缬沙坦逆转高血压患者左心室肥厚的临床观察

目的: 观察血管紧张素 Ⅱ受体拮抗剂 ———缬沙坦(代文) 的降压效果及其对高血压病合并左室肥厚的影响。 方法: 对 32 例轻、中度高血压病左心室肥厚患者进行 6 mon 的缬沙坦治疗, 通过治疗前后对血压、超声多普勒心动图检测的对比, 探讨缬沙坦对逆转左室肥厚的作用。结果: 经过 6 mon 的治疗, 血压从 162/102 mmHg 降至 135/84 mmHg(P <0.01), 左室心肌重量指数(LVMI) 也明显下降(P <0.01)。 结论: 缬沙坦长期治疗可使高血压患者左室肥厚逆转。     

Blockade of the serotonin 5-ht2a receptor suppresses cue-evoked reinstatement of cocaine-seeking behavior in a rat self-administration model.

The serotonin 5-HT2A receptor (5-HT2AR) may play a role in reinstatement of drug-seeking. This study investigated the ability of a selective 5-HT2AR antagonist to suppress reinstatement evoked by exposure to cues conditioned to cocaine self-administration. Cocaine self-administration (0.75 mg/kg/0.1 mL/6 s infusion; FR 4) was trained in na?ve, free-fed rats to allow interpretation of results independent from changes related to food deprivation stress. Pretreatment with the selective 5-HT2AR antagonist M100907 (volinanserin) failed to reduce rates of operant responding for cocaine infusions. On the other hand, M100907 (0.001–0.8 mg/kg ip) significantly suppressed the cue-induced reinstatement of cocaine-seeking behavior following extinction; effective M100907 doses did not alter operant responding for cues previously associated with sucrose self-administration. Importantly, a greater magnitude of active lever presses on the initial extinction session (high extinction responders) predicted the maximal susceptibility to M100907-induced suppression of cue-evoked reinstatement. The findings indicate that blockade of the 5-HT2AR attenuates the incentive-motivational effects of cocaine-paired cues, particularly in high extinction responders, and suggests that M100907 may afford a therapeutic advance in suppression of cue-evoked craving and/or relapse. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Model for the complex between the insulin-like growth factor I and its receptor: towards designing antagonists for the IGF-1 receptor

The type-1 insulin-like growth factor receptor (IGF-1R) is the cognate tyrosine kinase receptor for the insulin-like growth factor IGF-I and is expressed widely in many foetal and postnatal tissue cells. IGF-1R is overexpressed in a number of human tumour types and is a valid target for anti-cancer therapeutic efforts. Designing antagonists for IGF-1R would be greatly facilitated by the availability of structural information on the complex between IGF-I and IGF-1R. In the present work we model the three-dimensional structure of the complex between IGF-I and the first three domains of IGF-1R using a macromolecular docking method guided by selected experimental data. Interface metrics indicative of the binding affinity and reliability of the model are computed and compared with other biomolecular complexes. This model is consistent with experimental chimerical and mutagenesis data, provides a structural basis for understanding the primary interaction of IGF-I with its receptor and facilitates design of antagonist ligands.     

活性氧影响拮抗菌及果蔬采后抗病性的研究进展

活性氧引起的氧化胁迫作用作为生防系统中常见的影响因素引起了广泛的关注。活性氧作为生物体内的必须物质,是维持生命活动必不可少的内源性成分;但当其过量时,会损害大分子蛋白、核酸等有害物质,又必须被有效地清除。因此如何利用活性氧在生物防治系统中的重要作用是提高生防效果的方法之一。本文通过介绍活性氧的产生以及清除,系统地阐述了活性氧-氧化胁迫,氧化胁迫-拮抗菌以及氧化胁迫-果蔬之间的相互作用,并论述活性氧对拮抗菌生防能力以及果蔬抗病性带来的积极、消极作用,进一步探讨相关作用对于生防效果的影响。     

孟鲁司特治疗老年稳定期慢性阻塞性肺疾病患者的疗效分析

目的: 评价孟鲁司特治疗老年稳定期中重度慢性阻塞性肺疾病(COPD)患者的疗效及安全性。方法: 60例男性稳定期中重度COPD患者随机分为治疗组和对照组,在规则吸入布地奈德联合福莫特罗(信必可都保)的基础上,治疗组加服孟鲁司特,疗程6个月。比较两组患者治疗前后基础呼吸困难指数(BDI)、圣乔治呼吸问卷(SGRQ)评分、肺功能、诱导痰细胞分类及白三烯B₄(LTB₄)水平。结果: 47例患者完成试验,期间未发生孟鲁司特相关严重药物不良反应。两组患者经治疗后BDI均升高,SGRQ评分及诱导痰中性粒细胞百分比均下降(P<0.05),但肺功能均无明显改善(P>0.05)。与对照组相比,治疗组患者诱导痰中嗜酸性粒细胞百分比下降,且BDI、SGRQ评分、诱导痰LTB₄水平的改善作用更明显,两组改善率差异有统计学意义(P<0.05) 。结论: 孟鲁司特作为老年稳定期中重度COPD患者的补充治疗安全有效。     

Evidence That GABA Mediates Dopaminergic and Serotonergic Pathways Associated With Locomotor Activity in Juvenile Chinook Salmon (Oncorhynchus tshawytscha).

