Interaction of antipsychotic drugs with neurotransmitter receptor sites in vitro and in vivo in relation to pharmacological and clinical effects: role of 5HT2 receptors

In the introductory section an overview is given of the strategies which have been proposed in the search for side-effect free antipsychotics. Special attention is paid to the role of predominant 5HT₂ receptor blockade over D₂ blockade. Whereas D₂ receptor blockade seems to be essential for the treatment of positive symptoms of schizophrenia, it also underlies the induction of extrapyramidal side effects (EPS). Predominant 5HT₂ receptor blockade may reduce the EPS liability and can ameliorate negative symptoms of schizophrenia. We further report a nearly complete list of neuroleptics that are on the European market and eight new antipsychotics that recently entered clinical trial, 5HT₂ and D₂ receptor binding affinity (K_i values) and the rank order in affinity for various neurotransmitter receptor subtypes are also discussed. For the eight new antipsychotics and for six reference compounds the complete receptor binding profile (including 33 radioligand receptor binding and neurotransmitter uptake models) is reported. Furthermore, for a series of 120 compounds the relative affinity for D₂ receptors and D₃ receptors (a recently cloned new dopamine receptor subtype) is compared. Finally, original findings are reported for the new antipsychotic risperidone and for haloperidol and clozapine on the in vivo occupation of neurotransmitter receptors in various brain areas after systemic treatment of rats or guinea pigs. The receptor occupation by the drugs was measured ex vivo by quantitative receptor autoradiography. The receptor occupancy was related to the motor activity effects of the test compounds (measurements were done in the same animals) and to the ability of the drugs to antagonize various 5HT₂ and D₂ receptor mediated effects. With risperidone a high degree of central 5HT₂ receptor occupation was achieved before other neurotransmitter receptors became occupied. This probably co-underlies the beneficial clinical properties of the drug. Antagonism of the various D₂ receptor-mediated effects was achieved at widely varying degrees of D₂ receptor occupancy, from just about 10% to more than 70%. For therapeutic application it may be of prime importance to carefully titrate drug dosages. Antipsychotic effects may be achieved at a relatively low degree of D₂ receptor occupancy at which motor disturbances are still minimal. With drugs such as risperidone that produce shallow log dose-effect curves, differentiation between the various D₂ receptor mediated effects may be made more easily, allowing EPS-free maintenance therapy of schizophrenic patients.     

重度脑出血患者家属伦理行为的临床研究

目的：研究重度脑出血患者家属的伦理行为，对防止无过失医疗纠纷有积极意义。方法：对128例重度脑出血患者家属的伦理行为进行调查研究。结果：发现具有明显的三期特征：焦虑期、幻想期和绝望期。结论：对家属处在不同伦理时期患者采取不同的救治方法和态度能有效避免无过失医疗纠纷。     

不同强弱刺激对痛痹患者肢体血流图的影响

目的:探讨不同强度针刺刺激量对痛痹患者肢体血流图的影响。方法:选择以寒邪为主的下肢痛痹病人41例,在患肢悬钟针刺得气后行捻转手法,通过同一病人强、弱刺激后观察患侧肢体血流图,计算波幅值以做比较。结果:强刺激针后使波幅下降,弱刺激针后使波幅上升。结论:不同刺激量可以引起患肢血管舒缩机能截然不同的规律性反应。     

甲状腺乳头状癌与桥本甲状腺炎关系的免疫组化研究

目的探讨甲状腺癌与桥本甲状腺炎的关系。方法对27例甲状腺乳头状癌（7例合并桥本甲状腺炎）应用S—P法检测甲状腺癌细胞与HT中增生滤泡上皮中P53、C-erbB-2及PCNA的表达情况。结果癌细胞P53阳性23例（85．19％），C-erbB-2阳性21例（77．78％），PCNA高表达26例（96．3％）。HT增生滤泡上皮P53阳性5例（71．43％），C-erbB-2阳性4例（57．14％），PCNA高表达7例（100％）。结论HT中滤泡上皮增生属于异型增生，与癌细胞有一定的相关性，可视为癌前病变。     

医药产业发展与经济发展关系研究

目的:揭示国家(和地区)医药产业发展与经济发展的关系。方法:采用不同经济发展阶段的多个国家(和地区)同一时点医药产业发展的截面数据,拟合医药产业在不同经济发展时期的成长轨迹。结果与结论:医药市场销售额与国内生产总值(GDP)呈正相关,医药产业发展在人均GDP低于2500美元、2500～5000美元和5000美元以上时分别呈现明显的高速、缓慢、较高速增长的阶段性特征。     

Development of activation and rise of tension in an isometric tetanus

The force-velocity relation was determined at preset times after the beginning of the stimulus volley, either at low isometric tensions, during the raising phase of tetanus and the recovery after a quick release imposed at the plateau, or at the steady state. It is concluded that the characteristics of the force-velocity relation may be used to express the actual level of activation at any time during the contractile process and that the mechanical output of frog twitch muscle fibres implies two distinct steps: (i) activation of the contractile machinery; (ii) production of force.     

