吡酮酸类抗菌药物的研究——Ⅹ.1,7-双取代-6-氟-1,4-二氢-4-氧代喹啉-3-羧酸类化合物的合成与构效关系

本文合成了一系列1-位含有呋喃环系,异噁唑环系及取代苯基,7-位为不同取代氨基的吡酮酸类化合物,测定了这些化合物对大肠杆菌ATCC-25922,金黄色葡萄球菌ATCC-6538 p的MIC值,并与双氟哌酸进行对照,探讨了这些化合物的构效关系。     

Response Characteristics Of Cutaneous Mechanoreceptors In Neuropathic Rats

The activity of single myelinated afferents was recorded from dorsal roots L4-5 in normal Sprague-Dawley rats and animals that developed mechanical hypersensitivity following ischemic injury to the sciatic nerve. The mechanical response properties and conduction velocity of afferents conducting through the injury site (about 50% of units) were similar to controls. However, the majority of afferents not conducting through the injury site exhibited ongoing activity. The results suggest that mechanical allodynia may be at least partly due to the central integration of activity arising from these two populations of afferents in neuropathic rats.     

Drug-induced growth hormone and prolactin responses in schizophrenia research

1. Interpretation of neuroendocrine studies in schizophrenia requires consideration of (a) the large number of variables that affect drug-induced endocrine responses (b) the effect of prior neuroleptic therapy (c) heterogeneity of schizophrenia (d) heterogeneity of receptors (e) uniqueness of the hypothalamic-pituitary axis (f) selectivity and pharmacokinetics of administered drugs. 2. Apomorphine increases growth hormone secretion by an effect on dopamine receptors that are not linked to adenylate cyclase and which are located outside the blood brain barrier. 3. Hypothalamic-pituitary histaminergic H2 and alpha-adrenergic function are unchanged in chronic schizophrenia. 4. Schizophrenic symptoms persist despite complete blockade of dopamine receptors modulating prolactin secretion. 5. Studies on dopamine receptors modulating prolactin secretion are unlikely to shed light on the pathophysiology of schizophrenia. 6. Screening for drugs which block apomorphine-induced growth hormone secretion but do not increase prolactin may provide a way of detecting anti-schizophrenic drugs which are devoid of side effects associated with hyperprolactinemia and which do not induce parkinsonism or tardive dyskinesia.     

Effect of bromocriptine in patients with apomorphine-responsive erectile impotence: an open study.

An open pilot study was undertaken to investigate the therapeutic effect of the dopaminergic agent, bromocriptine (BC), in impotent patients who developed an erectile response to the dopamine receptor agonist, apomorphine. Eight out of 17 patients reported improvement in ability to obtain an erection; five of these 8 subjects were able to achieve penetration. The optimum dose of BC was 2.5 - 11.25 mg/day. A double-blind placebo-controlled study is merited.     

Elevated interleukin-13 in patients with active lupus nephritis

目的　探讨白细胞介素 13(IL 13)在活动性狼疮肾炎患者中的作用。方法　选择 10名健康人和 16名活动性狼疮肾炎患者。采用酶联免疫吸附法 (ELISA)测定IL 13血浆水平 ,反转录多聚酶链反应 (RT PCR)检测外周血单个核细胞IL 13基因表达水平。肾组织内IL 13基因表达采用原位杂交技术 (ISH)测定。结果　活动性狼疮肾炎患者IL 13血浆水平和外周血单个核细胞IL 13mRNA表达水平均较正常对照组增高 (P<0 0 0 1)。活动性狼疮肾炎患者肾组织内IL 13mRNA表达较正常对照组明显增高 (P <0 0 0 1)。直线相关分析结果表明 ,活动性狼疮肾小管间质区IL 13mRNA表达量与血肌酐浓度、肾小球活动指数和肾小管间质活动指数、血C3浓度相关 (P <0 0 5 )。结论　IL 13水平增高在活动性狼疮肾炎的分子发病机制中起一定的作用。     

化学合成法确证柄果花椒酰胺的结构

柄果花椒酰胺(podocarpamide)是从柄果花椒干树皮中分离得到的一结晶化合物。经药理筛选,体外有抗血小板凝聚作用和降转氨酶活性。该天然产物的结构从光谱推断有如下两种可能的组合方式:     

柄果花椒酰胺的化学结构

前文报道从湖南地区采集的芸香科植物柄果花椒(Zanthoxylum podocarpum Hemsl.)树皮中分离并经鉴定的结晶有β-香树脂醇、β-谷甾醇、ι-芝麻素、ι-细辛素、新棒状花椒酰胺、新木脂体柄果脂素和山萮酸为主的混合脂肪酸等。并从该植物中分得另一结晶(Ⅸ),本文报道结晶(Ⅸ)的化学结构。     

钙离子对4－氨基吡啶诱发肥大细胞释放组胺作用的影响

钙离子对４－氨基吡啶诱发肥大细胞释放组胺作用的影响徐建华，王佩，陈志刚，张剑　（浙江医科大学药学系药理学教研室杭州３１０００６）４－氨基吡啶（４－ａｍｉｎｏｐｙｒｉｄｉｎｅ，４－ＡＰ）是一种钾通道阻滞剂，它能促进神经末梢释放多种递质［１，２］，促进β...     

国产阿克拉霉素A的体内外抗肿瘤作用

国产阿克拉霉素A(aclacinomycin;ACM-A)能明显抑制体外培养小鼠白血病P₃₈₈和人体胃癌SGC-7901细胞的生长。在0.01 μg/ml浓度时能抑制65.4%的克隆形成,ED₅₀为0.0085μg/ml。ACM-A对白血病小鼠有显著治疗作用,延长小鼠生命时间143%,并有半数小鼠获得治疗。对Ehrlich腹水癌和肉瘤-180也有较强的抑制作用,对肉瘤-180的作用与adriamycin相似。ACM-A主要抑制³H-TDR和。H-UR分别参人人体胃癌细胞的DNA和RNA;大剂量时对蛋白质合成也有影响。P₃₈₈细胞实验中证明ACM-A对DNA合成的抑制程度与adriamycin相似,低于daunomycin。