华山参对中枢神经系统的药理作用

作者研究了华山参(Physochlaina infundibularis Kuang)对中枢神经系统的药理作用.华山参煎剂腹腔注射对小白鼠的LD₅₀为43(28.7-64.5)克/公斤;腹腔注射1克/公斤使大白鼠防御运动性条件反射潜伏期延长,部分动物条件反射破坏及分化抑制有解除现象;灌胃给药(2克/公斤)仅使条件反射潜伏期延长.腹腔注射1-4克/公斤显著降低大、小白鼠和家兔的自由活动,维持3-6小时,但不降低小白鼠的被动活动.腹腔注射4克/公斤,能协同硫喷妥钠及水合氯醛对小白鼠的催眠、麻醉作用;降低苯丙胺、咖啡因对小白鼠的兴奋活动,但在10克/公斤时对本丙胺的毒性作用及士的宁,戊四唑性惊厥无影响.给狗灌胃2-5克/公斤,有明显的镇静作用,但不能对抗去水吗啡的催吐效果.     

抗结核药丙硫异烟胺的药理与毒性的研究

丙硫异烟胺(Prothioamide)是第二线抗结核药。本文报道其药理与毒性研究结果。实验采用小白鼠、大白鼠和猫。药物配成5％混悬液一次或重复(每天给药,共30天)灌胃。对照组喂以生理盐水。结果表明,以0.1克/公斤给药后,小白鼠的活动次数减少3/4以上;剂量为0.5～1.0克/公斤时,经30～45分钟,全部动物的协调活动丧失,骨骼肌的张力降低,几小时后,动物处于侧卧状丙硫异烟胺(Prothioamide)是第二线抗结核药。本文报道其药理与毒性研究结果。实验采用小白鼠、大白鼠和猫。药物配成5％混悬液一次或重复(每天给药,共30天)灌胃。对照组喂以生理盐水。结果表明,以0.1克/公斤给药后,小白鼠的活动次数减少3/4以上;剂量为0.5～1.0克/公斤时,经30～45分钟,全部动物的协调活动丧失,骨骼肌的张力降低,几小时后,动物处于侧卧状     

加味黄芪建中汤抗大白鼠实验性胃溃疡作用的研究

本文对加味黄芪建中湯的抗大白鼠胃繯褡饔眉岸拘宰髁顺醪教教?建中湯煎剂给大白鼠皮下注射10克/公斤,可防止幽门结扎所致胃溃疡的发生;还能抑制胃液分泌、减少游离酸和总酸度;并使胃液pH值上升.但灌胃给药25克/公斤则不能防止溃疡的发生.建中湯煎剂对鸽胃正砊硕凹彝媚c运动都有抑制作用,并在一定程度上能对抗乙酰胆碱和毛果云香碱所致的腸痉挛.建中湯煎剂给小白鼠皮下注射的LD₅₀为48±7.2克/公斤.     

刺槐素的利尿作用

本文报导,黄酮类化合物刺槐素(Robinine)的不同给药途径对各种动物(大白鼠、家兔、狗)的利尿作用。大白鼠利尿试验:用体重140～240克大白鼠,每组8只,共4组。对照组给生理溶液,每100克体重5毫升,实验组除给生理溶液,并腹腔注射刺槐素分别为2.5、5、10毫克/公斤或口服10、15、50毫克/公斤。收集每只大白鼠5小时尿总量。家兔利尿试验:用体重2～3公斤雌、雄性家     

