Maggi C A, Giuliani S, Patacchini R, Conte B, Furio M, Santicioli P, Meli P, Gragnani L, Meli A
Pharmacology Department, A. Menarini Pharmaceuticals, Florence, Italy.
Eur J Pharmacol. 1988 Aug 2;152(3):273-9. doi: 10.1016/0014-2999(88)90722-4.
SC-19220 (5-20 mg/kg i.v.), a competitive receptor antagonist of PGE, increased the bladder capacity and reduced the voiding efficiency of micturition (elicited by slow transvesical filling) of urethane-anesthetized rats. The effect of SC-19220 was prevented by indomethacin pretreatment, whereas indomethacin per se mimicked the effects of SC-19220. SC-19220 produced a competitive rightward shift of the dose-response curve for the contractile effect induced by PGE2 on strips of rat detrusor muscle in vitro, whereas the amplitude of nerve-mediated twitches was unaffected. These findings support the hypothesis that endogenous PGE2 is physiologically involved in the regulation of vesicourethral motility in this species by facilitating attainment of the micturition threshold during the collection phase of the cystometrogram.
SC - 19220(静脉注射5 - 20毫克/千克),一种前列腺素E(PGE)的竞争性受体拮抗剂,可增加氨基甲酸乙酯麻醉大鼠的膀胱容量,并降低(由缓慢膀胱灌注引发的)排尿效率。吲哚美辛预处理可阻止SC - 19220的作用,而吲哚美辛本身可模拟SC - 19220的作用。在体外,SC - 19220使PGE2对大鼠逼尿肌条收缩作用的剂量 - 反应曲线发生竞争性右移,而神经介导的抽搐幅度不受影响。这些发现支持了这样一种假说,即内源性PGE2通过在膀胱测压图收集阶段促进排尿阈值的达到,在生理上参与了该物种膀胱尿道运动的调节。