Kagitani F, Gotoh Y, Kimura A, Nakayama H, Sato A
Department of the Autonomic Nervous System, Tokyo Metropolitan Institute of Gerontology, Itabashiku, Japan.
Eur J Pharmacol. 1997 Jul 30;332(1):89-95. doi: 10.1016/s0014-2999(97)01060-1.
The effects of a newly developed drug for incontinence, (5RS, 1'SR)-5-benzyl-3-(3'-morpholino-1'-phenylpropyl)-1,3-oxazolidin-2- one monofumarate (NC-1800), on bladder and periurethral skeletal muscle functions were tested in urethane-anesthetized rats. When the bladder pressure was low, i.v. administration of NC-1800 at doses of 4 to 16 mg/kg induced dose-dependent increases of vesical pressure associated with increases in pelvic efferent nerve activity. When the bladder was expanded, the same administration of NC-1800 induced dose-dependent inhibitions of both vesical micturition contractions and rhythmic pelvic burst discharges. Hypogastric efferent nerve activity was not affected. The periurethral electromyogram (EMG) activity was excited when the bladder was contracted, and EMG activity was inhibited when the bladder was relaxed by NC-1800. Pelvic ganglionic transmission, neuromuscular transmission of both bladder and urethra, and muscle contractility itself of bladder and urethra were not affected by NC-1800. These results suggest that NC-1800 modulates the functions of the bladder and urethra by influencing pelvic and pudendal nerve activity via the central nervous system.
在氨基甲酸乙酯麻醉的大鼠中测试了一种新开发的治疗尿失禁药物（5RS，1'SR）-5-苄基-3-（3'-吗啉代-1'-苯丙基）-1,3-恶唑烷-2-酮单富马酸盐（NC-1800）对膀胱和尿道周围骨骼肌功能的影响。当膀胱压力较低时，静脉注射4至16mg/kg剂量的NC-1800会引起膀胱压力的剂量依赖性增加，并伴有盆腔传出神经活动的增加。当膀胱扩张时，相同剂量的NC-1800注射会引起膀胱排尿收缩和有节奏的盆腔爆发性放电的剂量依赖性抑制。腹下传出神经活动未受影响。当膀胱收缩时，尿道周围肌电图（EMG）活动增强，而当NC-1800使膀胱松弛时，EMG活动受到抑制。盆腔神经节传递、膀胱和尿道的神经肌肉传递以及膀胱和尿道本身的肌肉收缩力均不受NC-1800的影响。这些结果表明，NC-1800通过中枢神经系统影响盆腔和阴部神经活动来调节膀胱和尿道的功能。
