Some aspects of the pharmacology of an homologous series of choline esters of fatty acids

The pharmacological effects of a series of fatty acid-choline esters have been studied on the isolated rabbit heart, the isolated guinea-pig ileum and the rat stomach. The effect changed with increasing chain length, and three different types of response were observed. The shortchain compounds produced depression of the isolated rabbit heart and spasm of the isolated guinea-pig ileum. Only one, butyrylcholine, had an erratic stimulating effect on hydrochloric acid secretion by the partially vagotomized rat stomach. Medium-chain compounds had a stimulating effect on the isolated rabbit heart, a mixed spasmogenic and relaxant effect on the isolated guinea-pig ileum, and no effect on the rat stomach. Long-chain compounds blocked the effect of acetylcholine on the isolated rabbit heart and the isolated guinea-pig ileum; they also depressed spontaneous hydrochloric acid secretion by the rat stomach. The nature of these three types of response is discussed.     

垂体后叶素联用普鲁卡因治疗中大量咯血的疗效观察

目的：对比普鲁卡因与垂体后叶素单用和联用治疗中大量咯血的止血效果和不良反应。方法：患者分3组：普鲁卡因组,垂体后叶素组,两者联用组。结果：普鲁卡因组和垂体后叶素组止血效果无统计学差异（P〉0.05）,但垂体后叶素组不良反应显著高于普鲁卡因组（P〈0.005）;两者联用组止血效果优于普鲁卡因组和垂体后叶素组（P〈0.05）。结论：普鲁卡因和垂体后叶素联用止血效果更强,不良反应更少。     

卡巴匹林钙主要药效学研究

目的：卡巴匹林钙（考察卡巴匹林钙）的解热镇痛作用，为临床用药提供药效学资料。方法：用小鼠醋酸扭体和电刺激大鼠尾部疼痛模型考察卡巴匹林钙的镇痛作用；用啤酒干酵母致大鼠发热模型考察卡巴匹林钙的解热作用；并测定小鼠口服给药和静脉注射给药的急性毒性。结果：小鼠口服卡巴匹林钙对腹腔注射醛酸致扭体反应有明显镇痛作用，作用强度与剂量相关；大鼠口服卡巴匹林钙对电刺激大鼠尾部疼痛亦有明显镇痛作用，疼痛电压阈值的提高和镇痛维持时间与剂量呈正相关，镇痛起效时间与剂量呈负相关。结论：卡巴匹林钙口服对动物发热模型和疼痛模型具有明显的解热镇痛作用，其镇痛作用较解热作用起效快，但解热作用维持时间长。     

小檗碱抗心力衰竭作用研究概况

小檗碱为异喹啉类生物碱，药理作用广泛，近年来药理学发现其具有治疗心力衰竭的作用。该文对小檗碱从心肌收缩力的正性肌力作用和负性肌力作用两方面在心力衰竭中的应用研究进行综述，并且提出了对小檗碱治疗舒张性心力衰竭的展望。     

氨基嘧啶对脊髓腹角神经细胞生长的影响

本文观察了氨基嘧啶对鼠胚脊髓腹角神经细胞生长的作用。不同浓度的氨基嘧啶使长突起的细胞数及突起数增加,有明显量效关系;氨基嘧啶能对抗秋水仙素对神经细胞突起的生长和提取的兔脑微管亚基管蛋白体外聚合成微管的抑制作用,又能使蛋白质含量高的细胞数增多。上述结果提示氨基嘧啶可能通过保护管蛋白聚合和增加蛋白合成而促进神经细胞的生长。     

孕酮对卵母细胞膜电位影响的分析

本实验采用微电极细胞内记录方法,观察了不同浓度孕酮及不同作用时间对卵母细胞膜电位影响。发现孕酮具有致充分生长的蟾蜍卵细胞膜电位去极化的作用,其去极化效应有时间与剂量依赖性关系。     

Evidence for a peripheral action of thyrotropin releasing hormone on gastrointestinal transit in mice

