Huddart H, Langton P D, Saad K H
J Physiol. 1984 Apr;349:183-94. doi: 10.1113/jphysiol.1984.sp015151.
Papaverine, up to 150 micron, was without effect on resting tension of vas deferens and urinary bladder smooth muscle strips, but caused a dose-dependent inhibition of the phasic component of the 100 mM-K contracture. At 150 micron, papaverine caused an 80 and 60% inhibition of phasic tension in vas deferens and urinary bladder muscle respectively. Papaverine caused a marked dose-dependent reduction in the tonic component of 100 mM-K contractures in both preparations. At 150 micron, papaverine often relaxed preparations below initial starting tension. Addition of 150 micron-papaverine to incubation media caused a fall of 25-30% in 45Ca uptake by both preparations. Papaverine at 150 micron caused a small fall in resting 45Ca efflux from vas deferens and a larger fall in efflux from bladder muscle. However, this papaverine concentration caused a large inhibition of the 45Ca uptake by and 45Ca efflux from both preparations when stimulated by high-K depolarization. Papaverine at 150 micron was without significant effect on Ca binding by either microsomes or mitochondria isolated from both vas deferens and urinary bladder smooth muscle. The main site of papaverine action appears to be on the Ca-influx mechanism responsible for regulating Ca entry during prolonged K depolarization.
高达150微摩尔的罂粟碱对输精管和膀胱平滑肌条的静息张力没有影响,但对100毫摩尔钾引起的挛缩的相性成分产生剂量依赖性抑制。在150微摩尔时,罂粟碱分别使输精管和膀胱肌的相性张力抑制80%和60%。罂粟碱使两种制剂中100毫摩尔钾挛缩的强直性成分显著降低,呈剂量依赖性。在150微摩尔时,罂粟碱常常使制剂松弛至初始起始张力以下。向孵育介质中加入150微摩尔罂粟碱会使两种制剂的45钙摄取量下降25 - 30%。150微摩尔的罂粟碱使输精管的静息45钙外流略有下降,使膀胱肌的外流下降幅度更大。然而,当受到高钾去极化刺激时,这种罂粟碱浓度会对两种制剂的45钙摄取和45钙外流产生很大抑制。150微摩尔的罂粟碱对从输精管和膀胱平滑肌分离的微粒体或线粒体的钙结合没有显著影响。罂粟碱的主要作用部位似乎是在负责在长时间钾去极化期间调节钙内流的钙内流机制上。