东莨菪碱诱发染色体畸变的剂量效应

东茛菪碱五个剂量(1、2、5、10、20μg/ml作用于12名健康成人外周血淋巴细胞培养液诱发染色体畸变,并设空白对照组(生理盐水)。染色体畸变率分别为3.±0.5,9.6±1.1,11.7±1.1,13.6±2.3,18.0±3.0和17.5±2.0％;细胞畸变率为3.1±0.6,9.2±0.6,10.0±0.8,10.8±1.5,11.6±1.8和12.2±14.％。各剂量组与对照组比较差异高度显著(P<0.01)。方差分析,各剂量组间变异的差异高度显著(P<0.01)。相关系数和回归系数也非常显著(P<0.01)。结果表明,东莨菪碱剂量与染色体畸变率和细胞畸变率有线性关系。     

山莨菪碱治疗麻醉剂依赖性

阿片成瘾者２５０例（男性２２２例，女性２８例，年龄３０±ｓ５ａ）应用山莨菪碱０．５－２ｍｇ／（ｋｇ·ｄ），分２－３次加入１０％葡萄糖２５０ｍＬ或５％葡萄糖生理盐水５００ｍＬ静脉滴注；东莨菪碱０．０２－０．０３ｍｇ／ｋｇ加入１０％葡萄糖２５０ｍＬ静脉滴注１次，必要时对重患者追加１次，疗程５－７ｄ。结果戒断症状均有改善（Ｐ＜０．０１），２７例需加用羟丁酸钠。不良反应轻，可作为阿片瘾者的脱瘾药物。＊Ｐ＜０．０１。碱确能解除阿片药物戒断症状。其对阿片戒断症状缓解时间在治疗４－５ｄ后，强烈觅药渴求也随之逐渐消失。１５０例（６０％）要求进食，１７５例（７０％）仍需借助安眠药睡眠。另６５例（２６％）戒断症状阵发性发作，每次持续０．５－１ｈ，症状轻重不一，轻者流泪、全身弥漫性疼痛，重者焦躁不安、心中猫抓虫咬样难受，甚至想自残，可配合艾司唑仑３－４ｍｇ／ｄ，ｐｏ或氯硝西泮６－１０ｍｇ／ｄ，ｐｏ；也可用氯硝西泮１－２ｍｇ／次，ｉｍ，每日２－３次；针刺胃俞、脾俞、中脘、足三里、印堂、太阳、百会、内关、合谷、命门、夹脊和肾俞穴位，根据临床症状任选其中３－５个穴位进行治疗或心理治疗能快速减轻患者戒断症状。治程中２７例（１０．８％）重?     

Effects of low-dose transdermal scopolamine on autonomic cardiovascular control in healthy young subjects

We studied how posture influences the effects of transdermal scopolamine on autonomic cardiovascular regulation in a randomized, double-blind, placebo-controlled crossover study of 10 healthy young volunteers. We recorded the electrocardiogram and auscultatory sphygmomanometric and continuous non-invasive finger arterial pressure (Finapres device) to obtain signals for the beat-by-beat R–R interval and systolic, mean and diastolic pressures. R–R interval and arterial pressure variabilities were characterized by power spectral analysis. Scopolamine increased the mean R–R intervals and reduced arterial pressure in both the supine and the standing positions, but did not affect blood pressure variability. Scopolamine increased the total variability of R–R interval and its mid- (0·07–0·15 Hz) and high- (0·15–0·40 Hz) frequency band power in the standing position during controlled breathing at 0·25 Hz. In the supine position, scopolamine did not affect R–R interval variability. In the deep breathing test, scopolamine increased the maximal expiratory–inspiratory R–R interval ratio. This study showed that low-dose scopolamine increases vagal cardiac inhibition in both supine and standing positions in healthy volunteers. However, scopolamine increases heart rate variability only in the standing position during partial vagal withdrawal. The study also demonstrates that transdermal scopolamine decreases blood pressure in healthy young subjects.     

