苦豆子总黄酮抗心律失常作用的实验观察

静脉注射苦豆子总黄酮50mg/kg,可显著对抗乌头碱诱发的大鼠心律失常;增加豚鼠对哇巴因的耐量;对抗氯仿—肾上腺素诱发的家兔心律失常;降低C_aCI_2,引起的大鼠室颤率和死亡率。腹腔注射50mg/kg 时,也可对抗氯仿诱发的小鼠室颤。此总黄酮也可明显减慢整体家兔和大鼠的心率,且可拮抗异丙肾上腺素的正性变率作用。     

奥氮平抗精神病作用的实验研究

目的：评价奥氮平的抗精神病作用。方法：通过苯丙胺诱导的小鼠定向运动实验、5-HTP诱导的小鼠头部抽动实验、大鼠僵住症试验,对奥氮平进行药效学观察,并与氯氮平及氟哌啶醇的药效进行比较。结果：奥氮平(ig,ED505.88mg/kg)、氯氮平(ig,ED5037.16mg/kg)、氟哌啶醇(ig,ED500.74mg/kg)能显著地拮抗苯丙胺诱导的小鼠定向运动,且有明显的量效关系。奥氮平(ig,ED500.54mg/kg)、氯氮平(ig,ED503.10mg/kg)、氟哌啶醇(ig,ED500.71mg/kg)能明显地拮抗5-HTP诱导的小鼠头部抽动。大鼠僵住症实验中,奥氮平、氯氮平、氟哌啶醇的ig,ED50分别是26,149,0.54mg/kg。结论：奥氮平有拮抗多巴胺及5-HT的活性,且其拮抗5-HT的作用比拮抗多巴胺的作用强,奥氮平的锥体外系不良反应轻,是一较好的抗精神病药物,奥氮平与氟哌啶醇合用对一些患者可能是较好的治疗方案。     

吗啉卡因的抗心律失常作用

腹腔内注射吗啉卡因(Mor)对抗氯仿诱发小鼠室速或室颤的ED_(50)为129mg/kg;静脉注射80mg/kg使豚鼠哇巴因产生室早、室速和室颤时剂量分别增加52、43和44％;腹腔注射Mor对抗乌头碱致小鼠心跳停止的ED_(50)为115mg/kg;静脉注射Mor100mg/kg随后静滴50mg/(kg·h)减少冠状动脉结扎大鼠室早数及室速时     

烟浪丁的抗心律失常作用

烟浪丁(NICO)100mg/kg iv,可明显对抗乌头碱和BaCl_2诱发大鼠及氯仿-肾上腺素引起兔的心律失常;降低CaCl_2所致的大鼠室颤率;提高豚鼠心脏哇巴因中毒的耐受量。NICO 50mg/kg iv也可预防结扎火鼠左冠状动脉引起的心律失常。50～100 mg/kg ip能降低氯仿或ACl_2-CaCl_2引起的小鼠室颤率或     

维生素K抗心律失常作用的初步研究

iv.维生素 K_1 4mg/kg,对抗肾上腺素诱发的家兔心律失常;iv.维生素 K_120mg/kg,对抗氯化钡诱发的大鼠心律失常;对乌头碱引起的大鼠心律失常及哇巴因引起的豚鼠心律失常无明显对抗作用;对氯化钙引起的小鼠心律失常死亡无明显影响。     

抗心律失常新药氨固酮和慢心利作用的比较

口服氨固酮20mg/kg对静脉灌注乌头碱引起的大鼠心律失常有预防效果,其作用约与口服慢心利30mg/kg相当。口服氨固酮20—30mg/kg对脑室内注射乌头碱所致大鼠心律失常有良好预防效果,同剂量慢心利则无效。小鼠腹腔注射(ip)氨固酮的LD_(50)为318.4mg/kg,慢心利为130.0mg/kg。大鼠恒速静脉灌注氨固酮或慢心利,最小致死量分别为142.5±15.9和42.1±7.8mg/kg。猫恒速静脉灌注氨固酮,可见血压逐渐降低,dp/dt不断减少,心率减慢,最小致死量为89.2±20.4mg/kg。     