The effect of the two analogs of thyrotropin-releasing hormone (TRH), namely MK-771 and DN-1417, administered peripherally, on the actions of morphine and loperamide on gastrointestinal transit, was investigated in mice. The actions of naltrexone and methyl naltrexone on these effects were also determined in order to assess the central or peripheral mechanism of action. The administration of morphine sulfate (5 mg/kg) inhibited gastrointestinal transit, as measured by the charcoal meal test. The effect of morphine was potentiated by MK-771 and DN-1417 at the 10 mg/kg dose. The peripheral administration of DN-1417 inhibited gastrointestinal transit but MK-771 had no effect. Naltrexone antagonized the potentiating effect of the peptides on the effect of morphine on gastrointestinal transit. Methyl naltrexone, which crosses the blood-brain barrier with difficulty, also antagonized the potentiating effect of the peptides on the action of morphine on gastrointestinal transit. A subthreshold dose (0.5 mg/kg) of loperamide, a peripherally acting opiate, which had no effect on gastrointestinal transit by itself, when combined with MK-771 or DN-1417 significantly inhibited gastrointestinal transit. The administration of methyl naltrexone had little effect on loperamide-induced inhibition of gastrointestinal transit but antagonized the potentiating effect of MK-771 and DN-1417. It is concluded that the effects of analogs of thyrotropin releasing hormone on gastrointestinal transit involve peripheral sites of action, the effect of DN-1417 was not antagonized by naloxone and that the inhibitory effect of DN-1417 on gastrointestinal transit is not mediated by opiate receptors.     

The contribution of the mu- and delta-opiate receptors to the realization of the vagotropic action of met-enkephalin

In cat experiments the effect of methenkephalin on the heart rate, on the chronotropic effect of the vagus and its components--tonic and synchronizing was compared with the influence of the selective agonists and antagonists mu- and delta-opiate receptors. The influence of methenkephalin on the initial heart rate and the synchronizing component of the vagal chronotropic effect was found to be realized through excitation of the delta-opiate receptors. The modulating effect of methenkephalin on the expression of the inhibiting tonic action of the vagus was mediated both by the mu- and delta-opiate receptors.     

冬苓扶正液对氟尿嘧啶增效解毒作用研究

目的：研究冬苓扶正液与氟尿嘧啶(FU)配伍用对小鼠移植肿瘤S180、H222、Lewis的抑瘤作用及对FU所致小鼠免疫功能抑制的保护作用。方法：按照抗癌药物筛选规程进行体内抑瘤实验；采用FU制各免疫功能低下模型，测定冬苓扶正液与FU配伍用对小鼠白细胞计数、免疫器官重量、腹腔巨噬细胞吞噬功能的影响。结果：不同剂量的冬苓扶正液与FU配伍用均能明显提高FU对小鼠移植肿瘤S180、H22、Lewis的抑瘤率，其中高剂量组抑瘤效果最佳，配伍用又能明显拮抗FU所致白细胞下降、胸腺、脾脏萎缩及腹腔巨噬细胞功能降低等毒副作用。结论：冬苓扶正液与FU配伍用具有明显提高FU抗肿瘤及降低其毒性作用。     

野金柴提取物对心血管系统的作用

目的:考察野金柴提取物对心血管系统的作用。方法:分别通过耐缺氧实验、尾静脉注射垂体后叶素方法、耳廓微循环法、双肾双夹肾血管性高血压模型依次考察野金柴提取物的抗应激作用、对急性心肌缺血的保护作用、对微循环的作用和降压作用。结果:野金柴提取物组能延长缺氧小鼠的死亡时间,降低心肌缺血小鼠血清AST,CK及LDH-L水平,显著提高微循环灌注量,但对肾血管性高血压模型小鼠的降压效果不明显。结论:野金柴提取物对心血管系统有一定保护作用。     

Action of bombesin on the motility of the stomach

1. The tetradecapeptide bombesin was tested for its activity on the stomach in rats, dogs and men. On the rat stomach bombesin displayed a striking spasmogenic activity apparently independent from the autonomic nervous system. 2. In the dog the peptide was spasmogenic on the denervated Heidenhain pouch and the antrum. The inhibitory activity predominated on the innervated stomach and body fundus. 3. In man the peptide exerted a contracting effect on the antrum and the pylorus and an inhibitory effect on the stomach body and the fundus. In vitro studies performed on human stomach isolated strips showed a constant stimulant effect. 4. Apparently bombesin has a direct effect on the in situ rat stomach and on the isolated preparations, whereas it has an indirect effect on the other in situ innervated preparations.     

