盐酸咪唑苯脲的合成

苄腈经混酸硝化、与乙二胺在硫粉催化下环合、铁粉还原得2-（3-氨基苯基）-4，5-二氢-1H-咪唑二盐酸盐，再与双光气缩合后成盐，制得抗梨形虫病药盐酸咪唑苯脲，总收率约50％。     

微波促进的化学反应在药物合成中的应用

综述了近年应用于药物合成的微波促进的反应类型，包括环合、不对称烷基化、Suzuki偶合、还原和氧化、亲核取代等。与经典的有机反应相比，微波促进的化学反应可缩短反应时间，提高反应的选择性和收率，减少溶剂用量，简化后处理过程，减少三废。     

Microwave-assisted Synthesis of an Important Intermediate of Benazepril

Rapid and efficient methods for the synthesis of an important intermediate of benazepril ethyl 3-phthalimido-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-one-1-acetate under the influence of microwave irradiation are described. A comparative study of conventional and microwave assisted method is briefly discussed.     

Antidepressant up-titration: pharmacological and psychological considerations

The use of antidepressant up-titration in starting therapies is useful in reducing side effects, but can induce delays in clinical response. Several aspects concerning slow or more aggressive titration have to be considered when using this strategy, such as pharmacological aspects (e.g., synaptic up-regulation) and psychological/clinical aspects (e.g., adherence to antidepressant treatment, and the temperament and expectations of patients). Data from the literature are controversial, and so the choice between rapid and slow titration must be tailored more to the patient, rather than to the drug.     

抗抑郁药盐酸度洛西汀的合成

目的合成盐酸度洛西汀并改进合成工艺。方法以2-乙酰噻吩为起始原料，经Mannich反应、还原、拆分、醚化、脱甲基、成盐等反应制得盐酸度洛西汀。结果所得产物经元素分析、紫外光谱、红外光谱、核磁共振谱及质谱等确证了结构。结论此工艺路线方法简便，原料易得，便于工业化生产。     

Microwave‐Assisted Synthesis and Tyrosinase Inhibitory Activity of Chalcone Derivatives

A series of chalcones and their derivatives were synthesized, and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were evaluated. The results showed that some of the synthesized compounds exhibited significant inhibitory activity, and four compounds exhibited more potent tyrosinase inhibitory activity than the reference standard inhibitor kojic acid (5‐hydroxy‐2‐(hydroxymethyl)‐4H‐pyran‐4‐one). Specifically, 1‐(‐1‐(4‐methoxyphen‐ yl)‐3‐phenylallylidene)thiosemicarbazide ( 18 ) exhibited the most potent tyrosinase inhibitory activity with IC₅₀ value of 0.274 μm . The inhibition mechanism analysis of 1‐(‐1‐(2,4‐dihydroxyphenyl)‐3‐phenylallylidene) thiosemicarbazide ( 16 ) and 1‐(‐1‐(4‐methoxyphenyl)‐3‐phenylallylidene) thiosemicarbazide ( 18 ) demonstrated that the inhibitory effects of the two compounds on the tyrosinase were irreversible. Preliminary structure activity relationships' analysis suggested that further development of such compounds might be of interest.     

抗抑郁药物在功能性胃肠病中的应用

功能性胃肠病（functional gastrointestinal disorders, FGIDs）指一组慢性或反复发作、不能以消化道结构或生化异常解释的症状，常规治疗方法效果不理想。研究发现，改善精神心理状态的药物对FGIDs有一定的治疗作用。最常用的为三环类抗抑郁药（tricyclic antidepressants, TCAs）和选择性5-羟色胺再摄取抑制剂（selective serotonin reuptake inhibitors, SSRIs）。新型的抗抑郁药5-羟色胺-去甲肾上腺素再摄取阻断药（serotonin noradrenalin reuptake inhibitors, SNRIs）也可能对FGIDs有效。抗抑郁药不但可以治疗同时合并的焦虑或抑郁障碍，并且本身对改善FGID患者转归有效，特别是当患者有持续性疼痛，或同时合并焦虑或抑郁障碍，抗抑郁药应作为治疗首选。     

抗抑郁药物在功能性胃肠病中的应用

功能性胃肠病（functional gastrointestinal disorders, FGIDs）指一组慢性或反复发作、不能以消化道结构或生化异常解释的症状，常规治疗方法效果不理想。研究发现，改善精神心理状态的药物对FGIDs有一定的治疗作用。最常用的为三环类抗抑郁药（tricyclic antidepressants, TCAs）和选择性5-羟色胺再摄取抑制剂（selective serotonin reuptake inhibitors, SSRIs）。新型的抗抑郁药5-羟色胺-去甲肾上腺素再摄取阻断药（serotonin noradrenalin reuptake inhibitors, SNRIs）也可能对FGIDs有效。抗抑郁药不但可以治疗同时合并的焦虑或抑郁障碍，并且本身对改善FGID患者转归有效，特别是当患者有持续性疼痛，或同时合并焦虑或抑郁障碍，抗抑郁药应作为治疗首选。     

抗抑郁药物在功能性胃肠病中的应用

功能性胃肠病（functional gastrointestinal disorders, FGIDs）指一组慢性或反复发作、不能以消化道结构或生化异常解释的症状，常规治疗方法效果不理想。研究发现，改善精神心理状态的药物对FGIDs有一定的治疗作用。最常用的为三环类抗抑郁药（tricyclic antidepressants, TCAs）和选择性5-羟色胺再摄取抑制剂（selective serotonin reuptake inhibitors, SSRIs）。新型的抗抑郁药5-羟色胺-去甲肾上腺素再摄取阻断药（serotonin noradrenalin reuptake inhibitors, SNRIs）也可能对FGIDs有效。抗抑郁药不但可以治疗同时合并的焦虑或抑郁障碍，并且本身对改善FGID患者转归有效，特别是当患者有持续性疼痛，或同时合并焦虑或抑郁障碍，抗抑郁药应作为治疗首选。     

Antidepressant prevalence for youths: a multi-national comparison

OBJECTIVE: To compare antidepressant prevalence data in youths across three western European countries (Denmark, Germany, and the Netherlands) with US regional data in terms of age and gender and to show proportional subclass antidepressant (ATD) use. METHOD: A population-based analysis of administrative claims data for the year 2000 was undertaken in 0 to 19-year-old enrollees who were part of the insured populations from four countries having a total of from 72,570 to 480,680 members. RESULTS: ATD medication utilization in the US dataset (1.63%) exceeded that of three Western European countries (prevalence ranged from 0.11 to 0.54%) by at least 3-fold. There were major variations in the use of subclasses: tricyclic antidepressants (TCAs) predominated in Germany while selective serotonin reuptake inhibitors (SSRIs) predominated in the US, Denmark and the Netherlands. CONCLUSIONS: Cross-national variations should be further explored to understand the factors related to these differences and how prevalence differences relate to effectiveness and safety. Community-based cohorts should be followed to establish outcomes in the usual practice setting.