抗棘球蚴药物研究:3-取代苯基-5-取代-1,2,4-噁二唑的合成

合成了3-取代苯基-5-取代-1,2,4-(口恶)二唑类化合物50个,经感染棘球蚴的小鼠初筛,部分化合物对棘球蚴有不同程度的作用,化合物13、28和30对棘球蚴的囊重抑制率分别为70、75.6和71.6%,其中化合物13对棘球蚴的生发层有损害作用。     

Gadolinium-enhanced breath-hold three-dimensional time-of-flight MR angiography of the abdominal and pelvic vessels: The value of ultrafast MP-RAGE sequences

MR angiography (MRA) was performed in 50 consecutive subjects (mean age, 59 years), who had been referred for abdominal MRA, on a 1.5-T superconductive unit that used a body phased-array coil. Three breath-hold three-dimensional sequences were evaluated both in phantom and clinical studies: (a) standard fast three-dimensional gradient-echo sequence (TR = 15, TE = 6; imaging time, 32 seconds), (b) ultrafast three-dimensional gradient-echo sequence (TR = 8.2, TE = 3; imaging time, 18 seconds), and (c) ultrafast magnetization-prepared (MP) rapid acquisition gradient echo (RAGE) (TR = 5.8, TE = 2.9, inversion time [TI] = 20; imaging time, 15 seconds). The initial 30 patients were randomized into three groups by three separate sequences. For the remaining 20 patients, ultrafast-gradient-echo and ultrafast MP-RAGE sequences were performed. Conventional angiography was performed on 36 patients. Signal measurements of the phantom and clinical images of the aorta, visceral branches of the aorta, iliac arteries, inferior vena cavae, and portal veins were performed. The overall image quality and background fatty tissue contrast of the vessels were rated subjectively. Comparison of images between MRA and conventional angiography also was performed. The contrast between the vessels and background fatty tissue was significantly higher in the ultrafast MP-RAGE sequence in both quantitative and qualitative analysis, and image-quality ultrafast MP-RAGE was superior to the other two sequences (P < .01). The aorta and iliac arteries could be visualized in all pulse sequences, and abnormalities of these vessels were diagnosed correctly. The renal artery was visualized more clearly with the two ultrafast sequences.     

Gadoteridol dose dependence in MR imaging of a liver abscess model

A necrotic liver abscess model was studied with magnetic resonance (MR) imaging at 1.5 T before and after intravenous administration of gadoteridol at doses of 0.1, 0.25, and 0.5 mmol/kg in 24 rabbits. Enhancement characteristics and lesion delineation were assessed with both breath-hold and non-breath-hold imaging techniques. Lesion delineation, as assessed both by signal intensity measurements and evaluations by two image readers blinded to imaging technique, was greatest on high-dose (0.5 mmol/kg) breath-hold images. Lesion rim enhancement was seen consistently only on postcontrast images obtained at a dose of 0.5 mmol/kg and progressed with time after injection of contrast material.     

Dynamic gadolinium-enhanced echo-planar MR imaging of the liver: Effect of pulse sequence and dose on enhancement

To develop guidelines for clinical magnetic resonance imaging of the liver, the authors undertook an animal study to investigate the effect of dose and pulse sequence on liver signal intensity in gadopentetate dimeglumine—enhanced echo-planar imaging. Serial imaging of the liver was performed in anesthetized rats after intravenous administration of five different doses (0.01, 0.05, 0.1, 0.2, and 0.5 mmol/kg) of contrast agent, with six different pulse sequences. The results show that gadopentetate dimeglumine—enhanced echo-planar images obtained during the perfusion phase can yield either positive (due to increased T1 relaxation rates) or negative (due to susceptibility-induced increased T2 relaxation rates) liver enhancement depending on choice of pulse sequence and dose. At the current clinically recommended dose of 0.1 mmol/kg, maximal liver signal enhancement was seen with a T1-weighted inversion-recovery sequence, while maximal liver signal diminution was seen with a T2*-weighted gradient-echo sequence. The authors conclude that gadopentetate dimeglumine—enhanced echo-planar imaging can provide T1, T2, and T2* contrast that may be exploited for both lesion detection and lesion characterization.     