Effect of elymoclavine on open field behaviour of rats and pharmacological analysis of its catecholaminergic mechanisms

The effect of elymoclavine on rat open field behaviour was examined. The participation of catecholaminergic mechanisms in the elymoclavine effect on rat open field behaviour was also studied using pharmacological tools for analyzing these mechanisms. Elymoclavine in increasing doses stimulated ambulation and rearing but inhibited defecation. Haloperidol blocked the responses to all doses of elymoclavine. The effect of elymoclavine on ambulation was potentiated by propranolol, desipramine and pargyline. Its effect on rearing was reduced by desipramine, pargyline, alpha-methyl-p-tyrosine (alpha-MpT), L-DOPA, DDC (diethyldithiocarbamate) and 6-OHDA (applied intracerebroventricularly). The effect of elymoclavine on defecation was reduced only by DDC. It is concluded that elymoclavine influences both locomotor components of exploratory behaviour in the open field (ambulation and rearing) and defecation. These behavioural effects of elymoclavine are realized through the participation of central catecholaminergic mechanisms (dopaminergic and to a less extent noradrenergic).     

Investigations of central interaction of ethanol and clonidine

The combined effect of ethanol and clonidine on rabbit EEG, and the effect of clonidine on ethanol sleep in mice, as well as on acute ethanol toxicity were investigated. Moreover, the effect of clonidine on ethanol level in rabbit blood and in mouse brain and the combined effect of ethanol and clonidine on rabbit arterial blood pressure were evaluated. It has been found that clonidine intensifies the effect of ethanol in EEG and prolongs ethanol sleep. Clonidine does not change acute ethanol toxicity and does not affect ethanol level in blood and the brain. Ethanol prevents the decrease of arterial blood pressure after an intravenous or intracerebroventricular administration of clonidine.     

六月雪不同组分提取物的抗菌解热作用研究

目的研究六月雪不同组分提取物的抗菌解热作用。方法制备六月雪不同组分提取物,采用平皿法进行体外抑菌实验,并进行体内抗菌实验。考察六月雪不同组分提取物对干酵母所致大鼠发热以及内毒素所致家兔发热的解热作用。结果六月雪提取物对大肠杆菌、金黄色葡萄球菌、枯草杆菌、绿脓杆菌、肠炎球菌都有一定的抑制作用。水提取物各剂量组对绿脓杆菌所致的感染均可产生明显的对抗作用。六月雪水提取物对干酵母所致大鼠发热、内毒素所致家兔发热的解热作用最强。结论六月雪水提取物的抗菌解热活性最强。     

Effect of lysolecithin and lecithin of blood serum on the sensitivity of heart to acetylcholine

The chemical nature of the blood serum lipid substance exerting the cholinolytic effect upon the myocard of different animals was determined by means of column, thin-layer and gas-liquid chromatography. The cholinolytic effect was due to lysolecithin (lysophosphatidylcholine) action. The protective action of lecithin upon the cholinolytic effect of lysolecithin was established. Cholinolytic activity of deoxylysolecithin and its analogues on the isolated frog heart ventricle was studied. This effect was shown to depend specifically on the chemical structure of these substances.     

Intracellular coupling of prostaglandin inhibition of acid secretion in isolated rabbit gastric parietal cells.

