Experimental study of oculocardiac reflex (OCR) with graded stimuli

The present study was conducted to observe the effect of graded mechanical stimuli on occurrence of oculocardiac reflex (OCR). The experiments were carried out in twenty albino rabbits of either sex weighing between 1-2 kg. Changes in heart rate and/or cardiac rhythm (oculocardiac reflex) were studied by applying traction with progressively increasing weights to medial rectus muscle. Mean threshold value of square wave mechanical stimulus just sufficient to produce oculocardiac reflex was found to be 19 +/- 8.52 g. As the traction weights were progressively increased, more and more decrease in heart rate was observed. It was concluded that once the threshold value of stimulus was reached, the oculocardiac reflex showed a graded response with progressively increasing traction weights.     

Experimental study on central effects of carboxyethyl-gamma-aminobutyric acid (CEGABA)

The central effects of carboxyethyl-gamma-aminobutyric acid (CEGABA) have been studied both in rabbits and in the guinea pig myoclonus model. This drug caused EEG synchronization and behavioural sedation both after intravenous (i.v.) and intracerebroventricular (i.c.v.) administration in a dose-dependent manner, in rabbits. CEGABA showed a protective action against myoclonus induced by means of L-5-HTP in young guinea pigs. These data substantiate the hypothesis that CEGABA is a drug active on the central nervous system and probably exerts its action by strengthening cortical inhibition and/or directly acting on lower brainstem.     

Pharmacokinetics,N1-glucuronidation and N4-acetylation of sulfamethomidine in humans

Sulfamethomidine metabolism was studied in 6 volunteers. In humans, only N1-glucuronidation and N4-acetylation take place, leading to the final double conjugate N4-acetylsulfamethomidine N1-glucuronide. The N1-glucuronides were directly measured by high pressure liquid chromatography. Fast and slow acetylators show a similar half-life for sulfamethomidine (26±6 h) and its conjugates sulfamethomidine N1-glucuronide (26±6 h) and N4-acetylsulfamethomidine (36±16 h). Approximately 50–60% of the oral dose of sulfamethomidine is excreted in the urine, leaving 40–50% for excretion into bile and faeces. The main metabolite of sulfamethomidine is its N1-glucuronide, which accounts for 36±7% of the dose, followed by N4-acetylsulfamethomidine (16±8%). N1-glucuronidation results in a 75% decrease in protein binding of sulfamethomidine. N4-acetylsulfamethomidine and its N1-glucuronide showed the same high protein binding of 99%. The renal clearance of N4-acetylsulfamethomidine is 7.9±2.2 ml/min and approximately 20 times as high as that of the parent drug (0.46±0.16 ml/min). Total body clearance of sulfamethomidine is 4.5±0.9 ml/min and the volume of distribution in steady state 10.6±1.7 1. No measurable plasma concentrations of the N1-glucuronides from sulfamethomidine are found in plasma. This may be explained by renal glucuronidation after active tubular reabsorption.     

Experimental study of mercury transfer between artificially contaminated sediment (CH3HgCl) and macrophytes (Elodea densa)

The quantification of metal transfer routes from a natural sediment enriched with methylmercury (4 mg · Hg kg⁻¹ fresh weight) to Elodea densa, shows a high mercury accumulation in the plant organs (leaves, stems and roots). The experimental approach developed shows that, in the long term (28 days), root absorption of the organic compound (direct route) represents the dominating vector of metal accumulation in the plant, the leaves being the principal organ for storage. Two mechanisms, far less important from a quantitative point of view, are superimposed in this direct transfer: contamination by the water, linked to the releasing phenomenon at the interface ‘water-sediment’, during the initial exposure phase (4 days), and inter-plant transfers resulting from decontamination processes, acting together with direct metal accumulation in the E. densa.     

