タイトル無し
スポンサーリンク
概要
- 論文の詳細を見る
MCI-9038 (MD-805, synthetic thrombin inhibitor No. 805), (2R, 4R)-4-methyl-1-[N2-(3-methyl-1, 2, 3, 4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2-piperidinecarboxylic acid monohydrate, is the new thrombin inhibitor that shows a potent and highly selective inhibitory effect.We devised the new experimental arterial thrombosis in rabbits and evaluated the effect of MCI-9038 on the thrombus formation of this thrombosis.This experimental thrombosis was developed at the carotid artery by injuring the vessel wall by acetic acid, which shows a marked potency of a penetration and stimulation to tissues, and the procedure was as follows; the exposed carotid arteries of a rabbit were surrounded with absorbent cotton in a plastic capsule, and then absorbent cotton was soaked sufficiently with an aqueous 90% acetic acid for three hours.The size of the thrombus was classified as follows; occlusion, large, middle, small and no thrombus. The thrombus was mainly consisted of platelets. The continuous infusion at rates of 1 and 3μg/kg/min of MCI-9038 showed the obvious inhibitory effects on the thrombus generation, the plasma concentrations being 0.16-0.17μM and 0.41-0.49μM respectively. Heparin was administered intravenously at five minutes before soak of acetic acid and showed the dosedependent inhibitory effects at a dose of 300units/kg or more.Oral administration of MCI-9038 at doses more than 10mg/kg (plasma concentration; 0.17-0.25μM) showed the inhibitory effect, but not at a dose of 2.5mg/kg.Aspirin snowed the obvious inhibitory effect at an oral administration of 300mg/kg.From above results, it is considered that MCI-9038 would be used clinically as an effective antithrombotic agent.
- 一般社団法人 日本血栓止血学会の論文
一般社団法人 日本血栓止血学会 | 論文
- 日本人のＡＤＡＭＴＳ１３
- Infection of specific strains of Streptococcus mutans exacerbated intracerebral hemorrhage
- Transcriptional regulation of megakaryopoiesis and thrombopoiesis
- 新規血小板活性化受容体ＣＬＥＣ－２ その発見から今後の展望まで:その発見から今後の展望まで
- １．臨床血栓止血学オーバービュー