Langlands J M, Rodger I W, Diamond J
Division of Pharmacology & Toxicology, Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, Canada.
Br J Pharmacol. 1989 Oct;98(2):336-8. doi: 10.1111/j.1476-5381.1989.tb12600.x.
The effect of a cyclic GMP phosphodiesterase inhibitor, M&B 22948, on methacholine- and histamine-induced contraction and inositol 1,4,5-trisphosphate (IP3) elevation was studied in guinea-pig tracheal rings. After addition of methacholine or histamine the rise in IP3 content was rapid and transient reaching a maximum after 5-15 s, which coincided with the maximum rate of tension development. Cyclic GMP levels of the tissue were elevated by M&B 22948 before agonist stimulation and further elevated by addition of methacholine or histamine. Cyclic AMP levels were not altered by any of these agents. M&B 22948 abolished IP3 generation induced by methacholine or histamine, but did not alter the rate or magnitude of tension development. Thus, IP3 generation does not appear to be responsible for the contractions induced by methacholine or histamine in this tissue.
在豚鼠气管环中研究了环鸟苷酸磷酸二酯酶抑制剂M&B 22948对乙酰甲胆碱和组胺诱导的收缩以及肌醇1,4,5-三磷酸(IP3)升高的影响。加入乙酰甲胆碱或组胺后,IP3含量迅速短暂升高,在5-15秒后达到最大值,这与张力发展的最大速率一致。在激动剂刺激前,M&B 22948使组织中环鸟苷酸水平升高,加入乙酰甲胆碱或组胺后进一步升高。环腺苷酸水平不受这些药物中任何一种的影响。M&B 22948消除了乙酰甲胆碱或组胺诱导的IP3生成,但不改变张力发展的速率或幅度。因此,在该组织中,IP3生成似乎不是乙酰甲胆碱或组胺诱导收缩的原因。