N－（4－乙氧苯基）苯甲酰胺类化合物的合成及抗炎、抗变态反应活性研究

Ｎ┐（４┐乙氧苯基）苯甲酰胺类化合物的合成及抗炎、抗变态反应活性研究周玉新１）党永红刘建飞２）徐颖刘百里（沈阳药科大学制药系，沈阳１１００１５）郑文义（东北第六制药厂，沈阳１１００４３）１９８１年，刘百里等〔１，２〕发现和研制的新药益肤酰胺，经药理实...     

拜虫杀和杀飞克对3种卫生害虫的药效报告

本文报道了两种菊酯类卫生杀虫剂，在不同载体表面对３种卫生害虫的触杀试验。结果：（１）拜虫杀在玻璃板面上６．２５ｍｇ／ｍ２时对家蝇速效ＫＴ（５０）为３．３ｍｉｎ；淡色库蚊为４．３ｍｉｎ；持效均达４９天；对德国小蠊ＫＴ（５０）为５．６ｍｉｎ，持效４２天。在木板表面１２．５ｍｇ／ｍ２时，对家蝇速效ＫＴ（５０）为４．３ｍｉｎ，对淡色库蚊为４．６ｍｉｎ，对前者持效４９天，后者４２天。对德国小蠊ＫＴ（５０）为４．９ｍｉｎ，持效３５天。在水泥板面２５ｍｇ／ｍ２时，对家蝇速效ＫＴ（５０）为４／ｍｉｎ，对淡色库蚊为５．０ｍｉｎ，前者持效３５天，后者４２天。对德国小蠊速效ＫＴ（５０）为６．４ｍｉｎ，持效２１天。（２）杀飞克在玻璃面上７．５ｍｇ／ｍ２时，对家蝇速效ＫＴ（５０）为３．７ｍｉｎ，对淡色库蚊为５．１ｍｉｎ，持效均达４９天。在木板面上１５ｍｇ／ｍ２时，对家蝇速效ＫＴ（５０）为４．２ｍｉｎ，对淡色库蚊为６．０ｍｉｎ，对前者持效４９天，后者为４２天。在水泥板面３０ｍｇ／ｍ２时，对家蝇速效Ｋｔ（５０）为４．４ｍｉｎ，对淡色库蚊为５．０ｍｉｎ，对前者持效３５天，后者４２天；对德国小蠊速效ＫＴ（５０）为６．４ｍｉｎ，持效２１天。     

Evaluation of monoclonal anti-D reagents using D variant cells

Monoclonal anti-D antibodies submitted to the Third Monoclonal International Workshop were evaluated against a number of D variant cells using standard serological techniques. The monoclonal antibodies were able to discriminate between the cells of Categories Va, VI and DFR but not Category III cells. Cells within each category did not give any aberrant results. The Rh:33 cells behaved as normal Rh(D) positive cells.     

P_（53）基因在乳腺癌细胞中异常表达的观察

Ｐ５３基因是一种重要的抑癌基因，它的突变和异常表达，与癌细胞的发生、发展密切相关。本文应用免疫组化ＡＢＣ法检测了５８例乳腺癌石蜡标本中Ｐ５３表达状况。结果表明：Ｐ５３基因异常表达为３９．７％（２３／５８）。并与肿瘤的分化程度、区域淋巴结转移和性激素受体有明显相关性，与乳腺癌患者术后五年生存率有一定关系。     

细小病毒H－1对正常仓鼠肝细胞DNA周期动力学的影响

健康成年金黄仓鼠腹腔内接种ＰＶＨ－１（５×１０６ｐｆｕ），ＦＣＭ动态检测肝细胞ＤＮＡ周期动力学变化，结果显示：ＰＶＨ－１接种后处于Ｇ０＋Ｇ１期的肝细胞与对照组动物相比无显著差异。Ｓ期肝细胞在第３天显著高于对照组动物（Ｐ＜０．０５），且在第７天时仍呈上升趋势，第１４天到３０天趋于正常水平。Ｇ２＋Ｍ期肝细胞在ＰＶＨ－１接种后第３０天升高（Ｐ＜０．０５）。结果提示，动物在ＰＶＨ－１接种后第３到第７天是病毒在肝细胞中的复制高峰，并阻滞仓鼠处于Ｓ期肝细胞分裂进入Ｇ２＋Ｍ期，但是这种阻滞作用较短暂、并可逆，在ＰＶＨ－１接种后１４～３０天自然消失。     

