Webb R A
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1985;80(2):305-12. doi: 10.1016/0742-8413(85)90061-1.
The in vitro uptake of [3H]5HT was investigated in tissue slices of the cestode Hymenolepis diminuta. A concentrative, sodium sensitive, high affinity uptake mechanism (Km 1.43 X 10(-6) M; Vmax 222 fmoles/mg wet wt/min), together with a sodium insensitive component (linear up to 5 X 10(-6) M) were present. In the presence of 2-nitroimipramine the sodium sensitive component was significantly suppressed (Vmax 33 fmoles/mg/wet wt/min) although the Km (1.37 X 10(-6) M) was not affected. Nitroimipramine showed an IC50 of approximately 2 X 10(-6) M. The sodium insensitive component was not affected by nitroimipramine. Biogenic amines and related indoleamines were weak inhibitors of the sodium sensitive and sodium insensitive components of 5HT uptake. The tricyclic antidepressants and fluoxetine were effective inhibitors of the sodium sensitive component of 5-HT uptake; receptor ligands were weak inhibitors or without effect. The metabolism of [3H]5HT in tissue slices of H. diminuta was examined by HPLC. The role of the sodium sensitive uptake and metabolism of 5HT in terms of inactivation and recycling of neurally released 5HT and the possible importance of exogenous recruitment of 5HT are discussed.
在微小膜壳绦虫的组织切片中研究了[3H]5-羟色胺(5HT)的体外摄取情况。存在一种浓缩的、对钠敏感的高亲和力摄取机制(米氏常数Km为1.43×10⁻⁶ M;最大反应速度Vmax为222飞摩尔/毫克湿重/分钟),以及一个对钠不敏感的成分(在高达5×10⁻⁶ M时呈线性)。在2-硝基丙咪嗪存在的情况下,对钠敏感的成分受到显著抑制(Vmax为33飞摩尔/毫克/湿重/分钟),尽管Km(1.37×10⁻⁶ M)未受影响。硝基丙咪嗪的半数抑制浓度(IC50)约为2×10⁻⁶ M。对钠不敏感的成分不受硝基丙咪嗪影响。生物胺和相关吲哚胺是5HT摄取的对钠敏感和对钠不敏感成分的弱抑制剂。三环类抗抑郁药和氟西汀是5-羟色胺摄取的对钠敏感成分的有效抑制剂;受体配体是弱抑制剂或无作用。通过高效液相色谱法(HPLC)检测了微小膜壳绦虫组织切片中[3H]5HT的代谢情况。讨论了5HT的对钠敏感摄取和代谢在神经释放的5HT的失活和再循环方面的作用,以及外源性补充5HT的可能重要性。