Morikawa K, Kakiuchi M, Yamauchi T, Hashimoto S, Miyashita N, Ichihashi M, Sawada Y, Kato H, Ito Y
Research Laboratories, Hokuriku Seiyaku Co., Fukui, Japan.
Nihon Yakurigaku Zasshi. 1988 Nov;92(5):311-24. doi: 10.1254/fpj.92.311.
The effects of HY-770 on micturition reflexes in rats, dogs and cats and urethral pressure in dogs were compared with those of flavoxate.HC1 (flavoxate), terodiline.HCl (terodiline) and oxybutynin.HCl (oxybutynin). 1) HY-770, in intravenous (2 and 4 mg/kg) and intraduodenal (12.5 and 25 mg/kg) administrations, dose-dependently abolished the rhythmic bladder contractions in anesthetized rats. The activity of HY-770, in intravenous administration (i.v.), was almost equal to those of flavoxate, terodiline and oxybutynin; and the activity of HY-770, like terodiline, was more potent than that of flavoxate in intraduodenal administration (i.d.). 2) In the cystometrograms, HY-770 (3, 4 or 8 mg/kg, i.v.) dose-dependently increased the time to micturition (capacity of bladder) without decreasing the amplitude of micturition contraction in anesthetized rats, dogs and cats, and HY-770 (25 mg/kg, i.d.) also increased the capacity in anesthetized cats. 3) HY-770 (4 and 8 mg/kg, i.v.) dose-dependently increased the capacity of the bladder in the cystometrograms of pollakiuria induced by either transection of both the hypogastric nerves or chronic cannulation to the bladder in anesthetized or conscious rats, respectively. 4) HY-770 (25 mg/kg, i.d.) slightly decreased the urethral pressure in anesthetized dogs. These results suggest that HY-770 is a promising drug for the treatment of pollakiuria induced by a neurogenic bladder or unstable bladder, etc.
将HY - 770对大鼠、犬和猫排尿反射以及犬尿道压力的影响与盐酸黄酮哌酯（黄酮哌酯）、盐酸特罗地林（特罗地林）和盐酸奥昔布宁（奥昔布宁）进行了比较。1）静脉注射（2和4mg/kg）和十二指肠内给药（12.5和25mg/kg）时，HY - 770剂量依赖性地消除了麻醉大鼠的膀胱节律性收缩。静脉注射（i.v.）时HY - 770的活性几乎与黄酮哌酯、特罗地林和奥昔布宁相当；十二指肠内给药（i.d.）时，HY - 770的活性与特罗地林一样，比黄酮哌酯更强。2）在膀胱内压描记图中，静脉注射HY - 770（3、4或8mg/kg）剂量依赖性地增加了麻醉大鼠、犬和猫的排尿时间（膀胱容量），且不降低排尿收缩幅度，十二指肠内注射HY - 770（25mg/kg）也增加了麻醉猫的膀胱容量。3）静脉注射HY - 770（4和8mg/kg）剂量依赖性地增加了分别通过切断双侧腹下神经或慢性膀胱插管诱导的尿频麻醉或清醒大鼠膀胱内压描记图中的膀胱容量。4）十二指肠内注射HY - 770（25mg/kg）使麻醉犬的尿道压力略有降低。这些结果表明，HY - 770是治疗神经源性膀胱或不稳定膀胱等引起的尿频的一种有前景的药物。
