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“8204”对心血管系统和支气管平滑肌的药理作用

PHARMACOLOGICAL ACTIONS OF "8204" ON CARDIOVASCULAR SYSTEM AND BRONCHIAL SMOOTH MUSCLE

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【作者】 朱志华杨萍唐祖年曾炎根董娟郑莉萍王增田

【Author】 ZHU Zhi-Hua, YANG Ping, TANG Zu-Nian, ZENG Yan-Gen~*, DONG Juan~*, ZHENG Li-Ping~* and WANG Zeng-Tian~*(Guilin Medical School, Guilin. ~*Henan Institute of Pharmaceutical Industrial Research, Kaifeng)

【机构】 桂林医学专科学校河南省医药工业研究所河南省医药工业研究所 桂林桂林开封开封

【摘要】 “8204”是新合成的化合物。动物实验表明:可使冠脉流量增加,心肌耗氧置降低,提高动物常压和低压情况下的缺氧耐力;对垂体后叶素诱发的缺血性心电图有保护作用,还能松弛离体豚鼠气管平滑肌,对抗乙酰胆碱和组胺引起的气管、支气管平滑肌收缩,增加豚鼠肺灌流量;对豚鼠吸入组胺引起的哮喘有明显保护作用。这些结果提示“8204”对治疗心肌缺血和支气管哮喘是有益的。

【Abstract】 "8204" (1- (2,3,4-trimethoxybenzyl)-4-(α-trimethysilyloxy-2-(4-amino-3′, 5′-dichlorophenyl) ethyl) piperazine dihydroehloride) was synthesized by Henan Institute of Pharmaceutical Industrial Research. "8204" had been shown to increase coronary flow in isolated rabbit heart. In anesthetized open-chest dogs, intravenous injection of "8204" (4 mg/kg) enhanced coronary venous flow, lowered myocardial O2 consumption and slowed heart rate."8204" was shown to increase the tolerance of mice to hypoxia and prevent rats from pituitrin induced change of ECG. "8204" exhibited relaxing effect on guineapig tracheal smooth muscle made to contract by acetylcholine and histamine. It increased the perfusion rate of isolated lung preparation of guinea-pig from 5.7±2.0 to 16.3±5.8 ml/min (p<0.001).Intraperitioneal injection of "8204" 2 mg/kg showed prominent protective effect against bronchial asthma induced by inhalation of histamine in conscious guineapig.In rats given "8204" 20 mg/kg or 40 mg/kg per day orally for three months, no obvious pathological change in various tissue was found.It appears that "8204" probably have helpful effects in the treatment of coronary heart disease, and may be an effective antiasthmatic agent.

  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1985年12期
  • 【被引频次】1
  • 【下载频次】15
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