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1990年,在瑞士召开的一次国际会议上的报告表明,磷酸二酯酶(PDE)Ⅲ型(cGMP抑制型)的抑制似乎可引起支气管扩张,而PDEⅣ型(cAMP 特异的)的抑制则与抗炎活性有关。两个 PDEⅡ/Ⅲ型抑制剂,zardaverine 和 AH21132在动物上具有抗炎活性,但后者不会引起与 PDE 抑制有关的呕吐。一种选择性 cGMP 特异的 PDE 抑制剂SK&F 96231具有支气管扩张作用。新的白三烯受体拮抗剂和5-脂氧化酶抑制剂对哮喘治疗的疗效及作用强度有待评价。在早期临床试验中,吸入 LTD_4后,用白三烯受体拮抗剂ICI 204219能使量一效曲线产生大于2 log 单位的位移;志愿受试者吸入过敏原后,ICI
In 1990, an international conference in Switzerland reported that inhibition of phosphodiesterase (PDE) type III (cGMP inhibitory) appeared to cause bronchiectasis whereas inhibition of PDE type IV (cAMP-specific) was associated with resistance Inflammatory activity related. Two PDE type II / III inhibitors, zardaverine and AH21132, have anti-inflammatory activity in animals, but the latter do not elicit vomiting associated with PDE inhibition. A selective cGMP-specific PDE inhibitor, SK & F 96231, has bronchodilatory effects. The efficacy and potency of new leukotriene receptor antagonists and 5-lipoxygenase inhibitors in the treatment of asthma have yet to be evaluated. In early clinical trials, the dose-effect curve produced greater than 2 log units displacement with the leukotriene receptor antagonist ICI 204219 after inhalation of LTD 4; after inhalation of allergens in volunteer subjects, ICI