Discriminative stimulus properties of the serotonin agonist MK 212

In an attempt to clarify the role of 5-hydroxytryptamine (5-HT) in the discriminative stimulus properties of MK 212 (6-chloro-2[1-piperazinyl]pyrazine), male Sprague-Dawley rats were trained to discriminate 0.5 mg/kg of this compound from saline. While the putative 5-HT agonists fenfluramine and m-chlorophenylpiperazine (MCPP) mimicked MK 212 in a dose-related manner, d-lysergic acid diethylamide (LSD), 8-hydroxy-2(di-n-propylamino)tetralin (8-OHDPAT), 5-methoxy-N,N-dimethyltryptamine (5-MeODMT), quipazine, Ru 24969, and 1-(m-trifluoromethylphenyl)piperazine (TFMPP) failed to substitute completely. The 5-HT₁/5-HT₂ antagonists BC 105, metergoline, and methysergide completely blocked the MK 212 cue, while the selective 5-HT₂ antagonists ketanserin and pirenperone, the dopamine antagonists haloperidol and spiperone, and the beta-noradrenergic antagonist propranolol were without effect. The substitutions of fenfluramine and MCPP for MK 212 support a role for 5-HT in the MK 212 cue; however, the lack of substitution of many other 5-HT agonists is difficult to explain. The complete antagonism by 5-HT₁/5-HT₂ but not by selective 5-HT₂, antagonists suggests the possibility that 5-HT₁ receptors mediate the stimulus properties of MK 212. Further research is needed to support this hypothesis and to investigate the relative role of 5-HT and other neurotransmitters in the stimulus effects of MK 212.Portions of this research were presented at the Meeting of the Committee on Problems of Drug Dependence Satellite Session (International Study Group Interested in Drugs as Reinforcers and the Society for the Stimulus Properties of Drugs) in Baltimore, MD (1985)     

应用3H-TdR掺入法对SMMC-7721细胞株药敏试验条件的探讨与应用

目的探讨3H-TdR掺入法在进行SMMC-7721系细胞肿瘤药敏试验实验时的最佳实验条件.方法确定出3H-TdR掺入法药敏实验时的最适细胞浓度、最适实验药物浓度、3H-TdR掺入最适时间;在最适条件下采用3H-TdR掺入法测定肝癌SMMC-7721细胞株对临床常用的9种抗癌药物的敏感性.结果应用3H-TdR掺入法检测肝癌SMMC-7721细胞株药敏试验的最适实验细胞浓度为1×104个/孔,最适试验药物浓度为1×PPC,3H-TdR最适掺入时间为收集细胞前8 h;肝癌SMMC-7721细胞株对DDP、ADM、5-FU、CPT高度敏感,对MTX、VP-16、MMC、NVB低度敏感,对PYM不敏感.结论 3H-TdR掺入法可用于肿瘤药物敏感性测定并确定出它的最适实验条件.     

益肾化浊注射液对慢性肾功能衰竭大鼠残余肾中细胞因子含量的影响

通过观察益肾化浊注射液对5／6肾切除大鼠残余肾中细胞因子含量的影响，益肾化浊注射液延缓慢性肾功能衰竭（CRF）模型大鼠肾功能减退的作用机理。结果显示：益肾化浊注射液可以降低5／6肾切在鼠血清肌,尿素氮（P＜0．01），下调肾组织中白细胞介素－1（IL－1）（P＜0．05），白细胞介素－8（IL－8）（P＜0．05）及肿瘤坏死因子（TNF）（P＜0．05）的总体水平，说明益肾化浊注射液可以通过下调5／6肾切除大鼠残余肾中相关细胞因子含量，抑制促炎细胞因子对肾脏的损害，从而延缓CRF的进展。     

泌尿系感染病原菌的变迁及耐药性分析

目的了解近年来泌尿系感染病原菌的变迁及耐药现状. 方法应用回顾性调查分析方法,对我院1997至2000年间泌尿系感染检测的1 026株病原菌的分布及耐药性进行统计分析. 结果在泌尿系感染的病原菌中,G+球菌上升,G-杆菌下降,真菌上升,其中粪肠球菌上升和变形菌属下降差异有显著性(P<0.05),药敏实验结果对以往常用的抗菌药物青霉素类、复方新诺明、红霉素、诺氟沙星及一代头孢显示较高的耐药性,2000年耐药率>81.6%,对三代头孢、环丙沙星、庆大霉素呈中度耐药,耐药率在42.9%～78.3%,对阿米卡星及头孢哌酮/舒巴坦呈轻度耐药,耐药率<36.7%. 结论随着抗生素的更新换代、人口老龄化及医院感染等因素的变化,泌尿系感染病原菌的分布及耐药性均发生了变迁.     

