Uckert S, Stief C G, Odenthal K P, Becker A J, Truss M C, Jonas U
Hannover Medical School, Department of Urology, Germany.
Arzneimittelforschung. 1998 Aug;48(8):836-9.
The spasmolytic activity of flavoxate (CAS 15301-69-6), anticholinergic agents oxybutynin (CAS 5633-20-5), and trospium chloride (CAS 10405-02-4), drugs commonly utilized in the therapy of hyperactive bladder, and phosphodiesterase (PDE) inhibitors papaverine (CAS 58-74-2) and vinpocetine (CAS 42971-09-5) on muscarinic contractions of detrusor smooth muscle strips isolated from human and porcine urinary bladder was studied in vitro using the organ bath technique. Trospium chloride was most effective in relaxing contractions elicited by muscarinic stimulation, while flavoxate was significantly less effective than all other drugs tested. The relaxing potency of oxybutynin was greater than those of PDE-inhibitors papaverine and vinpocetine but 3,000 fold less significant than those of trospium chloride. The effects of the individual drugs on muscarinic tension of both human and porcine detrusor muscle strips were nearly equal. The present results suggest that the pig might be an appropriate animal model for the study of effects of spasmolytic substances on the contractility of urinary bladder smooth muscle in vitro.
采用器官浴技术,在体外研究了黄酮哌酯(CAS 15301-69-6)、抗胆碱能药物奥昔布宁(CAS 5633-20-5)和曲司氯铵(CAS 10405-02-4)(常用于治疗膀胱过度活动症的药物)以及磷酸二酯酶(PDE)抑制剂罂粟碱(CAS 58-74-2)和长春西汀(CAS 42971-09-5)对从人和猪膀胱分离的逼尿肌平滑肌条毒蕈碱收缩的影响。曲司氯铵在松弛毒蕈碱刺激引起的收缩方面最有效,而黄酮哌酯的效果明显低于所有其他测试药物。奥昔布宁的松弛效力大于PDE抑制剂罂粟碱和长春西汀,但比曲司氯铵低3000倍。各药物对人和猪逼尿肌条毒蕈碱张力的影响几乎相同。目前的结果表明,猪可能是体外研究解痉物质对膀胱平滑肌收缩性影响的合适动物模型。