The bioavailability and nonlinear pharmacokinetics of MK-679 in humans

MK-679 (R(?)-3-((3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)(3-(dimethylamino)-3-oxopropyl)thio)methyl)thio(propanoic acid) is a potent and specific LTD₄-receptor antagonist. The disposition of MK-679 was investigated in a three-way crossover study in 12 healthy males receiving single intravenous doses of 75, 250, and 500 mg of MK-679. A greater than proportional increase in the area under the plasma concentration—time curve of MK-679 was observed with increase in dose. The plasma concentration data for each subject fitted well to the differential equations for a two-compartment model with linear tissue distribution and Michaelis-Menten elimination from the central compartment, indicating that the elimination of MK-679 in humans is saturable. In a previous study, the disposition of MK-679 in humans was also dose-dependent when given together with its S(+)-isomer, L-668,018. Thus, the disposition of MK-679 in humans is dose-dependent regardless of the presence of its stereoisomer. Also, the bioavailability of MK-679 was determined in six healthy males receiving simultaneously an oral dose of 250 mg of MK-679 and intravenous infusion of 1 mg ¹⁴C-MK-679. Results of this study indicate that the oral bioavailability of MK-679 is nearly quantitative.     

蛭弧菌与微生物污染的相互关系探讨

本文在实验室条件下动态观察了蛭弧菌含量与微生物污染的相互关系。结果表明：蛭弧菌含量的增加滞后于水体污染，而污染过后蛭弧菌则可在较长时间内维持较高水平，这一特性在水污染指示中的可能作用值得进一步探讨。     

健康人血清叶酸和维生素B_(12)水平的测定

本文对14岁以下健康小儿171名,成人30名及初生儿脐带血30份进行了血清叶酸和维生素B_(12)含量测定,171名小儿于采血前均经补足叶酸和维生素B_(12)。结果:血清叶酸(nmol/L)的正常值低限,<4岁者为6.1,4～14岁为8.4,成人为5.0;血清维生素B_(12)(pmol/L)的正常值低限,<1岁为459,1岁～成人为107。     

Carotid-cavernous sinus fistula associated with a primitive trigeminal artery

Carotid-cavernous sinus fistulas are not rare, but they have never been reported in association with persistent primitive trigeminal artery. We recently encountered such a case. The Jaeger-Hamby procedure was employed, with mandatory occlusion of the primitive trigeminal artery.     

子宫颈上皮不典型增生与宫颈癌细胞超微结构的观察比较

光镜和电镜观察慢性宫颈炎上皮不典型增生42例,宫颈癌21例,正常对照7例。上皮不典型增生之一是位于深部的储备细胞增生,细胞的核质比大,细胞器少,分化较低。鳞状上皮不典型增生细胞特点是核质比增大,核形不整,核膜内陷,细胞器增多,桥粒和张力原纤维减少。鳞癌细胞的核质比更大,核膜内褶深,细胞器更多,桥粒和张力原纤维很少或消失,分化低的癌细胞尤明显。粘液性腺癌腺上皮深部可见储备细胞转化的癌细胞。     

脊髓手术中体感诱发电位监测的临床研究

报告３０例脊髓手术中体感诱发电位（ＳＥＰ）连续监测的临床研究结果。ＳＥＰ记录包括脊髓ＳＥＰ（ＳＳＥＰ）和皮层ＳＥＰ（ＳＣＥＰ）。麻醉药物对ＳＥＰ有一定程度影响，ＳＣＥＰ相对较大。认为，至少术中ＳＥＰ潜伏期延长不超过８％和波幅降低不超过５０％，不会引起术后并发症，超过该范围由于病例较少，尚不能肯定与预后的关系，需进一步探讨。     

PCR法检测淋球菌的临床应用

应用PcR法提高了淋球菌阳性检出率并与培养法做比较。118例拟诊淋病患者的样本采自尿道分泌物或宫颈分泌物,部分采自前段尿。用双盲法测定,结果检出率分别为73.7％和49.1％,PcR法的阳性检出率明显高于培养法,P<0.05。总阳性符合率分别为92.7％和69.8％,PcR法显著高于培养法P相似文献   

Electrochemical oxidation of 5-hydroxytryptophol. I: Studies in acid solution

The oxidation chemistry of the endogenous central nervous system indole 5-hydroxytryptophol (5-HTOL) has been studied at pH 2 using electrochemical methods. The first voltammetric oxidation peak (I) appears to involve an initial one-electron abstraction giving a transient radical cation that, in the rate-controlling step, deprotonates to give a neutral radical. A radical-substrate reaction then occurs to give a dimer radical which is further oxidized to yield three simple dimers (4,4'-,4,6'-, and 2,4'-linked). The neutral radical can be further oxidized (1e) to a quinone imine that, as a result of very fast follow-up chemistry and electrochemistry, yields tryptophol-4,5-dione (B) which has been isolated in pure form. Reactions between intermediate species also result in three dimers containing residues of 5-HTOL and B and an unusual oxygen-bridged trimer.     

进一步重视脂肪新功能对创面愈合作用的研究

创面愈合的研究范围正随着相关领域的研究进展而不断拓展和完善。以皮下脂肪组织为例 ,以往多数的研究认为 ,脂肪组织来源于间充质细胞 (mesenchymalcell,MC) ,其功能仅是一个能量贮存仓库。但近年来的研究表明 ,脂肪组织还可能是一个重要的内分泌器官 ,在发育学、信号转导 ,以及干细胞作用等多方面与组织修复存在着密切联系。有专家认为 ,加强对脂肪细胞新功能的研究和开发 ,有可能对创面修复和组织再生机制产生新的认识 ,并寻找出新的促愈合手段。脂肪细胞参与创面愈合首先表现在它可能作为一个内分泌器官。迄今为止 ,已经发现人的脂肪细…     

血瘀证的研究发展脉络与评述

主要从4个方面论述了血瘀证50年来研究进展．理论研究，着重从古今文献论述血瘀证定义和含义；客观研究，着重对生理、生化、血液流变学、免疫学、病理学和微循环等方面对血瘀证进行研究；血瘀证的动物模型研究，主要对血瘀证动物模型的建立与造模方法和途径进行研究；诊断标准研究，包括诊断标准、诊断指标的研究。并对上述内容进行了评述，并提出了展望。