臭梧桐的药理研究 Ⅰ.臭梧桐热浸剂及提出物的毒性和降血压作用

1.本文就臭梧桐的一般性质作了实验性研究,结果证明其降血压成分易溶于水,难溶或不溶于乙醚、乙醇和氯仿,对热稳定,在碱性溶液中可被氯化钙沉淀出来。臭梧桐降血压效果可因产地而不同。开花前的和新鲜的臭梧桐降血压作用分别较开花后的和经长时间保存的要强。2.臭梧桐毒性甚小,其热浸剂和提出物给小鼠静脉注射时半数致死量分别为19.4克/公斤和0.98±0.075克/公斤。给大鼠每天用热浸剂(0.25—2.5克/公斤)灌胃经60天,除少数动物出现安静、轻度收缩压下降和大便变稀外,未发现其他毒性反应。3.臭梧桐提出物(50—100毫克/公斤)和热浸剂(150毫克/公斤)给麻醉大鼠和狗静脉注射时,可引起两度血压下降,但肌肉注射或经口给药,仅引起第二度降血压作用,其作用可维持2—3小时。静脉注射煎剂(麻醉大鼠和狗实验)仅出现第一度降血压作用,经口给药时无效。乙醚、乙醇和氯仿的浸出液不论静脉注射或经口给药,均不引起麻醉动物的血压下降。给肾型高血压大鼠每天经口投予臭梧桐热浸剂(0.5—5克/公斤)和提出物(50毫克/公斤)时,给药的第3—10天卽口出现血压下降,在给药的第二周和停药后的第一周,血压下降最明显,最大降血压作用可达原值的57.4%。多数高血压大鼠的血压在停药后的第二周恢复,少数在停药的2—4天或4周后恢复。     

防治血吸虫病药物的研究 ⅩⅩⅧ.敌百虫的毒性及其对日本血吸虫病的实验治疗

敌百虫是有机磷杀虫剂,又是胆碱酯酶抑制剂。本文試驗动物內用敌百虫的毒性和对日本血吸虫病的疗效,以及阿託品和PAM对敌百虫毒性与疗效的影响。小白鼠灌胃和皮下注射敌百虫1次的LD₅₀分別为0.8和0.6克/公斤。小白鼠在服敌百虫前30分钟注射阿託品和PAM的解毒效能比单用阿託品或单用PAM为佳。家兔每天灌胃30或60毫克/公斤共2周,抑制血浆胆碱酯酶活力70%左右。猴子灌胃剂量从4毫克/公斤开始,逐日递增4毫克/公斤,至第6天不食,胆碱酯酶活力也明显受到抑制,第7天躺臥不动,停药5天后恢复。小白鼠每天灌胃敌百虫200毫克/公斤,經2周后平均每鼠余存虫13±5条,和对照组24±6条相差非常显著.兔每天灌胃30毫克/公斤或皮下注射40毫克/公斤历2周后虫数也有减少.狗口服敌百虫2周后粪便转为阴性.然后停药2周解剖,平均每狗余存虫8±9条,比对照组6狗平均47±29条显著减少。在病狗治程中,血清磺溴酞钠存留率与血象无明显改变,血浆胆碱酯酶活力降为原来水平的25%左右.停药2周后恢复至原来水平的75%左右。敌百虫与吐酒石合并使用比单独应用一药治疗的效果要更好。阿品及PAM并不减弱敌百虫的疗效。敌百虫对动物的日本血吸虫病确有疗效,价格低廉,且可口服,为找寻有效的非锑剂开辟了新的途径。     

猪毛菜(茨蓬)浸膏对实验动物的药理研究

猪毛菜浸膏对麻醉动物有明显持久降压作用,无明显快速耐受現象。猪毛菜对乙酰胆碱及刺激迷走神經离中端所致降压作用无影响,阿託品不阻断猪毛菜的降压作用。双側迷走神經切断后,猪毛菜降压作用略減弱。猪毛菜不阻断頸上交感神經传导,亦无明显抗腎上腺素作用。猪毛菜抑制因压迫頸总动脉及刺激坐骨神經向中端所致的升压反射,二側竇神經切除亦不影响其降压作用。在猪毛菜引起降压作用时,带神經离体兔耳血管反射性扩张,因此推测猪毛菜对血管运动中枢或交感中枢有抑制作用。猪毛菜5,10克/公斤皮下注射能显著减少小白鼠自由活动。20克/公斤延长戊巴比妥鈉(35毫克/公斤)催眠作用的时間,并使非催眠剂量的水合氯醛(200毫克/公斤)产生催眠作用。但不能对抗中枢惊厥药(戊四氮及士的宁)的惊厥及致死作用。在小白鼠防御运动条件反射实驗中,皮下注射猪毛菜3克/公斤,对条件反射活动无明显影响。5克/公斤,10克/公斤时能使条件反射时延长,強化次数增加,分化相无变化。20克/公斤时条件反射显著抑制。5,10克/公斤皮下注射均能加速阳性条件反射消褪过程。小白鼠皮下注射猪毛菜LD₅₀为56克/公斤,大白鼠腹腔注射8克/公斤卽死亡。家兔口服(灌胃)40克/公斤未見毒性反应,80克/公斤时可見死亡。     

