Karlén B, Lundgren G, Lundin J, Holmstedt B
Naunyn Schmiedebergs Arch Pharmacol. 1979 Jul;308(1):61-5. doi: 10.1007/BF00499720.
The effect of physostigmine salicylate (0.5 mg/kg, i.p.) alone and in combination with atropine sulfate (25 mg/kg, i.p.) on levels of acetylcholine (ACh) and choline (Ch) and turnover of ACh has been studied in whole brain and striatum of mice. The animals were killed by focussed microwave irradiation and the turnover of ACh was studied after i.v. injection of deuterium labelled Ch by employing mass fragmentography. Physostigmine increased the levels of ACh in whole brain from 24.5--28.0 nmol/g(P less than 0.001) whereas there was no significant increase in striatum. The levels of Ch were also increased. The turnover rate of ACh was decreased in whole brain from 15.4 to 8.4 and in striatum from 52.9 to 24.4 nmol/g . min. Physostigmine given before or after atropine did not completely block the ACh lowering effect of atropine. When atropine was given before physostigmine the turnover rate of ACh in whole brain was increased to 24.2 nmoles/g . min. The results seem to indicate that there is no clear cut relation between the turnover rate and level of ACh in vivo. The increase of the turnover rate induced by atropine is masked unless a cholinesterase inhibitor is given to protect the newly synthesized labelled ACh released by atropine.
已研究了水杨酸毒扁豆碱（0.5毫克/千克，腹腔注射）单独使用及与硫酸阿托品（25毫克/千克，腹腔注射）联合使用对小鼠全脑和纹状体中乙酰胆碱（ACh）和胆碱（Ch）水平以及ACh周转的影响。通过聚焦微波辐射处死动物，并在静脉注射氘标记的Ch后采用质量碎片分析法研究ACh的周转。毒扁豆碱使全脑中ACh水平从24.5 - 28.0纳摩尔/克增加（P小于0.001），而纹状体中无显著增加。Ch水平也升高。全脑中ACh的周转率从15.4降至8.4，纹状体中从52.9降至24.4纳摩尔/克·分钟。在阿托品之前或之后给予毒扁豆碱并未完全阻断阿托品降低ACh的作用。当在毒扁豆碱之前给予阿托品时，全脑中ACh的周转率增加至24.2纳摩尔/克·分钟。结果似乎表明体内ACh的周转率与水平之间没有明确的关系。除非给予胆碱酯酶抑制剂以保护由阿托品释放的新合成的标记ACh，否则阿托品诱导的周转率增加会被掩盖。