Cholinergic and dopaminergic agents which inhibit a passive avoidance response attenuate the paradigm-specific increases in NCAM sialylation state

Summary The influence of cholinergic and dopaminergic agents on the acquisition of a passive avoidance response in the rat is demonstrated. Trifluoperazine (0.12 mg/kg), a dopamine antagonist, inhibited task acquisition when present during training or later, during consolidation, at the 10–12 h posttraining period and at no other intervening time point. Induction of amnesia was dose-dependent and was not apparent when the dose exceeded 0.12 mg/ kg. This effect appears to be due to an increase in dopamine release through presynaptic receptor antagonism as similar results could be obtained by the administration of apomorphine (0.5 mg/kg), a dopamine agonist, and this effect could be antagonized by the D 1 receptor selective antagonist SCH-23390. Scopolamine (0.15 mg/kg), a muscarinic antagonist, impaired acquisition of the passive avoidance response when administered during training and, separately, at the 6 h post-training period. This could not be attributed to presynaptic antagonism as oxotremorine (0.2 mg/kg), a muscarinic agonist, had no amnesic action. Administration of apomorphine or scopolamine during training and at the appropriate post-training period prevented subsequent paradigm-specific increases of neural cell adhesion molecule sialylation state in hippocampal immunoprecipitates obtained at 24 h after task acquisition and 4 h following intraventricular infusion of the labelled sialic acid precursor — N-acetyl-D-mannosamine. Oxotremorine alone did not influence neural cell adhesion molecule sialylation state. These observations provide further evidence of a regulatory role for neural cell adhesion molecule sialylation state in information storage processes.Abbreviations NCAM neural cell adhesion molecule - RSA relative specific activity - SDS-PAGE sodium dodecyl sulphate polyacrylamide gel electrophoresis - TCA trichloroacetic acid - TFP trifluoperazine     

党参总碱对东莨菪碱引起小鼠记忆障碍和脑内乙酰胆碱及胆碱乙酰化酶的作用

用跳台法观察到党参总碱(DSA)能改善东莨菪碱(Scop)引起的记忆障碍,并能对抗Scop所致小鼠脑内乙酰胆碱(ACh)浓度下降及胆碱乙酰化酶(ChAT)活性的降低。体外实验发现当在反应液中加入DSA后,ChAT生成ACh的量增加。     

Effects of Spascupreel versus hyoscine butylbromide for gastrointestinal cramps in children

BACKGROUND: Gastrointestinal spasms and cramps are common in children as well as in adults. Alternative medical practices such as chiropractice and homeopathy are becoming increasingly popular in Europe and the USA. The effectiveness and tolerability of the homeopathic preparation Spascupreel was compared with that of hyoscine butylbromide treatment in children <12 years of age. METHODS: An observational cohort study in 204 children <12 years was conducted over a 1 week treatment period. The efficacy of the respective therapies were evaluated on the effect on severity of spasms and clinical symptoms (pain/cramps, sleep disturbances, distress, eating or drinking difficulties and frequent crying). Compliance was evaluated on a four-point scale from 'very good' to 'low'. Evaluation was done by the practitioner based on information given by the patient or minder. RESULTS: The analysis showed comparative improvements with the homeopathic preparation and hyoscine butylbromide therapy on severity of spasms, pain/cramps, sleep disturbances, eating or drinking difficulties, and frequent crying, all as evaluated by the practitioner. Both treatments were very well tolerated. CONCLUSIONS: For patients opting for a homeopathic therapy, Spascupreel seems to be an effective and well tolerated alternative to conventional therapies in children suffering from gastrointestinal spasms.     

