Satoh H, Kobayashi T, Higo K, Karasawa A
Department of Pharmacology, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.
Jpn J Pharmacol. 1994 May;65(1):45-50. doi: 10.1254/jjp.65.45.
We investigated the effect of KW-3635, a selective thromboxane (TX) A2-receptor antagonist, on the arachidonic acid (AA)-induced transient cerebral ischemia in anesthetized dogs. Intracarotid-arterial injection of AA (0.25-1 mg/kg) produced a transient and reversible decrease in electroencephalographic (EEG) activity. The reduction of EEG power was inhibited by the intravenous injection of KW-3635 or aspirin, a cyclooxygenase inhibitor. Local cortical perfusion (LCP) measured by a laser-doppler flow meter was also reduced concomitantly with the reduction of EEG power. Although KW-3635 at 1 and 3 mg/kg (i.v.) did not affect the maximum reduction of LCP, the duration of the reduction period of LCP was significantly shortened by KW-3635. On the other hand, aspirin at 1 and 3 mg/kg (i.v.) inhibited both the maximum and the delay of LCP reduction. The intravenous administration of KW-3635 or aspirin caused dose-dependent inhibition of ex vivo platelet aggregation stimulated by AA (150 microM) at the doses that improve the EEG activity. These data suggest that TXA2 is one of the important factors in the AA-induced transient reduction of EEG activity in anesthetized dogs. The TXA2-receptor antagonist may be useful for protection against the ischemic brain damage following transient ischemic attack.
我们研究了选择性血栓素(TX)A2受体拮抗剂KW-3635对麻醉犬花生四烯酸(AA)诱导的短暂性脑缺血的影响。颈内动脉注射AA(0.25 - 1mg/kg)可导致脑电图(EEG)活动出现短暂且可逆的降低。静脉注射KW-3635或环氧化酶抑制剂阿司匹林可抑制EEG功率的降低。通过激光多普勒流量计测量的局部皮质灌注(LCP)也随着EEG功率的降低而同时降低。尽管静脉注射1mg/kg和3mg/kg的KW-3635不影响LCP的最大降低幅度,但KW-3635可显著缩短LCP降低期的持续时间。另一方面,静脉注射1mg/kg和3mg/kg的阿司匹林可抑制LCP降低的最大值和延迟。在能改善EEG活动的剂量下,静脉注射KW-3635或阿司匹林可引起剂量依赖性地抑制由AA(150μM)刺激的离体血小板聚集。这些数据表明,TXA2是AA诱导麻醉犬EEG活动短暂降低的重要因素之一。TXA2受体拮抗剂可能有助于预防短暂性脑缺血发作后的缺血性脑损伤。