酸枣仁与五味子防治烧伤的实验观察

作者观察到酸枣仁(5.0克/公斤)、五味子(1.0克/公斤)单用或合用(酸枣仁1.0—5.0克/公斤,五味子0.5—1.0克/公斤)均能提高烫伤小白鼠的存活率,延长存活时间;酸枣仁与五味子配伍还能推迟大白鼠烧伤休克的发生和延长存活时间,并能减轻小白鼠烧伤局部的水肿。此外,溴化钠与咖啡因的合剂(溴化钠0.5—1.0克/公斤,咖啡因0.002—0.025克/公斤)对小白鼠烫伤和大白鼠烧伤休克均有较良好的影响;吗啡0.025克/公斤对小白鼠烫伤水肿有显著的减轻作用。本实验中,冬眠合剂Ⅰ号(氯丙嗪0.01克/公斤,异丙嗪0.01克/公斤,嘜啶0.02克/公斤)及氯丙嗪(0.01克/公斤)对烧伤皆无防治效果。作者在本文中就酸枣仁与五味子防治烧伤的作用机制,进行了讨论。     

维生素C对大白鼠条件反射活动的影响

利用大白鼠运动防御性条件反射方法,研究了大剂量維生素C对健康动物高級神經活动的影响。結果証明,每日腹腔注射維生素C 0.2克/公斤能加速大白鼠阳性条件反射的形成。維生素C 0.1—1克/公斤可使大白鼠阳性条件反射潛伏期縮短,靜脉給药較腹腔給药效果显著。腹腔注射維生素C 0.2克/公斤与咖啡因(25毫克/公斤,皮下注射)并用对条件反射无明显协同作用;与氯丙嗪(3毫克/公斤,腹腔注射)并用有一定拮抗作用。当靜脉注射維生素C 0.2/公斤时,对氯丙嗪有明显的拮抗作用。腹腔注射維生紊C 0.4克/公斤对消退性抑制,以及靜脉注射維生素C 0.1克/公斤对分化性抑制皆无显著影响。     

中药苍术、萹蓄、芫花及车前子煎剂利尿作用的初步观察

苍朮[Atractylodes lancea(Thunb.)DC.]为菊种植物,药用其地下根状茎。“本草纲目”记载,可治“水肿胀满”。经利彬等以其流浸剂给麻醉犬靜脉注射,发现有轻微利尿作用。 萹蓄(Polygonum aviulare L.)属蓼科植物,药用其地上部分。中医临床常用其利尿消肿。黄厚聘等以其煎剂给大白鼠皮下注射或口服皆有利尿作用。芫花(Daphne genkwa Sieb.et Zucc.)为瑞香种植物,药用其花蕾。在中医临床上常用于逐水消肿。马统勋报告,该药对大白鼠与麻醉犬有利尿作用。邓祖藩等报告,健康人口服该药和家兔用该药灌胃后均有显著利尿作用。     

广寄生苷之利尿作用

广寄生系桑寄生属植物,按国产桑寄生因产地不同而有三种,产于珠江流域者称广寄生,产于长江流域者称杜寄生,产于华北及东北者称北寄生。我国自古即以桑寄生供药用,神农本草经将其列入上品,大明本草谓能“助筋骨,益血脉”。近代学者用做强壮剂、消肿……及治高血压,血管硬化性四肢麻木……。关于广寄生之化学研究,最近本文作者之一(曾广方)自广寄生(Loranthus paracticusL. C. Merr.)中分离出两种结晶,其中之一为—黄酮类苷,暂称为广寄生苷,水解所得之     

中国萝芙木的药理研究,Ⅱ.海南岛萝芙木的降压作用和毒性试验

在发现广东大陆部分出产蘿芙木后,植物学家又相继在海南岛、云南和广西发现了蘿芙木,经鉴定和广东所产为同一品种,即Rauwolfia verticillata (Lour.) Baill. 我们在肯定了广东所产蘿芙木叶的粗制剂和生物硷的降压作用后,首先用海南岛所产叶的粗制剂物和生物硷进行实验,结果也发现它们有显著的降压作用。由于化学研究指出根含生物硷较多,因而又进行试验,肯定了根的生物硷的降压作用。此外,又进行     

Pharmacology of dihydroxy-dibutylether, a specific choleretic drug.

