Antiplatelet and Antithrombotic Activities of NQ301, 2-Chloro-3-(4-acetophenyl)-amino-1, 4-naphthoquinone

• Published in: Biological & pharmaceutical bulletin Vol. 22; no. 12; pp. 1284 - 1287
• Main Authors: KANG, Won-Seek, RYU, Chung-Kyu, CHUNG, Kwang-Hoe, KO, Myoung-Wha, JOO, Jeong-Chul, YUK, Dong-Yeon, YOO, Hwan-Soo, YUN, Yeo-Pyo
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 01.12.1999; Maruzen; Japan Science and Technology Agency
• Subjects: 1, 4-naphthoquinone; Animals; anticoagulation; antiplatelet; antithrombosis; Biological and medical sciences; Bleeding Time; Blood Coagulation - drug effects; Blood Platelets - drug effects; Blood. Blood coagulation. Reticuloendothelial system; Fibrinolytic Agents - pharmacology; Fibrinolytic Agents - therapeutic use; Humans; In Vitro Techniques; Male; Medical sciences; Mice; Mice, Inbred ICR; Naphthoquinones - pharmacology; Naphthoquinones - therapeutic use; Pharmacology. Drug treatments; Platelet Aggregation - drug effects; Platelet Aggregation Inhibitors - pharmacology; Platelet Aggregation Inhibitors - therapeutic use; Rats; Rats, Sprague-Dawley; Thrombosis - prevention & control; Treatment efficiency; Rodentia; Oral administration; Cardiovascular disease; Naphthoquinone derivatives; In vitro; Thrombosis; Biological activity; Antiplatelet agent; Venous disease; Vascular disease; In vivo; Vertebrata; Chemotherapy; Experimental disease; Platelet; Mammalia; Treatment; Ex vivo; Mouse; Animal; Mechanism of action; Vein
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.22.1284

The antiplatelet and antithrombotic activities of a newly synthesized NQ301, 2-chloro-3-(4-acetophenyl)-amino-1, 4-naphthoquinone, were investigated on human platelet aggregation in vitro and rats ex vivo, and murine pulmonary thrombosis in vivo. NQ301 potently inhibited ADP-, collagen-, epinephrine- and calcium ionophore A23187-induced human platelet aggregation in a concentration-dependent manner in vitro. NQ301 significantly inhibited platelet aggregation in orally administered rats ex vivo. NQ301 prevented death due to pulmonary thrombosis in mice dose-dependently in vivo. NQ301 also showed significant prolongation of tail bleeding time in conscious mice. However, NQ301 did not alter such coagulation parameters as activated partial thromboplastin time, prothrombin time, and thrombin time in human plasma. These results suggest that NQ301 may be a promising antithrombotic agent, and the antithrombotic activity of NQ301 may be due to antiplatelet aggregation activity but not to in vitro anticoagulation.