Acid secretion from isolated rabbit gastric parietal cells can be stimulated by gastric secretagogues, histamine (cyclic-AMP pathway) and carbachol (inositol phosphate pathway). Prostaglandins (PG) from E series are potent inhibitors of acid secretion. The intracellular mechanism of this inhibition was examined by using a stable PGE1-analogue, misoprostol. Aminopyrine (AP) accumulations due to histamine, IBMX and forskolin were dose-dependently inhibited by misoprostol, whereas a weak but significant biphasic effect on carbachol-induced AP accumulation was observed. The cyclic-AMP formation induced by histamine and IBMX were also inhibited by misoprostol in a non-competitive way. The potent effect of forskolin on cyclic-AMP levels was not modified by misoprostol in parietal cells, whereas it was potentiated in non-parietal cells. The inhibitory effect of misoprostol on AP accumulation was reduced by incubation of parietal cells with Bordetella pertussis toxin (IAP) but not with Cholera toxin (CT). Pretreatment of the cells with IAP did not alter cyclic-AMP levels of resting and histamine-stimulated parietal cells but abolished the inhibitory effect of misoprostol. Treatment with CT increased basal and histamine-stimulated cyclic-AMP levels and masked the inhibitory effect of misoprostol. The biphasic effect of misoprostol on carbachol-stimulated AP accumulation in parietal cells was confirmed on carbachol-stimulated phospholipase C activity and on [Ca2+]i stimulated by carbachol. These data confirm a direct and specific effect of the prostanoid on the Gi-subunit of the adenylate cyclase coupled to the histamine H2-receptor, and a biphasic effect on the phospholipase C pathway of the parietal cells.     

前体对吸水链霉菌NND-52抗生素合成的调控

研究了不同前体对吸水链霉菌NND—52所产三种抗生素阿扎霉素B，除莠菌素A及nigericin的调控作用。且考察了NH4^ 对前体生成的影响，进一步探索了NH4^ 在NND—52抗生素合成中的调控作用，结果表明NH4^ 存在着阻遏与抑制缬氨酸脱氢酶的合成和活性的作用，从而抑制前体物质的合成，使抗生素产量降低。     

宫炎平片体内、外抑菌作用研究

目的观察宫炎平片对体内、外抑菌作用的影响。方法体外抑菌试验选用可定量、敏感性较高的液体试管法进行及动物体内抑菌法。结果体外抑菌宫炎平片对所试菌种,均有不同程度的抑菌作用。其中对金黄色葡萄球菌、乙型溶血性链球菌和福氏志贺氏菌、绿脓假单胞菌的作用较强。体内抑菌宫炎平高、中、低剂量组对乙型溶血性链球菌感染小鼠均有明显预防和治疗作用（P〈0．05）,宫炎平高剂量组对金黄色葡萄球菌感染小鼠均有一定的保护作用。结论宫炎平片对乙型溶血性链球菌在体内有明显的抗菌作用。     

蒜莲胶囊的药理作用

目的：研究蒜莲胶囊的抗菌、抗炎、镇痛及止泻作用。方法：用体外抗菌试验研究蒜莲胶囊的抗菌作用，用二甲苯法研究对小鼠的抗炎作用，用扭体法研究对小鼠的镇痛作用，通过蒜莲胶囊对小鼠胃肠道推进率的影响来研究其止泻作用。结果：蒜莲胶囊对痢疾杆菌、伤寒杆菌作用最强，对大肠杆菌与变形杆菌次之，肿胀抑制率较高，镇痛率为72．34％，肠推进率与对照组相比差异有显著性。结论：蒜莲胶囊具有一定的抗菌、抗炎、镇痛及止泻作用。     

Time course of the effect of insulin on bovine mesenteric artery

The time course for the effect of insulin on the bovine mesenteric artery, a medium sized artery with a high content of smooth muscle, was studied. The arteries were preincubated for varying times (0--180 min.) with and without insulin. The magnitude of the insulin effect, subsequently assayed on the accumulation of glucose carbon and the distribution of 3-0-methylglucose, was found to increase with the time of prior exposure to insulin, approaching a maximum after about 120 min. Insulin exposure also augmented its effect on the incorporation of leucine-14C into protein in a similar way. Preincubation without insulin had no appreciable influence on the magnitude of the insulin effect, indicating that the sensitivity to the hormone did not change with time. The threshold concentration for the effect of insulin on glucose-14C accumulation was 0.01 U/ml without preincubation and 0.001 U/ml after prior exposure to the hormone for 180 min. An action on protein synthesis may be involved in the increase in the magnitude of the insulin effect caused by prior exposure to insulin since no increase was found after inhibition of protein synthesis by puromycin.