The choleretic and the general pharmacological properties of dihydroxy-dibutyl ether (Discinil) were investigated in several animal species. Discinil (DHBE) increased the bile flow in conscious rats and dogs, after both oral and i.v. administration. A choleretic effect was also observed after i.v. injection into anaesthetized rats and guinea pigs. A dose-response relationship was always obtained, the threshold dose being 25--100 mg/kg. No evidence of tachyphylaxis was observed in rats after repeated treatments. The bile hyperflow was generally accompanied by an increased excretion of the total dry residue in guinea pigs and dogs. The choleretic effect in rats was still present after pretreatment with either DL-ethionine (causing parenchymal liver damage) or atropine (blocking the cholinergic control of bile production). At low doses (25--100 mg/kg i.v.) eliciting a definite choleretic response, DHBE did not show spasmogenic and spasmolytic effects in vivo on the smooth muscles of the gallbladder of guinea pigs and dogs, neither on the stomach and intestine of mice and dogs; while it constricted the pylorus sphincter of rats. At larger doses (200--400 mg/kg i.v.) the compound showed a mild relaxing activity on Oddi's sphincter of guinea pigs and a weak spasmogenic activity either on gall bladder or on small intestine. In vitro, it caused an unspecific antagonism against the spasm induced by acetylcholine, barium chloride, histamine, 5-hydroxytryptamine and norepinephrine. In anaesthetized rats, rabbits and dogs, DHBE caused a moderate and short-lasting hypotension, and tachycardia. The threshold doses for these effects were 2--4 times superior to those being choleretic. In conscious dogs, the compound was slightly hypertensive. DHBE did not provoke important respiratory and ECG changes, neither showed diuretic nor antiphlogistic effects.     

异钩藤碱的降压及血流动力学作用(英文)

在清醒正常血压大鼠,iv Isorhy2.5 mg/kg对BP及HR均无明显影响,iv5 mg/kg则使DAP和HR降低,但SAP无变化,剂量加大至10 mg/kg时,上述各项指标均明显降低。经十二指肠内给Isorhy10 mg/kg后20 min出现BP及HR降低,而20mg/kg剂量组于10 min开始出现BP及HR的进一步下降.Isorhy(10mg/kg和2 mg/kg,iv)亦能分别降低肾性高血压清醒大鼠和麻醉犬的BP。icv表明中枢不是降压作用的主要部位,在体条件下无α-受体和神经节阻断作用。Isorhy使清醒大鼠和麻醉犬的LVSP,dP/dt_(max),V_(max)等左室收缩性能指标短暂下降,而BP呈持久性降低。在麻醉犬给药后CO,CI,HR及LVWI下降的同时SV和SI不变,TPVR降低,反映心肌氧耗的TTI明显减少.结果提示Isorhy具有肯定的降压作用,其持续降压与扩张血管及减慢心率导致CO下降有关,而其负性肌力作用亦可能参与了早期的降压机理.Isorhy能减少心肌氧耗对高血压心肌劳损可能有保护意义。     

长春花生物碱部分之一 AC-875的抗肿瘤作用及毒性

木文对长春花(Catharanthus roseus Linn.G.Don)中分离提出的生物碱AC-875进行了毒性及抗癌作用的实验研究.试验结果表明AC-875在20-42毫克/公斤时,对小鼠Ehrlich腹水癌及腹水型肝癌均有明显的抑制作用.当剂量为10毫克/公斤时,对大鼠腹水型吉田肉瘤也有较好的疗效.在实体瘤的治疗中,注射35毫克/公斤,对小鼠S-180仅有轻度抑制作用,且不太稳定.对小鼠网织细胞瘤、Ehrlich腹水癌实体瘤、大鼠Jensen肉瘤及Walker癌等则无抑制作用.给小鼠腹腔注射AC-875的急性LD₅₀为170毫克/公斤,亚急性LD₅₀为61毫克/公斤.给大白鼠腹腔注射AC-875的意性及亚急性LD₅₀分别为122毫克/公斤及18毫克/公斤.给家兔静脉注射8毫克/公斤AC-875时,心电图无明显变化.静脉注射AC-875 1毫克/公斤、2.5毫克/公斤或皮下注射5毫克/公斤,对狗的肝、肾功能、尿常规、红血细胞、血红蛋白及体重均无明显影响,但2.5和5毫克/公斤组,狗的白细胞有下降现象.     