5-HT1A receptor agonists: recent developments and controversial issues

During the last decade, serotonin (5-HT)_1A receptors have been a major target for neurobiological research and drug development. 5-HT_1A receptors have been cloned and a variety of selective agonists, such as the aminotetraline 8-OH-DPAT and the pyrimidinylpiperazine ipsapirone, have become available. Demonstrations of apparent intrinsic activity of these ligands at 5-HT_1A receptors, however, depend highly on the particular assay system. This may be due to the possible existence of receptor subtypes and to assay (or brain region)-dependent differences in receptor reserve and the nature of receptor-effector coupling. Nevertheless, the apparent intrinsic activity of 8-OH-DPAT seems to be higher (although possibly not yet maximal) than that of the pyrimidinylpiperazines. In the brain, 5-HT_1A receptors are located presynaptically as somatodendritic receptors on 5-HT neurons and postsynaptically in particular limbic and cortical regions. Although it is generally accepted that presynaptic 5-HT_1A receptors control 5-HT neuronal activity, recent evidence suggests an additional role of postsynaptic 5-HT_1A receptors in cortex as part of a negative feedback loop. Anxiolytic and antidepressive properties of selective 5-HT_1A receptor agonists have now been confirmed by clinical studies. Although it is well established that the latter properties depend on theagonistic activity of these compounds, theoptimal level of intrinsic activity is still a matter of debate and may be dependent on the clinical indication. Such compounds may also have antiaggressive effects, and possibly anticraving effects (manifested by their alcohol intake-reducing effects in dependent animals), but the specificity of these so-called anti-impulsivity effects is still controversial and not yet tested clinically. Anticataleptic, antiemetic and neuroprotective properties have been demonstrated in different species. Behavioral studies on the mechanisms underlying the anxiolytic and antidepressive effects have examined the relative contribution of pre-and postsynaptic 5-HT_1A receptors by means of local cerebral application and lesion techniques. Most evidence points towards a critical involvement of presynaptic receptors in the anxiolytic effects of 5-HT_1A receptor agonists (although a possible contribution of postsynaptic receptors cannot be excluded). With regard to the antidepressive properties, a case can be made for the reverse; i.e., a strong involvement of postsynaptic receptors and a questionable contribution of presynaptic receptors. However, as the therapeutic effects of those 5-HT_1A receptor (partial) agonists which have been tested clinically require repeated administration, attention has been directed increasingly towards chronic studies. These studies have shown that a number of electrophysiological, biochemical, behavioral and endocrinological 5-HT_1A receptor-related events adapt differentially to repeated or sustained administration. Thus, several hypotheses accounting for the delayed onset of action have been advanced. Among these, time-dependent downregulation /desensitization of eitherpre- orpostsynaptic 5-HT_1A receptors, or cortical 5-HT₂ receptors have received much attention. However, these hypotheses have their weaknesses, and it is argued thatfunctional sensitization of particular postsynaptic 5-HT_1A receptor-mediated events remains a valuable alternate hypothesis. Basic research on the role of 5-HT_1A receptors in psychopathology and in the therapeutic effects of clinically effective therapeutics, as well as on the mechanism of action of 5-HT_1A receptor ligands, will enable rational design of ligands with particular profiles of intrinsic activity at different 5-HT_1A receptor populations, and may contribute to a more efficient treatment of a multiplicity of brain disorders.     

EndocrinologyHormonal profile during the follicular phase in cycles stimulated with a combination of human menopausal gonadotrophin and gonadotrophin-releasing hormone antagonist (Cetrorelix)

A third-generation gonadotrophin-releasing hormone antagonist(Cetrorelix) was used during ovarian stimulation in 32 patientsundergoing assisted reproduction, in order to prevent the prematureluteinizing hormone (LH) surge. In all patients, ovarian stimulationwas carried out with two or three ampoules of human menopausalgonadotrophin (HMG), starting on day 2 of the menstrual cycle.In addition, 0.5 mg of Cetrorelix was administered daily fromday 6 of HMG treatment until the day of ovulation inductionby human chorionic gonadotrophin (HCG). A significant drop inplasma LH concentration was observed within a few hours of thefirst administration of Cetrorelix (P<0.005). Moreover, noLH surge was detected at any point in the treatment period inany of the 32 patients. A mean oestradiol concentration of 2122±935ng/1 was observed on the day of the HCG administration, indicatingnormal folliculogenesis. Like LH, progesterone concentrationalso dropped within a few hours of the first administrationof Cetrorelix (P< 0.005). A 0.5 mg daily dose of Cetrorelixprevented a premature LH surge in all the 32 patients treated.     

云南水族人群红细胞酸性磷酸酶多态分布

采用淀粉凝胶电泳法对云南水族人红细胞酸性磷酸多态分布状况进行了调查，检出ＥＡＰＡ型６例，ＥＡＰＢＡ型４５例，ＥＡＰ５５例。计算出基因频率分别为：ＥＡＰ＾Ａ０．２６８９，ＥＡＰ＾Ｂ０．７３１１．ＥＡＰ在云南水族人群中的ＤＰ值为０．５１８５。文中对ＥＡＰ在不同人群中的分布进行了比较分析。     

枸杞地黄汤改善老年小鼠记忆障碍和自由基、免疫系统异常改变

目的：研究枸杞地黄汤对老年小鼠学习记忆、自由基及免疫系统的影响。方法：采用水迷宫行为实验检测枸杞地黄汤对老年小鼠学习记忆的影响，通过测定皮层、海马中MDA和SOD水平检测药物对老年小鼠自由基系统异常改变的影响，通过测定老年小鼠免疫器官指数变化检测药物对老年免疫系统异常改变的影响。结果：5、10、20g／kg的枸杞地黄汤不同程度减小老年小鼠学习记忆障碍，降低皮层、海马中MDA水平，增加SOD活性，提高胸腺、脾指数。结论：枸杞地黄汤能够改善老年小鼠学习记忆障碍．调节不正常自由基系统和免疫系统。     

亚麻子对鸡蛋黄及鸡体内DHA含量的影响

为了研究亚麻子对鸡蛋黄以及鸡体内二十二碳六烯酸 (DHA)含量的影响 ,用添加亚麻子的饲料喂养蛋鸡(剂量组 ) 1 0周后 ,用气相色谱法检测鸡蛋黄和鸡体内DHA的含量。结果显示 ,与对照组相比 ,剂量组鸡蛋黄中α 亚麻酸 (ALA)和DHA的含量呈明显上升趋势 ,并发现剂量组蛋鸡的肝脏、脑中DHA含量也相应增加。提示亚麻子对于开发新型的保健食品具有一定价值