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咯利普兰可抑制豚鼠体内由血小板活化因子、组胺和缓激肽诱导的气道微血管渗漏。

Rolipram inhibits airway microvascular leakage induced by platelet-activating factor, histamine and bradykinin in guinea-pigs.

作者信息

Ortiz J L, Cortijo J, Vallés J M, Bou J, Morcillo E J

机构信息

Department of Pharmacology, University of Valencia, Spain.

出版信息

J Pharm Pharmacol. 1993 Dec;45(12):1090-2. doi: 10.1111/j.2042-7158.1993.tb07188.x.

Abstract

Rolipram (0.1-1000 micrograms kg-1, i.v.) reduced the increase in microvascular permeability induced by platelet-activating factor (PAF; 50 ng kg-1, i.v.) at different sites of the guinea-pig airways. Rolipram (1-100 micrograms kg-1, i.v.) inhibited histamine (30 micrograms kg-1, i.v.)- and bradykinin (0.3 micrograms kg-1, i.v.)-induced airway microvascular leakage. These effects of rolipram were obtained at doses which inhibit histamine (7-20 micrograms kg-1 min-1)-induced bronchoconstriction (IC50 = 3 +/- 1 micrograms kg-1, i.v.) without depressing arterial blood pressure in the guinea-pig. Aminophylline (50 mg kg-1) did not change the effect of PAF. The anti-exudative effect of rolipram is of potential therapeutic value in asthma.

摘要

咯利普兰(0.1 - 1000微克/千克,静脉注射)可减轻豚鼠气道不同部位由血小板活化因子(PAF;50纳克/千克,静脉注射)诱导的微血管通透性增加。咯利普兰(1 - 100微克/千克,静脉注射)可抑制组胺(30微克/千克,静脉注射)和缓激肽(0.3微克/千克,静脉注射)诱导的气道微血管渗漏。咯利普兰的这些作用是在抑制组胺(7 - 20微克/千克·分钟)诱导的支气管收缩(IC50 = 3 ± 1微克/千克,静脉注射)且不降低豚鼠动脉血压的剂量下获得的。氨茶碱(50毫克/千克)不改变PAF的作用。咯利普兰的抗渗出作用在哮喘治疗中具有潜在的治疗价值。

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