Watanabe K, Hayashi Y, Ikeda K, Ohnishi H
Pharmaceuticals Research Laboratories, Fujirebio Inc., Tokyo, Japan.
Nihon Yakurigaku Zasshi. 1991 Mar;97(3):153-65. doi: 10.1254/fpj.97.3_153.
Effect of moxisylyte on the lower urinary tracts was studied with the urethral pressure profile (UPP) and balloon method in anesthetized female dogs. In the UPP, moxisylyte produced relaxation in both the proximal and distal urethras. The relaxation effects of prazosin and bunazosin on the distal urethra was weaker than on the proximal urethra. In the balloon method, moxisylyte, prazosin, bunazosin and phentolamine caused a decrease in urethral pressure dose-dependently. The ID25 values of moxisylyte, prazosin, bunazosin and phentolamine were 23.4, 0.43, 0.76 and 33.1 micrograms/kg, respectively. In the balloon method, moxisylyte noncompetitively antagonized phenylephrine induced contraction of the urethra at high doses, whereas prazosin, bunazosin, phentolamine and yohimbine competitively antagonized phenylephrine induced contraction of the urethra. These results suggest that moxisylyte relaxes both the proximal and distal urethras due to alpha 1-adrenoceptor antagonistic and direct urethral smooth muscle relaxant actions. Therefore, moxisylyte is useful for the therapeutic treatment of micturitional disorder.
在麻醉的雌性犬中，采用尿道压力分布图（UPP）和球囊法研究了莫西赛利对下尿路的影响。在UPP实验中，莫西赛利使尿道近端和远端均产生松弛。哌唑嗪和布那唑嗪对尿道远端的松弛作用比对近端尿道的作用弱。在球囊法实验中，莫西赛利、哌唑嗪、布那唑嗪和酚妥拉明均剂量依赖性地降低尿道压力。莫西赛利、哌唑嗪、布那唑嗪和酚妥拉明的ID25值分别为23.4、0.43、0.76和33.1微克/千克。在球囊法实验中，高剂量时莫西赛利非竞争性拮抗去氧肾上腺素诱导的尿道收缩，而哌唑嗪、布那唑嗪、酚妥拉明和育亨宾竞争性拮抗去氧肾上腺素诱导的尿道收缩。这些结果表明，莫西赛利通过α1-肾上腺素能受体拮抗作用和直接的尿道平滑肌松弛作用，使尿道近端和远端均产生松弛。因此，莫西赛利可用于治疗排尿障碍。
