrations of nicaraven tested were 3.50 x 10(-5) mol/L, 1.75 x 10(-4) mol/L, 3.50 x 10(-4) mol/L, and 1.75 x 10(-3) mol/L, respectively. The maximum aggregation rate induced by adenosine diphosphate (ADP) was significantly inhibited by nicaraven at concentration ranges of 3.50 x 10(-4) mol/L or higher in the healthy volunteer platelets. The maximum aggregation rate induced by collagen was significantly inhibited by 1.75 x 10(-3) mol/L of nicaraven. Using platelets from patients with cerebral thrombosis, the maximum aggregation rate induced by ADP was significantly inhibited by 1.75 x 10(-3) mol/L of nicaraven. Furthermore, the maximum aggregation rate induced by collagen were significantly reduced by 1.75 x 10(-3) mol/L of nicaraven.
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457KF8A3QQ
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SUBSTANCE RECORD
