他克林对心脏乙酰胆碱释放的影响。
The effect of tacrine on acetylcholine overflow in the heart.
作者信息
Lindmar R, Löffelholz K
机构信息
Department of Pharmacology, University of Mainz, F.R.G.
出版信息
Eur J Pharmacol. 1990 Nov 6;190(1-2):251-4. doi: 10.1016/0014-2999(90)94134-j.
Tacrine, 10(-6) M, enhanced the acetylcholine (ACh) overflow evoked in perfused chicken hearts by field stimulation (5 Hz, 1 min) from 183 to 346 pmol g-1 min-1. Increase to the same level were observed after pretreatment with diisopropylfluorophosphate (DFP) as well as after DFP plus 10(-6) M tacrine. Tacrine, 10(-5) M, caused further enhancement with or without DFP up to 851 pmol g-1 min-1. It was concluded that 10(-6) M tacrine enhanced the ACh overflow by choline esterase inhibition, whereas 10(-5) M tacrine caused, in addition, an increase of neuronal ACh release.
10⁻⁶ M的他克林可使灌注鸡心在5 Hz场刺激（持续1分钟）诱发的乙酰胆碱（ACh）溢出量从183皮摩尔/克·分钟增加到346皮摩尔/克·分钟。在用二异丙基氟磷酸酯（DFP）预处理后以及DFP加10⁻⁶ M他克林处理后，观察到ACh溢出量增加到相同水平。10⁻⁵ M的他克林无论有无DFP存在，均可使ACh溢出量进一步增加，最高可达851皮摩尔/克·分钟。由此得出结论，10⁻⁶ M他克林通过抑制胆碱酯酶增强ACh溢出，而10⁻⁵ M他克林除此之外还可增加神经元ACh释放。
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