脂蛋白（a）对血管内皮细胞损伤作用的实验研究

目的 研究脂蛋白（ａ）「Ｌｐ（ａ）」对血管内皮细胞（ＥＣ）的损伤作用和高密度脂蛋（ＨＤＬ）存在时对血管ＥＣ的损伤作用。方法 以体外培养的人脐静脉ＥＣ为模型,通过观察细胞形态、测定细胞功能了解Ｌｐ（ａ）和ＨＤＬ和Ｌｐ（ａ）对ＥＣ的损伤作用。结果 预加入ＨＤＬ再加入定量的Ｌｐ（ａ）后,ＥＣ收缩,胞浆呈分支状,乳酸脱氟酶（ＬＤＨ）释放量增高,６－酮－前列腺素Ｆｌａ（６－ｋｅｔｏ－ＰＧＦｌａ）合成明显关少     

Experimental and clinical pharmacology of glycosaminoglycans (GAGs)

The experimental and clinical pharmacology of glycosaminoglycans (GAGs) is discussed, including that of heparin and related compounds, hyaluronic acid and chondroitin sulfates.     

Experimental study of the biliary excretion of antibiotic (cefotiam) in the presence of biliary tract obstruction (author's transl)

Excretion of a new semisynthetic analogue of cephalosporin, cefotiam (CTM), and cefazolin (CEZ) in bile was investigated in dogs with experimental obstruction of biliary tract. In the control group, peak concentrations of antibiotics in bile after 50 mg/kg intravenous administration were as follows: In CTM administrated groups, 5,302 micrograms/ml at one hour after administration; and in CEZ administrated group, 1,249 micrograms/ml after one hour. The total biliary excretory rates summed to 6 hours after administration of antibiotics were 7.8% in the CTM group, and 2.1% in the CEZ group. On the other hand, in the biliary tract obstruction group, the peak concentration in bile in CTM group was 65.7 micrograms/ml after 1 hours, and in CEZ group, 62.4 micrograms/ml after 2 hours. The total biliary excretory rate in the CTM group was 0.202%, while in the CEZ group 0.12%. The peak concentration and the excretory rate of CTM in bile was four times higher than that of CEZ in the control group. No significant difference was revealed in the peak concentration and the excretory rate in bile between CTM and CEZ in the biliary tract obstruction group.     

肌肤生碘伏盖髓的动物实验和临床应用

目的探讨肌肤生碘伏盖髓的效果。方法采用新型的生物材料肌肤生和碘伏直接在动物牙齿上盖髓,对照组使用氢氧化钙。术后4、12周拔取牙齿做组织学观察。临床应用采用病例(50例)观察对照研究方法。结果组织学显示,用肌肤生碘伏盖髓牙本质细胞成熟较对照组快,形成牙本质桥较厚,临床疗效好。结论肌肤生碘伏盖髓能促进牙本质修复,在临床盖髓中不失为理想的盖髓剂。     

红花注射液引起过敏反应的实验研究

目的 研究红花注射液(心脑血管中药)引起过敏反应的免疫学机制.方法 用化学萃取、蒸馏及柱层析等方法,将红花注射液分离,并将这些组分通过对豚鼠腹腔注射致敏、心内注射激发的方法,榆测红花注射液及各组分的致敏作用.并用RT-PCR法检测红花注射液是否对巨噬细胞有刺激作用.结果 红花注射液能够引起豚鼠Ⅰ型过敏反应,在红花分离、提纯得到的各组分中,以乙醚提取物的致敏作用最强.结论 红花注射液巾脂溶性较大的成分有可能足引起过敏反应的主要过敏原.     

三七总皂甙对兔肺挫伤治疗作用的实验研究

目的 采用重物自由落体复制兔肺挫伤模型,通过检测炎症因子白介素-1β(interleukin-1β,IL-lβ),氧化应激指标脂质过氧化产物丙二醛 (malondialdehyde,MDA)及髓过氧化物酶(myeloperoxidase,MPO)水平,并结合肺组织湿干比重及病理变化,探讨三七总皂甙(panax noto...     

天茄子不同提取部位止血作用研究

目的研究天茄子不同提取部位的止血药理作用。方法依次以环己烷(T1)、水(T2)和乙醇(T3)为溶剂进行提取并对乙醇提取物依次用石油醚(T4)、乙酸乙酯(T5)、正丁醇(T6)进行萃取得到相应的部位以及水部位(T7),采用毛细玻管法、玻片法、剪尾法和测定血浆复钙时间检测其止血作用。结果 T3、T6、T7可缩短小鼠玻片法凝血时间,T3、T5、T6、T7可显著缩短小鼠毛细管法凝血时间,T3、T4、T5、T6、T7可显著缩短小鼠断尾法出血时间,T3、T6、T7可显著缩短小鼠血浆复钙时间。结论天茄子95%醇总提物、乙酸乙酯部位、正丁醇部位、水部位凝血效果显著,其中95%醇总提物、正丁醇部位、水部位凝血效果极其显著。     

