Heaslip R J, Giesa F R, Rimele T J, Grimes D
Eur J Pharmacol. 1986 Aug 22;128(1-2):73-9. doi: 10.1016/0014-2999(86)90559-5.
A comparison has been made of the abilities of salbutamol, forskolin and prenalterol to relax guinea-pig tracheal rings contracted equivalently with either prostaglandin F2 alpha (PGF2 alpha) or carbachol. In the absence of spontaneous tension, 10(-6) M PGF2 alpha and 4 X 10(-7) M carbachol induced equivalent contractions of tracheal rings. Tracheal contractions induced by PGF2 alpha were more sensitive to the relaxant effects of salbutamol, forskolin or prenalterol than were contractions induced by carbachol. Each tracheal relaxant had a lower IC50 value for inhibiting PGF2 alpha-induced contractions, and prenalterol (a beta-adrenoceptor partial agonist) induced more complete relaxation of PGF2 alpha- than carbachol-induced tracheal tension. It is concluded that the tracheal relaxant activity of these compounds is in part dependent upon the contractile agent which induces tension, and that the variable sensitivity of different isolated tracheal muscle preparations to the actions of tracheal relaxants may result from differences in the contracting stimulus being antagonized in each of these models.
已对沙丁胺醇、福斯可林和普瑞特罗使豚鼠气管环舒张的能力进行了比较，这些气管环用前列腺素F2α（PGF2α）或卡巴胆碱进行了等效收缩。在无自发张力的情况下，10(-6)M PGF2α和4×10(-7)M卡巴胆碱可引起气管环等效收缩。PGF2α诱导的气管收缩比卡巴胆碱诱导的收缩对沙丁胺醇、福斯可林或普瑞特罗的舒张作用更敏感。每种气管舒张剂抑制PGF2α诱导的收缩的IC50值较低，且普瑞特罗（一种β肾上腺素受体部分激动剂）比卡巴胆碱诱导的气管张力更能使PGF2α诱导的气管张力完全舒张。结论是，这些化合物的气管舒张活性部分取决于诱导张力的收缩剂，并且不同分离的气管肌肉制剂对气管舒张剂作用的可变敏感性可能是由于在每个这些模型中被拮抗的收缩刺激存在差异所致。
