Crema A, Frigo G M, Lecchini S, Manzo L, Onori L, Tonini M
Br J Pharmacol. 1983 Mar;78(3):599-603. doi: 10.1111/j.1476-5381.1983.tb08820.x.
1 In the isolated internal anal sphincter of the guinea-pig, adenosine 5'-triphosphate (ATP) and adenosine induced a concentration-dependent and tetrodotoxin-insensitive relaxation. 2 Pretreatment with theophylline (25-50 microM) had no significant effect on the concentration-response curves obtained with either purine compound. 3 Reactive blue 2 (25-100 microM) shifted the curve to ATP to the right in a dose-dependent fashion leaving that to adenosine unaltered. The antagonism appeared to be non-competitive. 4 Neither reactive blue 2 nor purine receptor occupation by ATP or adenosine altered the electrically-induced non-adrenergic, non-cholinergic inhibitory response. 5 The actions of ATP and adenosine in the guinea-pig internal anal sphincter appear to be mediated by separate receptors. These receptors are not involved in the nerve-mediated relaxation.
1 在豚鼠离体的肛门内括约肌中,5'-三磷酸腺苷(ATP)和腺苷可引起浓度依赖性且对河豚毒素不敏感的舒张反应。2 用茶碱(25 - 50微摩尔)预处理对两种嘌呤化合物所得到的浓度-反应曲线均无显著影响。3 活性蓝2(25 - 100微摩尔)以剂量依赖性方式使ATP的曲线右移,而腺苷的曲线未改变。这种拮抗作用似乎是非竞争性的。4 活性蓝2以及ATP或腺苷对嘌呤受体的占据均未改变电诱导的非肾上腺素能、非胆碱能抑制反应。5 ATP和腺苷在豚鼠肛门内括约肌中的作用似乎是由不同的受体介导的。这些受体不参与神经介导的舒张反应。