Mizrahi J, Couture R, Caranikas S, Regoli D
Pharmacology. 1982;25(1):39-50. doi: 10.1159/000137722.
Peptide and non-peptide agents were tested for their stimulatory or inhibitory effects on circular strips of guinea pig isolated tracheae. Substance P, eledoisin, physalaemin, neurotensin, angiotensin, histamine and carbachol were found to contract, while noradrenaline, dopamine, bradykinin, nucleotides (AMP, ADP, ATP) and prostaglandins (PGE1, PGE2, PGA2) induced concentration-dependent relaxations of tracheae contracted with substance P or carbachol. Indomethacin (2.8 X 10(-6) M) significantly potentiated the effect of substance P and blocked that of bradykinin. The contractions to substance P of tissues treated with indomethacin were not modified by atropine, methysergide, diphenhydramine, cimetidine, propranolol, phentolamine, [Leu8]-ATII, [Leu8]-des-Arg9-bradykinin, naloxone and baclofen. The order of potency of C-terminal fragments of substance P was: hexa(6-11) greater than hepta(5-11) greater than substance P greater than = octa(4-11). It is concluded that the guinea pig isolated trachea is a pharmacological preparation sensitive to numerous agents and useful for studying structure-activity relationship and the mechanism of cellular action of several peptides, particularly substance P.
测试了肽类和非肽类药物对豚鼠离体气管环形条的刺激或抑制作用。发现P物质、eledoisin、physalaemin、神经降压素、血管紧张素、组胺和卡巴胆碱可引起收缩，而去甲肾上腺素、多巴胺、缓激肽、核苷酸（AMP、ADP、ATP）和前列腺素（PGE1、PGE2、PGA2）可诱导对用P物质或卡巴胆碱收缩的气管产生浓度依赖性舒张。吲哚美辛（2.8×10⁻⁶ M）显著增强P物质的作用并阻断缓激肽的作用。用吲哚美辛处理的组织对P物质的收缩不受阿托品、甲基麦角新碱、苯海拉明、西咪替丁、普萘洛尔、酚妥拉明、[Leu8]-ATII、[Leu8]-去-Arg9-缓激肽、纳洛酮和巴氯芬的影响。P物质C末端片段的效价顺序为：六肽（6-11）＞七肽（5-11）＞P物质＞=八肽（4-11）。结论是豚鼠离体气管是一种对多种药物敏感的药理学制剂，可用于研究几种肽，特别是P物质的构效关系和细胞作用机制。
