Murray K J, Eden R J, England P J, Dolan J, Grimsditch D C, Stutchbury C A, Patel B, Reeves M L, Worby A, Torphy T J
SmithKline Beecham Pharmaceuticals, Herts, UK.
Agents Actions Suppl. 1991;34:27-46.
Selective inhibitors of the cyclic nucleotide phosphodiesterase (PDE) isoenzymes have been studied to assess the potential for such agents in the treatment of asthma. A novel selective PDE V inhibitor, SK&F 96231, reversed the bronchoconstriction induced in anaesthetised guinea pigs by histamine, a thromboxane-mimetic or by ovalbumin challenge. There was no effect of SK&F 96231 on heart rate or blood pressure in conscious dogs. Siguazodan (SK&F 94836, a selective PDE III inhibitor) caused bronchodilation but also had cardiovascular effects in conscious dogs. Studies on the PDE profile of various inflammatory cells have indicated that inhibition of PDE IV would be beneficial in the treatment of the inflammatory aspects of asthma and this is briefly reviewed.
已对环核苷酸磷酸二酯酶(PDE)同工酶的选择性抑制剂进行了研究,以评估此类药物在治疗哮喘方面的潜力。一种新型的选择性PDE V抑制剂SK&F 96231可逆转组胺、血栓素类似物或卵清蛋白激发在麻醉豚鼠中引起的支气管收缩。SK&F 96231对清醒犬的心率或血压无影响。西呱达旦(SK&F 94836,一种选择性PDE III抑制剂)可引起支气管扩张,但对清醒犬也有心血管作用。对各种炎症细胞的PDE谱的研究表明,抑制PDE IV对治疗哮喘的炎症方面有益,本文对此进行简要综述。