Differential effects of scopolamine on neuronal survival in ischemia and glutamate neurotoxicity: relationships to the excessive vulnerability of the dorsoseptal hippocampus

The neurodegeneration in the CA1 subfield of hippocampus exhibited a dorsal-ventral gradient of susceptibility in global ischemia (82% dorsoseptally and only 16% ventrotemporally). Scopolamine (SCOP) did not improve the neuronal damage caused by the global ischemic challenge in rats and did not reduce the infarct area after the focal MCA-occlusion in mice. No differences were observed between saline and SCOP-treated animals in the physiologic parameters, except for a slight increase in rectal temperature. In contrast, treatment of hippocampal cultures with increasing concentrations of SCOP (1 nM to 1 mM) under glutamate incubation had a beneficial effect on neuronal viability. These data show that (1) there is substantial gradient of vulnerability of the hippocampus from dorsal to ventral in global ischemia and (2) that interactions between the NMDA, muscarinic receptors and their corresponding neurotransmitter inputs to hippocampal neurons are evident in vitro and may play a crucial role in neuronal neurodegeneration. However, the mechanisms underlying the high vulnerability of dorsal hippocampus still remain enigmatic.     

The involvement of glutamatergic transmission in the mechanism of movement disorders induced by reversive rotation of white mice

The ability of the selective non-competitive NMDA receptor blocker MK-801 and a series of new glutamate antagonists—the adamantane derivatives IEM-1754 and IEM-1857 and phencyclidine (IEM-1925)—to prevent movement disorders induced by reversive rotation in mice was studied. I.p. MK-801 at a dose of 0.15 ml and IEM-1754 at a dose of 5.0 mg/kg prevented the development of akinesia in response to reversive rotation, as effectively as scopolamine, a known agent which provides effective prophylaxis for movement diseases. IEM-1857, the quaternary analog of IEM-1754, was not effective. IEM-1925 significantly increased the responses of mice to reversive rotation, possibly because of its high activity in relation to other subtypes of glutamate receptors. These data provide evidence for the involvement of glutamatergic transmission in the mechanism of movement disorders of vestibular origin. Translated from Rossiiskii Fiziologicheskii Zhurnal imeni I. M. Sechenova, Vol. 85, No. 4, pp. 497–501, May, 1999.     

东莨菪硷对兔急性脑损伤保护作用的实验研究

目的 :研究M受体拮抗剂东莨菪硷对兔急性脑损伤的保护作用 ,并初步探讨乙酰胆碱 (ACh)在创伤性脑伤早期病理变化中的作用。方法 :用自由落体打击器制作兔脑外伤模型 ,并于伤后 5min ,2h腹腔注射东莨菪硷 ,用经颅多谱勒监测大脑中动脉血流速度和搏动指数的变化 ;取脑组织检测Ca2 +、伊文思蓝 (EB)、超氧化物歧化酶 (SOD)、丙二醛 (MDA) ,并作病理检查。结果 :病检证实本模型符合临床所见加速性脑损伤的病理变化 ,东莨菪硷可降低兔脑外伤后脑组织中Ca2 +,MDA ,EB含量 ,升高SOD ,增加脑血流。结论 :脑外伤后早期ACh可致神经元钙超载、氧自由基反应、脑血管痉挛和血脑屏障 (BBB)通透性增强 ,M受体拮抗剂东莨菪硷可改善这些病理变化 ,具有脑保护作用     

不同方法使用东莨菪碱脱毒效果的比较

目的：观察东莨菪碱（scopolamine,Spm)和氯丙嗪（chloprmazine,Clo)对吗啡戒断反应的影响。方法：采用吗啡依赖大鼠模型,不同剂量单多次皮下注射（sc)东莨菪碱及合并使用氯丙嗪处理动物后,腹腔注射（ip)纳洛酮5mg/kg诱发戒断反应,观察戒断症状。结果：单次sc东莨菪碱1.0mg/kg及多次sc东莨菪碱0.5mg/kg可明显抑制吗啡依赖大鼠的身体戒断反应,合并注射氯丙嗪20.0mg/kg时的效果更好.结论:东莨菪碱通过Ach受体可以抑制吗啡戒断反应,氯丙嗪则可能通过作用于蓝斑墙 枢部位α2受体与东莨菪碱起到协同作用.