Post M J, te Biesebeek J D, Wemer J, van Rooij H H, Porsius A J
Department of Pharmacotherapy, Faculty of Pharmacy, University of Utrecht, The Netherlands.
Agents Actions. 1990 Apr;30(1-2):30-3. doi: 10.1007/BF01968990.
The effects of adenosine and some of its analogues on bronchoconstriction and mediator release were studied in isolated lungs of actively sensitized rats. Adenosine (ADO) and its analogues R-phenyl-iso-propyl-adenosine (R-PIA) and N-ethyl-carboxamide-adenosine (NECA), enhanced antigen-induced bronchoconstriction in a dose-dependent manner. The enhancement of anaphylactic bronchoconstriction by adenosine and its analogues was accompanied by a rise in histamine release. The observed rank order of potency for adenosine and analogues (NECA greater than or equal to R-PIA greater than ADO) did not permit an unequivocal classification of the adenosine receptor involved. Dipyridamole and S-(p-nitrobenzyl-6-thioinosine) (NBTI), both inhibitors of adenosine uptake, had no inhibitory influence on the adenosine-induced enhancement of anaphylactic bronchoconstriction. Therefore, this enhancement was likely to be mediated through an extra-cellular receptor. Theophylline inhibited the enhancement of anaphylactic bronchoconstriction by adenosine in a concentration-dependent manner, without affecting preformed mediator release.
在主动致敏大鼠的离体肺中研究了腺苷及其某些类似物对支气管收缩和介质释放的影响。腺苷(ADO)及其类似物R-苯基-异丙基-腺苷(R-PIA)和N-乙基-羧酰胺-腺苷(NECA)以剂量依赖性方式增强抗原诱导的支气管收缩。腺苷及其类似物对过敏性支气管收缩的增强作用伴随着组胺释放的增加。所观察到的腺苷及其类似物的效力顺序(NECA≥R-PIA>ADO)无法明确确定所涉及的腺苷受体类型。双嘧达莫和S-(对硝基苄基-6-硫代肌苷)(NBTI)这两种腺苷摄取抑制剂,对腺苷诱导的过敏性支气管收缩增强没有抑制作用。因此,这种增强作用可能是通过细胞外受体介导的。茶碱以浓度依赖性方式抑制腺苷对过敏性支气管收缩的增强作用,而不影响预先形成的介质释放。