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.     

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。     

大黄总甙、大黄素和番泻甙对小鼠离体肠管葡萄糖转运电位的影响

本实验采用记录翻转小肠和结肠囊葡萄糖转运电位的方法,来研究大黄泻下作用的有效成分大黄总甙、大黄素和番泻甙对小肠及结肠囊跨肠壁电应差的变化,发现上述成分可阻止葡萄糖和Na~+的转运,这一结果为进一步阐明大黄泻下作用的原理提供新的理论依据。     

彩色多普勒在心脏起搏器综合征诊断中的应用价值

目的 :探讨运用彩色多普勒血流显像 (CDFI)并结合心电图 (ECG)诊断起搏器综合征 (PMS)的临床价值。方法 :对具有详实临床及ECG资料的心室按需 (VVI)起搏器安置患者 6 0例及对照组 4 8例进行CDEI检查 ,观察起搏组与对照组的三尖瓣返流 (TR)的发生率、返流程度 ,并分析二者之间的相关性。结果 :起搏组出现逆传P波 (即PMS阳性 )者 15例 ,CDFI检测出现TR者 2 0例 ,明显高于对照组 ,且PMS阳性者TR发生率明显高于PMS阴性者 ,表明安置VVI起搏器后出现逆传P波与TR的发生相关性良好。结论 :CDFI对PMS的诊断具有重要意义 ,尤其将ECG与CDFI结合应用有助于诊断率的提高。     

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…