骆驼蓬有效成分两种给药途径的毒性比较研究

目的:开展骆驼蓬有效成分骆驼蓬碱、去氢骆驼蓬碱两种给药途径的小鼠急性毒性比较研究。方法:采用Bliss法测定小鼠经口灌胃和静脉注射给药骆驼蓬碱、去氢骆驼蓬碱的LD_(50),同时观察小鼠中毒症状及中毒反应的起止时间。结果:骆驼蓬碱经口灌胃的LD_(50)及其95%可信区间为118.9 mg/kg(105.8~133.9 mg/kg),静脉注射的LD_(50)及其95%可信区间为80.3 mg/kg(60.6~146.1 mg/kg);去氢骆驼蓬碱经口灌胃的LD_(50)及其95%可信区间为250.3 mg/kg(210.0~293.3 mg/kg),静脉注射的LD_(50)及其95%可信区间为74.1 mg/kg(67.2~83.1 mg/kg)。小鼠经口灌胃给药时,骆驼蓬碱小鼠死亡时间早于去氢骆驼蓬碱小鼠死亡时间;小鼠静脉注射给药时,去氢骆驼蓬碱小鼠死亡时间早于骆驼蓬碱小鼠死亡时间。结论:小鼠经口灌胃给药骆驼蓬碱毒性去氢骆驼蓬碱毒性,小鼠静脉注射给药去氢骆驼蓬碱毒性骆驼蓬碱毒性。     

紫菜多糖对机体细胞的保护作用

小鼠ip紫菜多糖150mg/kg能对抗~(60)Coγ射线的辐射,存活率为对照组的1.8倍;对抗环磷酰胺引起的白细胞下降和微核增加,对抗率分别为79.60%和29.96%;对CCl_4所致的小鼠肝损伤SGPT升高有明显对抗作用,对抗率为68.04%;对肉瘤S-180有一定抑制作用,抑制率为47.55%;大鼠ip 180mg/kg,有较明显的对抗鹿角菜胶所致的炎症作用。正常小鼠ip、po 50mg/kg,3h后血糖分别下降58.45%和68.39%;对四氧嘧啶所致高血糖小鼠ip 50mg/kg,24h后血糖下降37.96%。     

心喘齐灵毒理实验研究

心喘齐灵为我国合成的扩张冠状动脉、降压、抗心律失常、平喘新药。小鼠口服心喘齐灵急性中毒表现惊厥、死亡,LD_(50)为328.90±53.28mg/kg。Wistar 大鼠口服心喘齐灵53mg/kg/d,连续6个月引起 Hb 降低(p<0.05)、血 Na~+减少(p<0.05)和可逆性肝、肾轻度损害。26.8mg/kg/d 亦可引起Hb 降低(p<0.05)。但是,5.3mg/kg/d 无明显毒性,表明治疗量是安全的,这和临床报告一致。用豚鼠试验无速发型变态反应。     

氟哌啶醇衍生物F3抗心律失常作用的观察

氯化钡诱发大鼠心律失常，舌下静脉注入剂量分别为1mg/kg、2mg/kg、4mg/kg的氟哌啶醇衍生物F     

羟乙基香兰素实验药理研究

一个新的合成药的中间产物——羟乙基香兰素,经药理实验研究,发现它有类似香兰素的抗癫痫作用。一、抗惊作用(一)、抗戊四氮惊厥:腹腔注射羟乙基香兰素500mg/kg(1/3LD_(50))20分钟后腹腔注射戊四氮80mg/kg,结果对照组惊厥率为95%而给药组为55%,说明药物能对抗戊四氮对小鼠引起的惊厥。如灌胃给药1055mg/kg(1/3LD_(50)),于给药后20分钟抗惊作用为61.1%,至一小时作用基本消失。     

Acute Toxicity and Cardio-Respiratory Effects of 2-Deoxy-D-Glucose： A Promising Radio Sensitiser

