陈琦, 王晓良. 硝苯地平及克罗卡因对离体大鼠膀胱和主动脉平滑肌的影响J. 药学学报, 1997, 32(10): 740-743.
引用本文: 陈琦, 王晓良. 硝苯地平及克罗卡因对离体大鼠膀胱和主动脉平滑肌的影响J. 药学学报, 1997, 32(10): 740-743.
Q Chen, XL Wang. EFFECTS OF NIFEDIPINE AND CROMAKALIM ON ISOLATED RAT BLADDER TISSUE AND AORTA STRIPJ. Acta Pharmaceutica Sinica, 1997, 32(10): 740-743.
Citation: Q Chen, XL Wang. EFFECTS OF NIFEDIPINE AND CROMAKALIM ON ISOLATED RAT BLADDER TISSUE AND AORTA STRIPJ. Acta Pharmaceutica Sinica, 1997, 32(10): 740-743.

硝苯地平及克罗卡因对离体大鼠膀胱和主动脉平滑肌的影响

EFFECTS OF NIFEDIPINE AND CROMAKALIM ON ISOLATED RAT BLADDER TISSUE AND AORTA STRIP

  • 摘要: 用体外大鼠胸主动脉条和膀胱条的制备,比较了钙拮抗剂硝苯地平(nifedipine)和钾通道开放剂克罗卡因(cromakalin)对受体激活和KCl引起的平滑肌收缩的作用。结果表明,对NE引起的大鼠主动脉收缩,nifedipine的抑制作用明显强于cromakalim;而用氨甲酰胆碱(carbachol)激动胆碱能M受体引起大鼠膀胱环形肌和纵形肌收缩时,两者的抑制作用无明显差异。由KCl 27.5mmol·L-1去极化引起收缩时,nifedipine对大鼠膀胱环形肌、纵形肌及血管这3种组织的舒张作用均明显比cromakalim强。提示:在由受体介导的收缩中,cromakalim对膀胱组织的舒张作用较强,而nifedipine对血管平滑肌则作用更强;但在由KCl去极化引起的收缩中,nifedipine对血管和膀胱这两种组织的抑制作用较强。

     

    Abstract: Relaxing effects of nifedipine and cromakalim on rat aorta strip, bladder ring and bladder strip were compared on receptor and KCl mediated contraction. The IC50 of nifedipine to inhibit NE induced contraction (by stimulation of α1-adrenoceptor in aorta strip) was found to be 2.76±0.79 nmol·L-1. For the same action the IC50 of cromakalim (a potassium channel opener) was 48±25 nmol·L-1. However, to inhibit 27.5 mmol·L-1 KCl induced contraction, the IC50 for nifedipine and cromakalim were 1.83±1.3 nmol·L-1 and 64±19 nmol·L-1, respectively. On bladder ring, to inhibit carbachol mediated contraction (by cholinergic M-receptor stimulation), the IC50 for nifedipine and cromakalim were found to be 15±13 nmol·L-1 and 13±80 nmol·L-1, respectively. To inhibit KCl induced contraction, the IC50s were 2.05±1.26 nmol·L-1 and 38±26 nmol·L-1. On bladder strip, nifedipine and cromakalim antagonized carbachol mediated contraction with IC50s of 12±12 nmol·L-1 and 32.0±2.4 nmol·L-1. Both compounds reduced the contraction force mediated by KCl with IC50 of 1.57±0.7 nmol·L-1 and 71±25 nmol·L-1, respectively.Our study showed that cromakalim was better to relax receptor mediated contraction of bladder ring. While, nifedipine was more potent to antagonize NE induced aorta strip contraction. Nifedipine also showed greater effect on KCl induced responses in all three tissue preperations.

     

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