Ross S B, Kelder D
Naunyn Schmiedebergs Arch Pharmacol. 1976 Dec;295(3):183-9. doi: 10.1007/BF00505085.
The effect of the depolarizing agent veratridine on the accumulation and release of of 3H-noradrenaline and 3H-bretylium in in the rat vas deferens in vitro was examined. Veratridine produced inhibition of the accumulation and induced marked release of the amines. In vas deferens from non-reserpinized rats the release of noradrenaline evoked by veratridine was partially antagonized by omission of Ca2+ in the incubation medium and partially inhibited by low concentrations of desipramine. In reserpinized vas deferens the release of noradrenaline like that of bretylium in normal vas was not affected by omission of Ca2+ but inhibited by low concentrations (3-5 X 10(-7) M) of desipramine. Tetrodotoxin and the local anesthetics millicaine and lidocaine antagonized the effect of veratridine on the accumulation and release of the amines, probably due to prevention of the depolarization. High concentration (3 X 10(-5) M) of desipramine had a similar effect on the release of noradrenaline in normal tissue in presence of external Ca2+. It is concluded that noradrenaline is released by veratridine from normal vas deferens by two mechanisms: 1) an exocytosis release, 2) a carrier mediated desipramine sensitive outward transport; In reserpinized tissue the second mechanism is solely responsible for the release of noradrenaline. Bretylium is only released by the second mechanism. It is suggested that the inhibiton of the amine accumulation by veratridine is due to an equilibrium of the influx at a low tissue to medium ratio.
研究了去极化剂藜芦定对大鼠离体输精管中3H-去甲肾上腺素和3H-溴苄铵积累和释放的影响。藜芦定抑制胺类的积累并诱导其显著释放。在未用利血平处理的大鼠输精管中,藜芦定诱发的去甲肾上腺素释放部分被孵育介质中Ca2+的缺失所拮抗,部分被低浓度的地昔帕明所抑制。在利血平处理的输精管中,去甲肾上腺素的释放与正常输精管中溴苄铵的释放一样,不受Ca2+缺失的影响,但被低浓度(3 - 5×10(-7)M)的地昔帕明所抑制。河豚毒素以及局部麻醉剂丙胺卡因和利多卡因拮抗藜芦定对胺类积累和释放的影响,这可能是由于阻止了去极化。高浓度(3×10(-5)M)的地昔帕明在有细胞外Ca2+存在时对正常组织中去甲肾上腺素的释放有类似作用。得出的结论是,藜芦定从正常输精管中释放去甲肾上腺素通过两种机制:1)胞吐释放,2)载体介导的对地昔帕明敏感的外向转运;在利血平处理的组织中,第二种机制单独负责去甲肾上腺素的释放。溴苄铵仅通过第二种机制释放。有人提出,藜芦定对胺类积累的抑制是由于在低组织与介质比例下流入的平衡。