Objective To evaluate the acute toxicity of 2-deoxy-D-glucose （2DG） by oral （p.o.） and intravenous （i.v.） routes, and also the cardio-respiratory effects following high doses of 2DG in animal models. Methods The LD50 of 2DG （in water） was determined in rats and mice by p.o. route and in mice by i.v. route. The effect of 2-DG （250 mg/kg, 500 mg/kg, and 1000 mg/kg, i.v.） was studied on various cardio-respiratory parameters viz., mean arterial blood pressure, heart rate and respiratory rate in anaesthetised rats. The effect of 2DG （500 mg/kg, 1000 mg/kg, and 2000 mg/kg, p.o.） was also studied on various respiratory parameters viz., respiratory rate and tidal volume in conscious rats and mice using a computer program. Results The p.o. LD50 of 2DG was found to be 〉8000 mg/kg in mice and rats, and at this dose no death was observed. The LD50 in mice by i.v. route was found to be 8000 mg/kg. At this dose 2 out of 4 mice died and the death occurred within 6 h. A significant increase in the body weight was observed after p.o. administration of 2DG in rats at 500 mg/kg, 1000 mg/kg, and 2000 mg/kg doses. There was no significant change in the body weight at 4000 mg/kg and 8000 mg/kg by the p.o. route in rats and up to 8000 mg/kg by p.o. as well as i.v. routes in mice. Intravenous administration of 2DG （250 mg/kg, 500 mg/kg, and 1000 mg/kg） in anaesthetised rats showed a time-dependent decrease in the mean arterial blood pressure. There was no change in the heart rate in any of the treatment groups. The tidal volume was not changed significantly by p.o administration in conscious rats, but a significant decrease in the respiratory frequency at 500 mg/kg and 1000 mg/kg doses was observed. In the mice also there was no change in the tidal volume after p.o, administration, but the respiratory frequency decreased significantly at 2000 mg/kg dose. Conclusion 2DG is a safe compound but can cause a fall in the blood pressure and a decrease in respiratory frequency at high doses.     

山麦冬水溶物口服给药对实验性心律失常的影响

山麦冬水溶性提取物10g/kg口服给药可显著缩短BaCl_2致大鼠心律总异常时间;5g/kg与10g/kg口服给药可显著缩短乌头碱致大鼠心律总异常时间;4.5g/kg口服给药可明显延长氯仿—肾上腺素致家兔心律失常的潜伏期,并显著缩短心律失常的持续时间。     

国产Lorcainide对实验性心律失常的作用

<正> 本文以四种实验性心律失常动物模型研究了Lorcainide抗心律失常的作用。静脉注射Lorcainide 2.5mg/kg,能明显提高猫静注地高辛(0.05mg/ml)中毒引起室性心律失常至死亡的剂量(P<0.05);亦能缩短家兔静注氯化钡2～4 mg/kg所致心律失常的持续时间(P<0.05);尚可减弱或消除家兔静注肾上腺素50μg/kg后引起多种心     

氢溴酸右美沙芬对实验性咳嗽的镇咳作用

目的：研究氢溴酸右美沙芬对实验性咳嗽的镇咳作用。方法：化学品引咳法，电刺激引咳法。结果：氢溴酸右美沙芬１０ｍｇ／ｋｇ和２０ｍｇ／ｋｇ给小白鼠灌胃能有效地抑制氨水所致小鼠咳嗽的次数和延长潜伏期；５．５ｍｇ／ｋｇ和１１ｍｇ／ｋｇ给豚鼠灌胃给药对丙烯醛所致咳嗽有明显镇咳作用；３．２ｍｇ／ｋｇ和６．４ｍｇ／ｋｇ给豚鼠腹腔注射，对电刺激引起的咳嗽有明显镇咳作用。咳嗽次数减少率大于５０％，抑制率分别为５９．０２％和６３．９４％。结论：氢溴酸右美沙芬对多种实验方法引起的咳嗽有明显的镇咳作用。     

舒筋灵对家兔溴氰菊酯静脉染毒的拮抗作用

家兔静脉染毒溴氰菊酯所产生的急性毒性症状与大鼠相似,半数致死量为1.35mg/kg。家兔静脉染毒溴氰菊酯2.7mg/kg后立即静脉注射舒筋灵300mg/kg,可有效地拮抗溴氰菊酯的毒作用,缓解中毒症状,使家兔死亡率从100%降低至25%(P<0.05)。家兔溴氰菊酯2.15mg/kg静脉染毒后5分钟给予舒筋灵300mg/kg,可降低死亡率50%(P<0.05)。在染毒后10分钟给舒筋灵,舒筋灵已不能拮抗溴氰菊酯对家兔的毒作用。表明舒筋灵对以溴氰菊酯的拮抗作用只在溴氰菊酯的作用初期有效。     