可乐定抑制胃肠运动及机理研究

可乐定(15～120μg/kg,sc)剂量依赖式地抑制小鼠及大鼠胃肠推进运动及小鼠排便反射,此作用明显强于吗啡。可乐定(120μg/kg·d×10d,sc)对小鼠上述作用未产生耐受性。icv可乐定(12μg/kg)抑制大鼠胃肠推进运动作用强于sc同剂量的可乐定。育亨宾(0.5～5mg/kg,sc)剂量依赖式地拮抗可乐定对小鼠胃肠推进运动及排便的抑制作用。     

Renal effects of veratridine

Veratridine hydrochloride injected subcutaneously into unanaesthetized rats inhibited water diuresis. A linear relationship between log dose and antidiuretic effect could be established over the dose range 50 to 200 μg./100 g. of body weight. When veratridine hydrochloride was injected intravenously in doses from 10 to 30 μg./100 g., this relationship was also linear. In terms of its antidiuretic action, the alkaloid was approximately five times as effective when given intravenously. Rats anaesthetized with urethane responded to an intravenous injection with a more pronounced inhibition than unanaesthetized animals. Protoveratrine injected intravenously into unanaesthetized rats showed no clear relationship between dose and magnitude of antidiuretic effect. Veratridine hydrochloride injected intravenously had a pronounced hypotensive effect in both anaesthetized and unanaesthetized rats. Treatment with atropine did not affect this hypotensive action significantly. Atropine given subcutaneously 30 min. before an intravenous injection of veratridine hydrochloride abolished or diminished the inhibitory effect of veratridine on water diuresis. Veratridine hydrochloride injected intravenously into unanaesthetized rats caused a marked depression of the clearance of inulin and p-aminohippurate. In unanaesthetized rats with an osmotic diuresis, veratridine hydrochloride produced its usual antidiuretic effect. The urine of rats injected with veratridine hydrochloride produced an antidiuretic effect when injected intravenously into other animals. The antidiuretic potency of such urines was not affected by treatment with thioglycollate. Animals injected with veratridine excreted small amounts of a veratridine-like substance in the urine. These results do not suggest that veratridine in antidiuretic and hypotensive doses stimulated the neurohypophysis in the rat.     

Effects of bombesin on erythropoietin production in the anaesthetized dog

Summary Bombesin, a tetradecapeptide isolated from the skin of some European discoglossid frogs, has been reported previously to reduce renal blood flow and glomerular filtration rate and to increase plasma renin activity in anaesthetized dogs.In the present study bombesin was infused intravenously in anaesthetized dogs at dose levels of 3, 6 and 12 ng/kg/min for 6 h and renal blood flow, glomerular filtration rate, oxygen consumption, oxygen extraction by the kidney tissue, as well as plasma erythropoietin levels (ESF) and plasma renin activity were measured. Plasma levels of ESF increased during bombesin infusion only when renal blood flow was reduced to a level of 1 ml/g/min or less. In this situation glomerular filtration was blocked, renal oxygen consumption was decreased to 10% of normal and oxygen extraction by the kidney was increased by 2 times. No correlation was found between plasma renin activity and ESF concentrations during bombesin infusion. It is concluded that the stimulant action of bombesin on ESF production is a consequence of the renal hypoxia induced by the reduction in renal blood flow.     

Cardiovascular activity of 9-hydroxy-ellipticine.

The cardiovascular activity of 9-hydroxy-ellipticine (9-OH-E) has been studied on anaesthetized dogs. The drug has been administered intravenously in one dose ranging from 1 to 10 mg/kg. The variations in the myocardial contractility, the systemic haemodynamics, the respiration and the general metabolism of the anaesthetized dogs were studied to make evident the mechanism of 9-OH-E cardiostimulating action. 9-OH-E from 5 mg/kg i.v. stimulates the contractility of myocardium and improves the cardiac performances of the anaesthetized dogs. This heart-stimulating action is long-lasting and is not accompanied by any modification in the arterial blood pressure. It is inhibited or at least strongly attenuated by beta-adrenergic blocking agents and by the depletion of catecholamines.