再论“证”与病理过程的相关关系

追踪近 2 0余年来关于中西医结合的途径与方法 ;论述了中医在医学史上的特殊地位 ,以及现代医学模式对中医“自然整体医学模式”的挑战 ;在中西医结合研究中主张“拿来主义” ,即把现代医学关于“病理过程”的研究成果拿来 ,作为中医的“证”所由产生的内在根据 ;提出了一个新的医学命题 ,即“证与病理过程相关” ;将中西医结合进程设想为“并轨”、“入网”及“定位”3个步骤。     

针刺与运动疗法不同干预次序组合对卒中偏瘫患者即时SEP波幅的影响

目的:观察不同疗法间干预次序组合对疗效的影响。方法:将卒中偏瘫康复期患者分为先电针患侧曲池合谷、后Bobath握手上举运动组,先Bobath握手上举运动、后电针患侧曲池合谷组,记录并比较患侧半球体感诱发电位(SEP)的变化情况。结果:①单纯电针或运动都能提升患侧SEP波幅,与针刺或运动前比较差异有非常显著性意义(P<0·01),而且二者之间的升幅比较无明显差异(P>0·05);②先针刺后运动组或先运动后针刺组不仅与治疗前差异有非常显著性意义(P<0·01),且这两组间的波幅差值也有非常显著性意义(P<0·01)。结论:在脑卒中患者的恢复期,电针及运动疗法均可即刻改善患侧SEP,但电针及运动疗法二者不同干预次序的组合对患侧SEP的影响不同,以先针刺后运动组合对脑卒中患者脑功能改善更有利。     

心室复极化时程变异的谱分解技术及其临床应用

当今,心血管疾病发病率日益增加,研究者业已致力于从心曜误事 提取对心脏疾病能早期诊断、监护及预后评估有价值的信息。心室肌发生病变时,心室复极化时程与ＲＲ间期的关系会发生相应变化。且具有明显的特征性。因此有必要建立心室极化时程与ＲＲ间期关系所分析方法,以便对心室复极化时程的生理机抽进一步深入研究,并最终为心血管疾病的诊治提供新的无创性的方法。我们利用系统辨识方法建立了心室复极化时程的ＲＲ间期系统的动态线性参数模型,利用功率谱分解技术把心室复极化时程的功率谱分解成与生理因素有关和与病理因素有关两种成分,定量描述心肌细胞的受损程度。我们开展了这方面的临床研究工作,分别研究正常人各年龄组间以及正常人（老年组）和病人（老年组）间相应指标的变化。对缺血性心脏病人的研究结果表明,在心室复极化时程变异的功率谱中,与病理因素有关的成分显著增大;而且反映心脏病人心肌细胞状态不可测因素（病理因素）的有色随机噪声的能量亦显著增大。心室复极化时程与ＲＲ间期关系的分析方法,具有无创性和可定量性。随着心室复极化时程与ＲＲ间期关系研究的不断深入,将评价心血管疾病和功能的无创性方法日臻完善,必将对临床心血管疾病的早期诊断、治疗和预后评估等发挥积极的作用。     

Anatomic variation of the relation between the facial nerve and the retromandibular vein during superficial parotidectomy: A rare case report

IntroductionIdentification and preservation of the facial nerve (FN) is a major challenge when performing parotidectomy. Anatomic variations of the relation between the FN and the retromandibular vein (RMV) pose a high risk of nerve injury and bleeding during the operation.Presentation of caseAn unusual anatomic variation of the relation between the FN and the RMV was unexpectedly detected during superficial parotidectomy. The operation was uneventful. A meticulous review of the recent literature was conducted as well.DiscussionVariations of the relation between the FN and the RMV are mainly identified during the operation, since when performing parotidectomy, surgeons typically detect all the FN branches by locating the RMV. Such kind of variations, are not as rare as considered and their presence complicates parotid surgery and increases the potentiality of nerve injury and hemorrhage.ConclusionSurgeons’ deep knowledge and perpetual awareness concerning the probable anatomic variations of the relation between the FN and the RMV combined with detailed exposure of the operative field and of the relationship between these adjacent anatomical structures lead to safe parotid surgery.