Hughes A D, Schachter M
Department of Clinical Pharmacology, St Mary's Hospital Medical School, Imperial College of Science Technology and Medicine, London, UK.
Cell Calcium. 1994 Apr;15(4):317-30. doi: 10.1016/0143-4160(94)90071-x.
The influx of calcium in response to vasopressin receptor stimulation is an important component of excitation-contraction coupling. We have examined the routes by which Ca2+ and other divalent cations enter vascular smooth muscle cells using a cultured vascular smooth muscle cell line (A7r5). Confluent A7r5 cells were loaded with Fura-2 to permit measurement of intracellular divalent cation concentration (Ca2+, Ba2+, Mn2+). Combinations of excitation wavelengths (340/380, 340/356, 356/380 and 340/370) were used depending on the divalent cation being studied. Emission was measured at 510 nm for all studies. Ca2+, Ba2+ and Mn2+ permeated unstimulated A7r5 cells. Vasopressin increased intracellular Ca2+ in cells both in the presence and absence of extracellular Ca2+, although responses in the absence of extracellular Ca2+ were smaller and had no sustained component. Amlodipine, a voltage-dependent calcium channel blocker, had no effect on Ca2+ entry, but Ni2+ did block Ca2+ influx. Vasopressin-induced elevations of intracellular Ca2+ in Ca(2+)-free physiological saline were abolished by ionomycin and thapsigargin. In the presence of extracellular Ba2+ vasopressin increased intracellular Ca2+ transiently and caused a small sustained increase in intracellular Ba2+ concentration. Ionomycin and thapsigargin increased intracellular Ca2+ but had no effect on Ba2+ influx. In contrast vasopressin, ionomycin and thapsigargin had no effect on Mn2+ influx. Econazole and SKF 96365, imidazoles reported to be blockers of receptor-induced cation entry, increased intracellular Ca2+ by releasing intracellular Ca2+ from a different site to that mobilized by vasopressin or thapsigargin in A7r5 cells. Econazole and SKF 96365 partially inhibited passive influx of Ca2+ and Ba2+ but did not inhibit passive influx of Mn2+, or vasopressin-induced influx of Ba2+. U73122, a putative inhibitor of phospholipase C partially inhibited passive entry of Ca2+ but not passive entry of Mn2+ and Ba2+. U73122 also inhibited vasopressin-induced release of intracellular Ca2+ and agonist-induced Ca2+ influx but did not block vasopressin-induced Ba2+ influx. Divalent cations enter A7r5 cells by a number of routes - 'passive' pathway(s) that admit Ca2+, Ba2+ and Mn2+ and receptor-operated pathway(s) that are permeable to Ca2+, Ba2+ but not Mn2+. On the basis of ionic permeabilities and the effect of various blocking agents, there appear to be two distinct passive influx routes. One is permeable to Ca2+ and Ba2+ and is blocked by econazole or SKF 96365. The other is permeable to Mn2+ and is blocked by Ni2+. There also appear to be two different routes of divalent cation entry involved in responses to receptor activation.(ABSTRACT TRUNCATED AT 400 WORDS)
血管加压素受体受刺激时钙的内流是兴奋 - 收缩偶联的重要组成部分。我们使用培养的血管平滑肌细胞系(A7r5)研究了Ca2+和其他二价阳离子进入血管平滑肌细胞的途径。使汇合的A7r5细胞加载Fura - 2以测量细胞内二价阳离子浓度(Ca2+、Ba2+、Mn2+)。根据所研究的二价阳离子,使用不同的激发波长组合(340/380、340/356、356/380和340/370)。所有研究均在510 nm处测量发射光。Ca2+、Ba2+和Mn2+可透过未受刺激的A7r5细胞。无论有无细胞外Ca2+存在,血管加压素均能增加细胞内Ca2+,尽管在无细胞外Ca2+时反应较小且无持续成分。氨氯地平,一种电压依赖性钙通道阻滞剂,对Ca2+内流无影响,但Ni2+确实能阻断Ca2+内流。在无Ca2+的生理盐水中,血管加压素诱导的细胞内Ca2+升高被离子霉素和毒胡萝卜素消除。在有细胞外Ba2+存在时,血管加压素使细胞内Ca2+短暂升高,并使细胞内Ba2+浓度有小幅度的持续升高。离子霉素和毒胡萝卜素增加细胞内Ca2+,但对Ba2+内流无影响。相反,血管加压素、离子霉素和毒胡萝卜素对Mn2+内流无影响。酮康唑和SKF 96365,据报道是受体诱导阳离子内流的阻滞剂,通过从与血管加压素或毒胡萝卜素在A7r5细胞中动员的位点不同的位点释放细胞内Ca2+来增加细胞内Ca2+。酮康唑和SKF 96365部分抑制Ca2+和Ba2+的被动内流,但不抑制Mn2+的被动内流或血管加压素诱导的Ba2+内流。U73122,一种推测的磷脂酶C抑制剂,部分抑制Ca2+的被动内流,但不抑制Mn2+和Ba2+的被动内流。U73122还抑制血管加压素诱导的细胞内Ca2+释放和激动剂诱导的Ca2+内流,但不阻断血管加压素诱导的Ba2+内流。二价阳离子通过多种途径进入A7r5细胞——允许Ca2+、Ba2+和Mn2+通过的“被动”途径以及对Ca2+、Ba2+可通透但对Mn2+不可通透的受体操纵途径。基于离子通透性和各种阻滞剂的作用效果,似乎存在两种不同的被动内流途径。一种对Ca2+和Ba2+可通透,并被酮康唑或SKF 96365阻断。另一种对Mn2+可通透,并被Ni2+阻断。在对受体激活的反应中,似乎也存在两种不同的二价阳离子进入途径。(摘要截选至400字)