Synthesis of 14C‐labeled piperidines and application to synthesis of [14C]SCH 351125, a CCR5 receptor antagonist

1‐Benzyl‐4‐hydroxy[2‐¹⁴C]piperidine, a useful intermediate in labeled compound synthesis, was prepared from [¹⁴C]formaldehyde in high yield. The distribution pattern of ¹⁴C in the product is consistent with a mechanism involving reversible iminium ion formation and rapid equilibration of the iminium ion through a cationic aza‐Cope rearrangement. These steps precede the rate‐determining intramolecular cyclization step. SCH 351125 is a potent, selective CCR5 receptor antagonist with potential as a treatment for HIV infection. [¹⁴C]SCH 351125, required for metabolism studies, was prepared from 1‐benzyl‐4‐hydroxy[2‐¹⁴C]piperidine in six steps. [¹⁴C]SCH 351125 is a mixture of four atropisomers. Preparation of [¹⁴C]SCH 351125 besylate salt of the desired atropisomer pair is also described. Copyright © 2007 John Wiley & Sons, Ltd.     

Lack of spontaneous activity of cutaneous spinal dorsal horn neurons in awake, drug-free, spinally transected cats

Extracellular single-unit activity was recorded from neurons with cutaneous input in the dorsal horn of the spinal cord (L4-L6) of awake, drug-free cats before (for several weeks) and after (day 1 through day 7) cord transection (T12). The spontaneous activity of the neurons was minimal or nonexistent in both recording conditions. The lack of spontaneous activity following spinal cord transection contrasts sharply with activity recorded in acute spinal-cord transected preparations in which high rates of spontaneous activity have been reported. This discrepancy may reflect an important difference between the chronic, awake, drug-free and acute preparations.     

血康口服液与他莫昔芬联合治疗免疫性血小板减少性紫癜疗效观察

联合应用血康口服液和他莫昔芬治疗成人免疫性血小板减少性紫癜(ITP)20例。疗程超过2月。15例患者的血小板(BPC)计数明显上升,有效率为75％(15/20),对于激素治疗无效者,仍有良效。对月经过多者和不适合应用激素者尤为适应。两药合用无明显副作用。治疗起效时间较快,平均13天。疗效持续时间较长,长者已达一年以上。     

正常人眼筛板的结缔组织纤维结构

采用组化特染，透射电镜和图象分析仪观察了３５只正常人眼筛板结缔组织的纤维成分和结构形态，根据生物力学原理分析了筛束的力学性质和筛板的结构特征，探讨了筛板的损害形式和在眼压与视神经损害间的中介作用及其影响因素。结果显示，筛束含有细胞间质所有三种纤维，具有弹性、塑性和刚性三重复合性质，筛板纵向椭圆、筛束行径和密度象限性差异及筛板厚度个体性差异等与筛板抗损害性能有关。眼压对筛板作用有两种途径，筛板损害是     

多巴酚丁胺负荷对缺血性扩张型心肌病患者左心室充盈的影响：病理生理学及预后意义

目的：本研究旨在探讨多巴酚丁胺对缺血性心肌病（ICM）患者左心室（LV）充盈功能的影响，并确定峰值负荷时限制性充盈型（RFP）是否具有预后预测价值。背景：ICM患者峰值负荷时RFP的预后价值尚属未知。方法：在静息和负荷情况下，采用多普勒超声心动检查研究了69例ICM患者；RFP定义为跨二尖瓣E／A比≥1．0、等容舒张时间（IVRT）〈80ms及E波减速时间（EDT）〈120ms。结果：69例患者中有42例静息时出现RFP，其中有24例患者负荷情况下转变为非RFP（EA），18例患者RFP持续存在（EE）；69例患者中27例静息和峰值负荷时均无RFP（AA）。     

Could bipolar vessel sealers prevent bile leaks after hepatectomy?

BACKGROUND AND AIMS: The aim of this work was to test the feasibility of using a bipolar low thermal acting system inducing collagenic sealing but not protein coagulation to secure hepatic parenchyma cutting. MATERIALS AND METHODS: Thirty consecutive hepatectomies were carried out using kellyclasy plus ligatures and clips (controls), while the following 50 hepatectomies used kellyclasy plus bipolar vessels sealer (BVS). Blood loss, duration of hepatic pedicle clamping, length of hospital stay, and complications were recorded. RESULTS: There was no statistically significant difference in blood loss and duration of clamping between controls and BVS. Specific complications (9/21 in the control group vs 1/49 for the BVS group, p<0.00045) and length of hospital stay (14 days in the control group vs 11 days in the BVS group, p<0.014) were statistically lower in BVS group than in the controls, mainly due to prevention of bile duct leakages. CONCLUSIONS: Our data suggest that BVS may be particularly efficient to achieve bilistasis leading to the highest level of safety in performing hepatectomies. Further studies are now needed to confirm its superiority on the classical biliary ducts occlusion techniques.     

Expression of neuron-specific enolase and olfactory marker protein in the developing olfactory mucosa of human fetuses]

OBJECTIVE: To study the expression of neuron-specific enolase (NSE) and olfactory marker protein (OMP) in the developing olfactory mucosa of human fetuses. METHOD: The expression of NSE and OMP in the olfactory mucosa of 6 human fetuses (12, 16, 20, 24, 28 and 34 weeks) was studied using the technique of immunohistochemistry. RESULTS: NSE immunological positive reactions were seen in all 6 fetal mucosa from gestational 12 (G12) to G34, with plenty of positive-stained dual-pole neuron cells. At G12, the positive cells aligned tightly, the cell bodies were localized in the lower portion of olfactory epithelium and the positive-stained area occupied upper 2/3 of fetal nasal mucosa. With the development, the positive cells gradually became multilayer, but the density and the relative area of positive-cells reduced. At G34, the positive cells were located only in upper 1/3 of nasal mucosa. OMP-positive reactions were localized in a few dual-pole neurons at G12, the number was much less than NSE-positive cells in the same fetus. With the development, the OMP-positive cells gradually increased with most of the cell bodies located in the upper portion of epithelium, but number still relatively less than the NSE-positive cells at the same age. CONCLUSION: At G12, there were lots of olfactory neuron in the olfactory mucosa and only a few olfactory neurons had became mature. With the development, the olfactory epithelial area reduced but the number of mature olfactory neurons increased. At the last trimester, fetal olfactory sensor was almost matured.