Possible mechanisms related to contraction of the bovine iris sphincter in the presence of acetylcholine and carbachol

Using tension-recording methods, we compared the effects of acetylcholine (Ach) and carbachol on the bovine iris sphincter. The isolated muscle strips were mounted in a 0.2 ml organ bath, through which Krebs solution at 36 °C flowed continuously. There was a tenthousandfold difference in potency between carbachol and Ach in this tissue. Neostigmine or eserine, acetylcholinesterase (AchE) inhibitors, produced a larger contraction of the muscle than did Ach. Ach-induced contractions were potentiated by low doses of anti-AchEs and were inhibited by atropine.This in vitro study suggests that Ach and/or endogenous chemical agents may be spontaneously released from tissues and that AchE activities in this tissue strongly inhibit or mask the Ach action, probably in order to protect the nerve terminals from released Ach.     

PRENATAL DIAGNOSIS Ⅰ. EARLY DIAGNOSIS OF OPEN NEURAL TUBE DEFECTS BY QUALITATIVE ACETYLCHOLINESTERASE ISOENZYME IN AMNIOTIC FLUID

The measurement of amniotic fluid (AF) acetylcholinesterase isoenzyme (AChEI) is a relatively new method for early diagnosis of open neural tube defects (NTDs). As quantitative methods are of unproven reliability at present, the authors used a high resolving power qualitative method-vertical slab polyaerylamide gel electrophoresis. The benefits of this technique are: simplicity of operation, accuracy, unsophisticated equipment, and easily available reagents. Combined results of 9 NTDs studies revealed that samples from early pregnancy gave more accurate results than those from late pregnancy.     

角膜损伤后神经再生的实验研究

应用神经组织化学技术观察了兔角膜NA能神经及AchE阳性神经在角膜损伤后的再生,证实术后1月,两种神经均有再生轴突进入植片;术后3月可见交界区和植床内神经密度明显增加;同时,对术后两种神经再生的功能意义进行了讨论。     

肟类药物对塔崩等神经性毒剂抑制的大鼠脑AChE的体外重活化作用

系统地研究了肟类药物对塔崩抑制的大鼠脑AChE的体外重活化作用,并与梭曼、沙林和VX进行了比较。结果表明,沙林和VX抑制的AChE较易被药物重活化,而塔崩和梭曼抑制的AChE则较难。37℃、pH7.2条件下,塔崩抑制的大鼠脑AChE可浓度依赖性地被TMB_r和LuH_6重活化,2-PAM在高浓度下也有一定作用,但HI-6在所用3个浓度下均无重活化。通过降低抑制温度成功地建立了未老化的梭曼膦酰化AChE模型。药物试验表明,未老化的梭曼膦酰化大鼠脑AChE可被高浓度(1mmol/L)HI-6重活化,而不被2-PAM、TMB_4及LuH_6重活化。提示药物自身内在活性在重活化作用中的重要性。TMB_4和LuH_6对塔崩磷酸化AChE有较强重活化,而对未老化梭曼膦酸化AChE无重活化,HI-6则相反,对未老化梭曼膦酰化AChE重活化效果好,而对塔崩磷酰化AChE无重活化作用。塔崩和梭曼膦酰化AChE在未老化以前对药物的响应就有所不同,毒剂残基的空间效应可能起重要作用。     

Vaccination against gastrointestinal nematodes of sheep using purified secretory acetylcholinesterase from Trichostrongylus colubriformis– an initial pilot study

Purified secretory acetylcholinesterase (sAChE) from Trichostrongylus colubriformis was used as a candidate vaccine against mixed T. colubriformis, Haemonchus contortus and C. oncophora challenge infections of sheep. Cross species protection was achieved with an average reduction in worm burden of all species of 31%, rising to 58% in individual cases. There was no consistent reduction in faecal egg counts and increases in anti-T. colubriformis sAChE IgG antibody levels following vaccination were modest. We suggest that improved antigen delivery systems will result in increased host protection.     

Postsynaptic potentiation of end-plate currents in the rat diaphragm during variation in synaptic acetylcholinesterase activity

Leningrad University. (Presented by Academician of the Academy of Medical Sciences of the USSR S. N. Golikov.) Translated from Byulleten' Éksperimental'noi Biologii i Meditsiny, Vol. 111, No. 5, pp. 458–460, May, 1991.     

