组胺H1和H2受体拮抗剂与豚鼠离体心房及小鼠肿瘤性肥大细胞体外组胺摄取和代谢的相互作用。
Interaction of histamine H1-and H2-receptor antagonists with histamine uptake and metabolism by guinea-pig isolated atrium and mouse neoplastic mast cells cells in vitro.
作者信息
Fantozzi R, Franconi F, Mannaioni P F, Masini E, Moroni F
出版信息
Br J Pharmacol. 1975 Apr;53(4):569-74. doi: 10.1111/j.1476-5381.1975.tb07396.x.
Abstract
- Burimamide, metiamide, chlorpheniramine, triprolidine and cocaine, were tested as inhibitors of histamine uptake and metabolism in the guinea-pig atrium and in mouse neoplastic mast cells. 2. Cocaine did not affect the uptake and metabolism of histamine, either in the atrium or in the mast cells. All the antihistamines tested blocked the uptake and metabolism of histamine in both preparations. The order of potency was burimamide greater than chlorpheniramine greater than triprolidine greater than metiamide in the atrium; and burimamide greater than metiamide greater than triprolidine greater than chlorpheniramine, in the mase cells. 3. Comparison of the present results with the antihistamine activity of these blocking agents suggests that no correlation exists between the receptor blocking activity and the ability of these substances to act as inhibitors of histamine uptake and metabolism.
摘要
- 对丁咪胺、甲硫咪胺、氯苯那敏、曲普利啶和可卡因进行了测试，以研究它们对豚鼠心房和小鼠肿瘤性肥大细胞中组胺摄取和代谢的抑制作用。2. 可卡因对心房或肥大细胞中组胺的摄取和代谢均无影响。所有测试的抗组胺药均能阻断两种制剂中组胺的摄取和代谢。在心房中，效力顺序为丁咪胺＞氯苯那敏＞曲普利啶＞甲硫咪胺；在肥大细胞中，效力顺序为丁咪胺＞甲硫咪胺＞曲普利啶＞氯苯那敏。3. 将目前的结果与这些阻断剂的抗组胺活性进行比较表明，受体阻断活性与这些物质作为组胺摄取和代谢抑制剂的能力之间不存在相关性。
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