三氧化二砷治疗哮喘作用机制的实验研究

目的　研究三氧化二砷 (As2 O3 )对哮喘豚鼠气道嗜酸性粒细胞 (EOS)凋亡和核因子 κB(NF κB)表达的影响作用 ,探讨As2 O3 对哮喘可能的治疗机制。方法　豚鼠 2 0只建立哮喘模型后随机分为对照组和As2 O3 (2mg/kg)治疗组。每组 10只 ,采用TUNEL技术原位标记细胞凋亡 ;免疫组织化学染色技术检测豚鼠气道壁NF κB ;计算机图像分析技术对气道壁EOS凋亡和NF κB表达进行定量检测。结果　对照组豚鼠支气管壁EOS凋亡指数为 (0 2 3± 0 0 5 ) % ,整个肺组织包括气管、支气管、肺泡和脏层胸膜构成了一个NF κB+ 细胞网络 ,其中支气管壁胞核NF κB+ 细胞密度为 (12 6 1± 190 )个 /mm2 上皮面积 ;哮喘豚鼠经As2 O3 处理后 ,支气管壁EOS凋亡指数显著增加 (P <0 0 1) ,胞核NF κB+ 细胞密度显著下降 (P <0 0 1) ,并且气道壁EOS凋亡指数与胞核NF κB+ 细胞密度之间呈显著性负相关 (r =- 0 91,P <0 0 1)。结论　抑制气道NF κB激活 ,促进EOS凋亡 ,可能是As2 O3 治疗哮喘的重要机制之一。     

Experimental study on the circulatory effects of 2-(2,6-dichlorophenylamino)-2-imidazolinehydrochloride in man

Summary The circulatory effects of a new antihypertensive agent, dichlorophenylamino-imidazoline (DCAI), were investigated in 17 normotensive and 17 hypertensive subjects. The following parameters were measured: Arterial pressure (AP), peripheral venous pressure (PVP), muscle blood flow (MBF), skin blood flow (SBF), heart rate (HR), total blood volume (TBV), and the excretion of catecholamines (CA) and vanillinmandelic acid (VMA). DCAI was administered in single doses of 0.15–0.3 mg intravenously or, in long-term experiments, in daily doses of 0.3–1.5 mg per os. — DCAI i. v. produced a short (mean: 2 min) increase in both systolic and diastolic AP, followed by a long lasting decrease. HR was slightly reduced during both phases. PVP was not significantly altered. MBF was unchanged or transiently slightly increased. Immediately after injection of DCAI, SBF sharply decreased to 50–60% of the resting flow; subsequently it rose gradually towards control values without reaching them during the time of observation. —Effective oral treatment with DCAI in 5 hypertensive patients produced no change in TBV. — The urinary excretion of CA and VMA was not significantly altered by a single i. v. dose of 0.15 mg DCAI. — The responses of AP, PVP, MBF and SBF to adrenaline, noradrenaline and angiotensin were not altered qualitatively by pro-treatment with single i. v. doses of DCAI. The duration of the depressor effect of adrenaline is, however, slightly but significantly prolonged. The decrease in SBF elicited by all 3 substances is diminished following DCAI, most probably as a consequence of the reduction in the control values caused by DCAI. Tolazoline antagonized the effects of DCAI on AP and SBF. It may be useful clinically as an antidote. — The results are discussed with regard to the hemodynamic changes occurring during the first (pressor) and second (depressor) phase of action of DCAI.

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Experimentelle untersuchung der kreislaufwirkungen von 2-(2,6-dichlorphenylamino)-2-imidazolin-hydrochlorid am menschen