Indirect detection of anti-acetylcholinesterase compounds in microcolumn liquid chromatography using packed bed reactor with immobilized human red blood cell acetylcholinesterase and choline oxidase

The inhibiting compounds were separated by micro-column liquid chromatography in the mobile phase containing the natural substrate acetylcholine. A home-made packed bed microbioreactor system containing immobilized enzyme acetylcholinesterase (ACHE) in human red blood cell membrane and choline oxidase (CHO) from alcaligenes was used for the post-column conversion of acetylcholine to hydrogen peroxide which was detected by an electrochemical detector. The inhibition effect of the solutes caused a decrease in the acetylcholinesterase activity, a decrease in the formation of hydrogen peroxide and also a decrease in the response corresponding to the concentration of the solutes. The rate of the enzyme regeneration was also recorded. The micro-system was compared with a conventional LC system comprising commercially prepared enzyme reactor. The stability of the enzymes is at least 3 weeks at ambient temperature. The limit of detection depends on biological activity of inhibition and for galanthamine was 1 pmol.     

人胎胸腺乙酰胆碱酯酶阳性反应细胞的形态观察

应用乙酰胆碱酯酶组织化学方法在光镜下观察了５￣６个月胎儿胸腺实质中乙酰胆碱酯酶阳性反应细胞的分布及形态结构。结果表明：乙酰胆碱酯酶阳性反应细胞主要分布于胸腺的髓质中，这些细胞可能是淋巴细胞，上皮性网状细胞及上皮性网状细胞－淋巴细胞复合体。就此种细胞的功能进行了讨论。     

Ache、P-selectin、CDK5在病毒性脑炎中的表达及相关性研究

目的 探究乙酰胆碱酯酶(acetylcholinesterase, Ache)、P-选择素(P-selectin)、细胞周期素依赖蛋白激酶5(cyclin-dependent kinase 5,CDK5)在病毒性脑炎(viral encephalitis, VE)中的表达及相关性。方法 本研究选取在本院健康体检及神经内科就诊治疗、住院治疗的病毒性脑炎患者130例作为研究对象,并纳入研究组,根据患者的病情时间将其分为急性期和恢复期,其中急性期组85例,恢复期组45例。根据患者的临床表现,将其分为轻度组和重度组,其中轻度组76例,重度组54例,选择同期在我院接受体检的健康患者60例作为对照组。应用丁酰硫代胆碱底物法检测Ache水平;酶联免疫吸附法检测血清P-selectin水平;CDK5分离试剂盒检测CDK5水平。观察研究组和对照组、急性期和恢复期及重度组和轻度组患者Ache、P-selectin、CDK5水平,分析病毒性脑炎患者Ache、P-selectin和CDK5之间相关性,利用ROC曲线比较Ache、P-selectin、CDK5单独检测及联合检测在VE中的诊断价值。结果 研究组A...     

A Comparison of the Cholinergic Activity of Selected H2-Antagonists and Sulfoxide Metabolites

Famotidine and selected H₂-antagonists were evaluated with respect to toxicity and selected pharmacological activities. When administered intraperitoneally to mice at a dose equivalent to 10 times their respective H₂-antagonist ED₅₀ values, no deaths were observed. Similarly, no alteration in brain ACh concentrations or overt pharmacological effects were noted. However, at 400 mg/kg, ranitidine produced 89% lethality, followed by cimetidine (11%) and famotidine. Only cimetidine and famotidine at this dose significantly elevated brain acetylcholine levels. These results do not correlate with the in vitro data, where ORF-17578 and ranitidine were the most potent entities with respect to acetylcholinesterase inhibition (1–2 × 10^–6 M), followed by nizatidine > cimetidine > famotidine. The sulfoxide metabolites of ranitidine and cimetidine were approximately one-tenth as potent as their parent compounds with respect to inhibition of acetylcholinesterase. Direct muscarinic stimulation or potentiation of acetylcholine-induced contraction in ileal tissue was not observed for any of the H₂-antagonists.