Cough and converting enzyme inhibitors

Persisting cough developed in three children treated with converting enzyme inhibitors. The symptoms disappeared within 3–7 days after withdrawing medication. These observations in children complement previous reports in adults and indicate that cough may be induced by treatment with these agents.     

假腔内注射凝血酶治疗股动脉假性动脉瘤(附6例临床分析)

目的：探讨超声引导下假腔内注射凝血酶对股动脉假性动脉瘤的治疗效果。方法：对本科1999年9月－2002年8月行心脏介入诊疗后并发的6例右侧股动脉假性动脉瘤进行假腔内凝血酶注射治疗，并对其结果进行了分析。结果：6例患者均即刻治疗成功，未见明显并发症，随访30d无复，结论：假腔内注射血酶是一种安全，简便，快速，耐受性佳，经济和有效的治疗股动脉假性动脉瘤的方法。     

Olfactory Absorption of Insulin to the Brain

A vast number of potent neuropharmaceuticals, many of which are peptides, are excluded from entry into the brain because of the highly selective blood-brain barrier. The fact that a number of drugs have been shown to be transported directly to the central nervous system following application to the olfactory region of the nose is therefore of major interest. In the present study, the feasibility of delivering peptides to the brain via the olfactory route was assessed using insulin as a model peptide. Systemic hyperinsulinemia induced by subcutaneous injection did not significantly reduce the amount of ¹²⁵I-insulin transported from the nose to the brain in vivo, which suggests that the impact of systemic absorption on drug transport is minimal. A linear relationship was seen between insulin accumulation in the brain and the dose applied, without any relevant saturation. Contrary to what was expected, both systemic and olfactory absorption of insulin was enhanced when the pH of the medium was near the isoelectric point. The amount absorbed to the brain was found to be linearly related to the net charge of the molecule (r = -0.61; n = 20). It was concluded that insulin gains access to the central nervous system from the olfactory region of the nose by a nonspecific pathway. The olfactory route may therefore become an important means to deliver peptides to the brain.     

Local analgesic and vascular effects of intradermal ropivacaine and bupivacaine in various concentrations with and without addition of adrenaline in man

Ropivacaine, a new long–acting amino–amide local anaesthetic agent, and bupivacaine, in various concentrations with or without addition of adrenaline, were tested in a randomized, double–blind study using intradermal wheals. Ten non–smoking, healthy, young male volunteers participated. In series I plain solutions of ropivacaine (0.25%, 0.5%, 0.75% and 1%) and bupivacaine (0.25%, 0.5% and 0.75%) were injected intradermally and in series II the same concentrations, with the addition of adrenaline 5 ug ml^-1 ( 1 :200 000), were used. The same volunteers took part in both series, with an interval of at least three weeks between the experiments. Saline was included as control in both series. Pin–pricking was used to assess the dermal analgesia. Plain solutions of ropivacaine produced significantly longer durations of dermal analgesia than did plain solutions of bupivacaine, in all tested concentrations. A significant increase in duration was seen for both local anaesthetics when adding adrenaline. Local vascular effects at the injected areas were determined by visual inspection (nil, pink, pale). Local blanching (pale) was significantly more frequent for plain solutions of ropivacaine, in all tested concentrations. Local redness (pink) was significantly more frequent with plain bupivacaine, in a dose–dependent relation. An initial redness was frequently observed for both local anaesthetics containing adrenaline, followed by blanching at most sites.     

四季鹅下丘脑单位放电的研究

实验利用慢性微电极技术观察了清醒活动四季鹅(产蛋期鹅和休产期鹅)下丘脑细胞自发放电及第Ⅱ脑室注入去甲肾上腺素(NE)对单位放电的影响.结果表明无论是产蛋期鹅还是休产期鹅.其下丘脑放电均以中频为主,但产蛋期鹅高频放电高于休产期鹅.放电有单个连续、束状、组群式等3种形式,无论是产蛋期鹅还是休产期鹅,其下丘脑均以单个连续放电为主,但产蛋期鹅组群式放电高于休产期鹅.第Ⅱ脑室注入NE后,75%的单位放电数增加,25%的单位放电数减少.     

提高抗肝癌药物的肝脏浓度并降低心脏,血液浓度的实验研究

实验研究结果表明：阿霉素（ＡＤＭ）在采用推进法注射时，经肝血管或外周静脉途径二者的肝、心与血液浓度均无显著差别．如采用控速缓慢输注法，则经肝血管较经外周静脉在提高肝脏浓度方面具有显著效果，心脏内浓度也有一定程度降低。如在肝血管内输注时与血液净化联合应用，则更能提高上述要求。以上结果将为临床抗癌药介入治疗应用方法的开展提供依据和参考价值。