Zusammenfassung Die Kreislaufwirkungen einer neuen blutdrucksenkenden Substanz, Dichlorphenylaminoimidazolin (DCAI) wurden an 17 normotonen und 17 hypertonen Versuchspersonen untersucht. Die folgenden Parameter wurden gemessen: Arterieller Blutdruck, peripherer Venendruck, Muskeldurchblutung, Hautdurchblutung, Herzfrequenz, Gesamt-Blutvolumen und die Ausscheidung von Brenzkatechinaminen und Vanillin-Mandelsäure. DCAI wurde in Einzeldosen von 0.1–0.3 mg intravenös bzw. bei länger dauernden Experimenten in Tagesdosen von 0.3–1.5 mg per os verabreicht. — DCAI bewirkte intravenös gegeben, einen durchschnittlich 2 min dauernden Anstieg sowohl des systolischen als auch des diastolischen arteriellen Blutdrucks, dem ein langanhaltender Druckabfall folgte. Die Herzfrequenz nahm während beider Phasen gering ab. Der periphere Venendruck änderte sich nicht signifikant. Die Muskeldurchblutung blieb unverändert oder nahm vorübergehen gering zu. Unmittelbar nach der Injektion von DCAI fiel die Hautdurchblutung bis auf 50–60% der Ruhedurchblutung ab, anschließend stieg she allmählich wieder in Richtung auf die Ausgangswerte an, ohne these jedoch während der Beobachtungszeit zu erreichen. — Im Verlauf einer wirksamen oralen Behandlung mit DCAI bei 9 Hypertonikern änderte sich das Gesamt-Blutvolumen nicht signifikant. — Die Ausscheidung von Katecholaminen und Vanillin-Mandelsäure wurde durch einmalige intravenöse Gabe von 0.15 mg DCAI nicht sicher beeinflußt. — Die durch Adrenalin, Noradrenalin und Angiotensin ausgelösten Reaktionen des Blutdxucks, des Venendrucks sowie der Muskel — und Hautdurchblutung wurden durch DCAI qualitativ nicht verändert. Die Intensität der durch allo 3 Substanzen ausgelösten Durchblutungsabnahme in der Haut war infolge des durch DCAI stark verminderten Ausgangswertes herabgesetzt. — Tolazoline antagonisierte die Wirkungen von DCAI auf den arteriellen Blutdruck und die Hautdurchblutung. Es kommt klinisch als Antidot in Betracht. — Die Resultate wurden im Zusammenhang mit den hämodynamischen Veränderungen während der ersten (pressorischen) und zweiten (depressorischen) Phase der DCAI-Wirkung diskutiert.

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Dedicated to Professor Hans Schaefer, Heidelberg, on his 60th birthday.

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Supported by a grant from the Stiftung Volkswagenwerk.     

血必净对窒息大鼠复苏后心功能不全的影响

目的探讨血必净对复苏后心功能不全的影响。方法建立心肺复苏大鼠模型,96只SD大鼠随机分为假手术组（B组,仅进行麻醉和气管切开插管、血管穿刺,不进行窒息及心肺复苏）、常规复苏组（C组,常规复苏＋生理盐水4ml／kg,血必净低剂量治疗组（D组,血必净2ml／kg＋生理盐水2ml／kg）和血必净高剂量治疗组（E组．血必净4ml／kg）,动态观察平均动脉压（MAP）、左室舒张末压（LVEDP）、左室内压最大上升和下降速率（±Vdp／dt）的变化。结果（1）与B组同时点比较,C、D组复苏后6hMAP低于B组（P〈0．01．P〈0．05）;LVEDPC、D组复苏后2、4、6h均高于B组（P〈0．01,P〈0．05）,E组各观察时点略高于B组（P〉0．05）;±LV dp／dtC组复苏后2、4、6h均低于B组（p〈0．01）．D、E组略低于B组（P〉0．05）。（2）与复苏前比较,C组MAP复苏后6h低于复苏前（P〈0．05）;C组复苏后2、4、6hLVEDP高于复苏前,±LV dp／dt低于复苏前,差异均有统计学意义（P-~C．0．01）,LVEDPD组复苏后4、6h高于复苏前（P〈0．05）,±LVdp／dtD组复苏后2、4、6h均低于复苏前（P≮0．01）,B、E组差异无统计学意义。（3）与C组同时点比较,E组复苏后6hMAP高于C组（P00．05）;±LVdp／dtE组2h、D组4h和E纽4、6h、D组6h高于C组（P〈0．05,P〈0．01）;LVEDP E组4h、D组6h和E组6h低于C组（P〈0．05,P〈0．01）。（4）与D组同时点比较,±LVdp／dtE组2、4、611均高于D组（P％0．05）,LVEDP无差异（P〉0．05）。结论血必净可以改善心肺复苏后心功能不全,高剂量血必净作用更佳。