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The mechanism of action of KBT-3022, a new antiplatelet agent.

作者信息

Matsuo K, Yokota K, Yamashita A, Oda M

机构信息

New Drug Research Laboratories, Kanebo, Ltd., Osaka, Japan.

出版信息

Gen Pharmacol. 1997 Feb;28(2):229-35. doi: 10.1016/s0306-3623(96)00190-5.

DOI:10.1016/s0306-3623(96)00190-5
PMID:9013200
Abstract
  1. The mechanism of action of a new antiplatelet agent, KBT-3022 (ethyl 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl]pyrrol-1-ylacetate) and its active main metabolite, desethyl KBT-3022, was investigated. 2. KBT-3022 and desethyl KBT-3022 inhibited cyclooxygenase from ovine seminal gland with IC50 values of 0.69 and 0.43 microM, respectively. 3. At concentrations higher than those required for cyclooxygenase inhibition, desethyl KBT-3022 inhibited cAMP-phosphodiesterase, specific binding of U46619, and release of phosphatidic acid from thrombin-stimulated platelets. 4. Oral administration of KBT-3022 inhibited the production of thromboxane B2 during blood coagulation more potently than the production of 6-keto-prostaglandin F1 alpha from aortic strips in guinea pigs. 5. These findings suggest that KBT-3022 may inhibit platelet activation principally via the inhibition of cyclooxygenase by desethyl KBT-3022.
摘要

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