绵毛黄芪苷和苦玄参苷的中枢抑制作用

报道了绵毛黄芪苷(SK)及其同类结构苦玄参苷(PIA)给予昆明种式BLC_(57)/1小鼠50mg/kg腹腔注射能明显延长硫贲妥钠的睡眠时间,用扭体法或热板法证实同量SK或PIA静脉注射能产生明显的镇痛作用。用格斗试验证实:同量SK或PIA腹腔注射可使小鼠格斗试验次数明显减少。提示两种苷可能具有中枢镇静、镇痛和安定作用;此类中枢抑制作用说明四环三萜皂苷类具有药用价值的前景。     

盐藻提取物对阿霉素诱发小鼠心脏毒性的影响

本文观察β-胡萝卜素和盐藻提取物对减轻阿霉素(ADM)诱发的小鼠心脏毒性的作用。ADM 为单次腹腔内注射,剂量为12mg/kg 或15mg/kg。β-胡萝卜素(0.6mg/kg)、盐藻提取物(0.75mg/kg)和溶剂(0.2ml/每只鼠)在注射 ADM 前24h 腹腔内注射。结果为光镜检查小鼠心肌组织发现,ADM 应用前预先腹腔注射盐藻提取物的小鼠心肌组织中的空泡和 PAS 阳性明显减少。ADM 注射后第4天或35天,单用 ADM 和 ADM 注射前腹腔注射过β-胡萝卜素及溶剂小鼠的心脏湿重均比 ADM 注射前预先腹腔注射盐藻提取物小鼠的明显减轻(P<0.05)。12mg/kg 的 ADM 单次注射以及在注射该量 ADM 前,经盐藻提取物和β-胡萝卜素预先处理小鼠的存活率。在 ADM 注射后的第35天分别是40%、100%和63%。ADM 剂量改为15mg/kg,在ADM 注射后14天.上述分组小鼠的存活率分别是0%、50%和12.5%。有无盐藻提取物预先处理的小鼠存活率之间的差异明显(P<0.05),而预先注射β-胡萝卜素和单用 ADM 小鼠存活率之间的差异无显著性(P>0.05)。这些结果提示,盐藻提取物在对抗 ADM 诱发的致死性心脏毒性上,具有保护作用,而β-胡萝卜素则缺乏保护作用。     

米托蒽醌的急性毒性研究

Acute toxicity of mitoxantrone (DHAQ) synthetized by Department of Organic Chemistry, School of Pharmacy, WCUMS was studied in mice and dogs. The toxic effects were compared with those of adriamycin (ADR). The LD50 were 6.6 +/- 1.3 and 7.1 +/- 1.6 mg/kg DHAQ, 7.9 +/- 2.1 and 10.7 +/- 2.2 mg/kg ADR (P = 0.95) respectively on observation with a single dose i.v. and i.p., for 21 days in Kunming mice. The toxicity appeared to be delayed with DHAQ and ADR. The earliest death occurred on 4th day after treatment in mice. In the third week still a few died. There were obvious decreases in WBC counts in the peripheral blood of mice receiving either 1-2.5 mg/kg DHAQ or 2.5-5 mg/kg ADR with a single dose i.p.. The WBC count could return to normality after 3 weeks with the withdrawal of the drugs. On electron microscopic examination of myocardial samples from mice 4 days after a single dose of 20 mg/kg DHAQ i.p., mitochondria swelling and vacuoles formation in some cells were shown. Besides the above-mentioned changes, some myocytes exhibited disorientation and loss of myofilaments in the mice which received equivalent dose of ADR. In dogs anaesthetized a temporary falling of blood pressure and slowing of heart rate were observed following 5-10 mg/kg DHAQ i.p.. When a dose of 50-100 mg/kg was given, the blood pressure dropped continuously until death.     

丙戊酸钠的抗实验性心律失常作用

一次静脉注射丙戊酸钠150mg/kg,能显著缩短氯化钡诱发大鼠心律失常的持续时间,推迟乌头碱致大鼠心律失常的出现时间,明显延迟肾上腺素诱发家兔心律失常的发生,并缩短其持续时间,显著提高豚鼠对哇巴因的中毒剂量,降低氯伤引起小鼠室颤的发生率。