Reference

Inhibition of thrombin-induced platelet adherence to vascular cells by synthetic thrombin inhibitor No

Inhibition of thrombin-induced platelet adherence to vascular cells by synthetic thrombin inhibitor No. 805. Czervionke, Robert L.; Hoak, John C.; Haycraft, Donna L.; Fry, Glenna L. (Coll. Med., Univ. Iowa, Iowa City, IA 52242, USA). Trans. Assoc. Am. Physicians, 96, 271-7 (English) 1983. CODEN: TAAPAI. ISSN: 0066-9458. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Under the conditions of this study, No. 805 [74863-84-6] did not inhibit collagen- and ADP-induced human platelet aggregation, but it did inhibit thrombin [9002-04-4]-induced platelet aggregation. Inhibition of thrombin aggregation could be overcome if the thrombin level in the same platelet suspension was elevated. With thrombin-treated vascular monolayers, synthetic thrombin inhibitor No. 805 was an effective inhibitor of thrombin-induced platelet adherence to endothelial and fibroblast monolayers and empty culture dishes. With thrombin-induced platelet aggregates, No. 805 inhibited platelet adherence to endothelium, but only partially inhibited adherence to the more thrombogenic fibroblast and empty dish surfaces.

In vitro studies of a new synthetic thrombin inhibitor

In vitro studies of a new synthetic thrombin inhibitor. Green, David; Ts'ao, Chung Hsin; Reynolds, Nancy; Kahn, David; Kohl, Helga; Cohen, Isaac (Med. Sch., Northwestern Univ., Chicago, IL, USA). Thromb. Res., 37(1), 145-53 (English) 1985. CODEN: THBRAA. ISSN: 0049-3848. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) MCI-9038 [(2R,4R)-4-methyl-1-[Na-(3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfony l)-L-arginyl]-2-piperidine carboxylic acid](I) [74863-84-6] was a potent synthetic inhibitor of thrombin [9002-04-4]. In concns. as low as 1 mM, the thrombin time, prothrombin time, and partial thromboplastin time were more than doubled. The venom (Bothrops atrox) time was similarly prolonged. The drug also inhibited the thrombin-induced activation of factor VIII [9001-27-8] and factor XIII [9013-56-3]. While MCI-9038 in concns. of 10-4 M had no effect on platelet aggregation induced by collagen, ADP, epinephrine, and arachodonate, nanomolar concns. inhibited thrombin-induced platelet aggregation and the release of platelet ADP. The drug also significantly inhibited the adhesion of thrombin-treated platelets to cultured bovine aortic endothelial cells. Apparently, MCI-9038 is an extremely potent inhibitor of the effects of thrombin on platelets and clotting factors.