The authors examined the control of locomotor activity in juvenile salmon (Oncorhynchus tshawytscha) by manipulating 3 neurotransmitter systems--gamma-amino-n-butyric acid (GABA), dopamine, and serotonin--as well as the neuropeptide corticotropin releasing hormone (CRH). Intracerebroventricular (ICV) injections of CRH and the GABAA agonist muscimol stimulated locomotor activity. The effect of muscimol was attenuated by administration of a dopamine receptor antagonist, haloperidol. Conversely, the administration of a dopamine uptake inhibitor (4′,4″-difluoro-3-alpha-[diphenylmethoxy] tropane hydrochloride [DUI]) potentiated the effect of muscimol. They found no evidence that CRH-induced hyperactivity is mediated by dopaminergic systems following concurrent injections of haloperidol or DUI with CRH. Administration of muscimol either had no effect or attenuated the locomotor response to concurrent injections of CRH and fluoxetine, whereas the GABAA antagonist bicuculline methiodide potentiated the effect of CRH and fluoxetine. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

More Rare Males in <Emphasis Type="Italic">Ostrinia</Emphasis>: Response of Asian Corn Borer Moths to the Sex Pheromone of the European Corn Borer

A previous flight tunnel study showed that 3–5% of European corn borer (ECB) moths, Ostrinia nubilalis (Z/E11-14:OAc), could fly upwind and make contact with sources releasing the sex pheromone of the related Asian corn borer (ACB), Ostrinia furnacalis (2:1 Z/E12-14:OAc). In this study, we show that rare males (3–4%) are also present in South Korean ACB that respond to the sex pheromone blends of the ECB UZ (97:3 Z/E11-14:OAc) and BE (1:99 Z/E11-14:OAc) pheromone races. We also show that the upwind flight response of a significant proportion of male ACB was antagonized by the addition of 1% Z9-14:OAc to the ACB blend, a compound that also antagonizes the upwind flight of ECB males. Male ACB flight behavior was not, however, affected by adding either of the ECB blends to the ACB blend, or by the addition of 50% 14:OAc, a compound identified from female pheromone glands of ACB and a number of other Ostrinia species. Additional flight tunnel tests with ACB to study the comparative aspects of ECB and ACB pheromone response specificity showed that male ACB exhibited maximal levels of upwind flight and source contact with doses of pheromone (30 and 100 μg on rubber septum sources) that also elicited maximal levels in the two ECB pheromone races. The maximal level of source contact for ACB (66%) was lower than observed with the UZ race of ECB to its pheromone blend (>95%), but comparable to those for the BE race of ECB (65–70%). Male ACB also flew upwind in high proportions to a broader range of ratios of Z/E12-14:OAc (80:20 to 20:80) than was previously observed for either of the ECB races.     

左旋西替利嗪盐酸盐的合成

以苯甲酰氯为原料,经酰化,还原,环合等反应合成左旋西替利嗪盐酸盐,反应总收率为8.05%。     

利用米糠蛋白制备类阿片拮抗肽和降血压肽的研究

采用离体豚鼠回肠(GPI)检定法测定不同米糠蛋白胰蛋白酶水解物的类阿片拮抗活性,结果发现跟新鲜米糠一样,低温脱脂米糠蛋白的酶解物具有较高的类阿片拮抗活性,高温脱脂米糠蛋白的酶解物无类阿片拮抗活性。采用低温脱脂米糠蛋白为原料,研究其制备类阿片拮抗肽后的残留蛋白酶解物的ACE抑制活性,结果发现在6种酶解物中,水解度(DH)为15.4%的碱性蛋白酶水解物的ACE抑制活性最高。     

米糠类阿片拮抗肽的氨基酸序列分析

采用氨基酸分析仪、LC-MS对米糠类阿片拮抗肽的结构进行了分析，米糠类阿片拮抗肽由Asp、Gly、Ser、Val和Arg组成，它的氨基酸序列为Asp-Gly-Ser-Val-Arg。