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。     

脊椎滑脱症合并腰椎间盘突出的治疗

1987年6月至1995年1月我院共治疗脊椎滑脱55例,其中17例合并腰椎间盘突出,占31％,临床表现为顽固的腰骶痛和下肢根性放射痛。手术复位、融合不稳定脊椎的同时,均摘除突出的椎间盘髓核组织。经半年以上随访,疗效满意,作者分析了本病的病因病理,认为诊断该病必须综合性检查分析,脊髓造影或CT检查有一定影像学诊断价值,治疗宜早行探查手术。     

国产氟康唑对小鼠隐球菌病的疗效

以５×１０３ｃｆｕ／鼠的新型隐球菌给小鼠脑室感染（ｉｃ）１ｈ后，分别口服氟康唑（Ｆｌｕ）５和１０ｍｇ／（ｋｇ·ｄ）或酮康唑（Ｋｅｔ）５０和１００ｍｇ／（ｋｇ·ｄ），ｂｉｄ×９ｄ。对ｉｃ小鼠连续观察４０天的存活率和平均存活时间，Ｆｕｌ分别为５０％～７０％和８～１５天，Ｋｅｔ是３０％～４０％和５～９天。由小鼠侧尾静脉注射１０６ｃｆｕ／鼠新型隐球菌３天后产生的全身感染，分别给小鼠口服Ｆｌｕ２．５～１０ｍｇ／（ｋｇ·ｄ）或Ｋｅｔ２５～１００ｍｇ／（ｋｇ·ｄ），ｂｉｄ×９ｄ。感染２４、２８和３２天的ＰＤ５０Ｆｌｕ是２．７、３．５和６．７ｍｇ／ｋｇ，Ｋｅｔ为２８．４、７０．４和８３ｍｇ／ｋｇ；Ｆｌｕ和Ｋｅｔ的平均存活时间分别是２３～３４天和２０～３１天。在上述两种实验模型中分离脑和肺做细菌培养，Ｆｌｕ均与对照和５０ｍｇ／（ｋｇ·ｄ）的Ｋｅｔ比较，对ｉｃ１０天及静脉注射感染１３天的小鼠，口服５和１０ｍｇ／（ｋｇ·ｄ）或２．５～１０ｍｇ／（ｋｇ·ｄ）Ｆｌｕ均显著抑制新型隐球菌生长。     

苯并恶唑类化合物的研究——Ⅰ.化合物的合成及光物理性能

合成了四种结构类型的苯并恶唑化合物共15个:测试了它们的红外吸收光谱,以及它们在DMF中的紫外吸收、荧光发射和激光发射光谱。苯基取代物的荧光量子产率在0.64～0.66,无激光性能。其余的化合物荧光量子产率都大于0.70,在最大吸收波长下的激光转换效率为2.5～5.9%。     

脂肪栓塞综合征：附19例报告

脂肪栓塞综合征是创伤或骨折的严重并发症，死亡率高，通过对１９例临床观察分析及复习文献，提出对本征诊断有重要意义的４项标准：（１）“暴风雪”样肺片；（２）皮肤或粘膜有出血点；（３）低氧血症；（４）血小板减少，并认为应用高压氧治疗本征是一种有效的方法。     

胸腰椎骨折脱位157例临床分析

本文报告157例胸腰椎骨折脱位病人,非手术治疗36例,手术治疗116例。作者对临床治疗中的有关问题进行了讨论。     

肌蒂移植术治疗陈旧性脊髓损伤(附56例报告)

作者采用肌蒂移植术治疗胸腰段陈旧性脊髓损伤56例.脊髓功能恢复率提高至Franke 1个等级以上者占76.8%(43/56).本文讨论了肌蒂移植术对陈旧性脊髓损伤的适应证.安徽省宿州市骨伤科医院淮北煤矿基建局医院