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本研究目的旨在观察ＰＤＥＩＶ抑制剂咯利普兰对沙丁胺醇（ＳＢ）耐受性的影响。用豚鼠离体气管标本，预先接触ＳＢ１μｍｏｌ·Ｌ－１，１ｈ可使ＳＢ对抗乙酰甲胆碱气管收缩作用的剂量反应曲线右移５倍，最大松弛率下降３０％，形成ＳＢ气管松弛作用的耐受性。磷酸二酯酶（ＰＤＥ）ＩＶ抑制剂咯利普兰能翻转ＳＢ气管松弛作用的耐受性，但ＰＤＥＩＩ抑制剂氰胍哒嗪则不能。虽然蛋白合成抑制剂环己酰亚胺对ＳＢ耐受性无预防作用，但上述结果仍提示ＳＢ气管松弛作用的耐受性可能与ＰＤＥＩＶ活性的增高有关。
The purpose of this study was to investigate the effects of PDEIV inhibitor rolipram on salbutamol (SB) tolerance. With guinea pig isolated tracheal specimens, pre-exposure to SB1μmol·L-1, 1h SB dose-response curve of anti-methacholine contraction of the right 5 times, the maximum relaxation rate decreased by 30%, the formation of SB tracheal relaxation resistance By sexual. Rolipram, a phosphodiesterase (PDE) IV inhibitor, was able to overturn the SB tracheal relaxation tolerance, but not the PDEII inhibitor cyanidazine. Although the protein synthesis inhibitor cycloheximide did not prevent SB tolerance, the above results suggest that SB tracheal relaxation may be related to the increase of PDEIV activity.