Contrast agents in functional MR imaging

Contrast agents have greatly expanded the role of MR imaging (MRI) to allow assessment of physiologic, or “functional,” parameters. Although activation mapping generally does not require contrast agents, other forms of functional MRI, including mapping of cerebral hemodynamics (eg, perfusion imaging), are best done with the use of contrast agents. Serial echo planar images are obtained after bolus injection of lanthanide chelates. Application of susceptibility contrast physics and standard tracer kinetic principles permits generation of relative cerebral blood volume maps. Deconvolution of cerebral blood flow and mean transit time parameters is also possible within technical limitations. By using diffusion and perfusion pulse sequences, an imaging correlate to the ischemic penumbra can be identified. Functional MRI perfusion imaging of intraaxial tumors is analogous to positron emission tomography for delineation of metabolic activity, yet may be even more sensitive to neovascularity and possesses improved image quality. Clinical applications include biopsy site selection and postirradiation follow-up. Further improvements in data analysis and map generation techniques may improve diagnostic accuracy and utility.     

胎肌条件培养液抗损伤效应的观察

胎肌条件培养液（ＦＭＣＭ）可在ＣＦＵ－ＧＭ体外培养中提供集落刺激活性。研究发现它还能在体外培养中保护ＣＦＵ－ＧＭ，减轻理化损伤因素对其生长的抑制效应。所用化学损伤因素为５×１０－７Ｍ的阿糖胞苷与９×１０－９Ｍ的三尖杉酯碱，物理损伤因素为放射（３．５Ｇｙ），热（４４℃，６０分钟）与冷（—２０℃，１６分钟）。在损伤因素作用下，ＣＦＵ－ＧＭ的集落产率受到明显抑制，用２０％ＦＭＣＭ处理后，抑制现象可以减轻。ＦＭＣＭ可以对抗多种因素对ＣＦＵ－ＧＭ的抑制作用，没有特异性。用胰蛋白酶或热（８５℃，３０分钟）处理后的ＦＭＣＭ不具上述保护效应，用酸（ＰＨ＝２），碱（ＰＨ＝１０），ＤＮＡ酶与透析处理则无明显影响。提示ＦＭＣＭ中起保护作用的活性物质可能为分子量大于１００００的蛋白质。     

Dynamic contrast-enhanced ultrasound with carbon dioxide microbubbles as adjunct to arteriography of liver tumors

Purpose The goal of the study is to evaluate utility of contrast enhanced ultrasound (US) with carbon dioxide microbubbles in evaluation of hepatic lesions.Methods Twenty eight patients with single or multiple t hepatic lesions (11 hepatocellular carcinoma, 8 hemangiomas, 5 metastases, 1 adenoma, 1 focal nodular hyperplasia, 2 regenerative nodules) were examined. US exam was performed during intraarterial injection of 10 ml of CO₂ through the same catheter employed for liver arteriography. The US exam was videotaped in its salient phases. Characteristics of enhancement were evaluated and correlated with histological findings or patient follow up.Results Sonographic angiography clearly demonstrated vascularization of the lesions. Hepatocellular carcinoma, hemangioma, metastases, focal nodular hyperplasia, and regenerative nodules had very characteristic patterns. The injection of CO₂ allowed detection of small additional nodules.Conclusion Sonographic angiography can improve characterization and staging of hepatic tumors. Low cost and the simplicity of the technique should encourage further experimentation.     

Conventional MRA and contrast- enhanced MRA of extracranial vessel segments

Summary The introduction of fast gradient systems allows a reliable visualization of the extracranial carotid vessels by the magnetic resonance angiography (MRA) which meanwhile is implemented into clinical routine. By the mainly applied time-of-flight (TOF) technique, vessels can be imaged without contrast agent (CA). Due to the application of ultra-fast gradient-echo-sequences, the first-pass evaluation of an intravenous bolus-injection of Gadolinium in the carotids from the aortic arch up to the skull base can be performed in less than 30 s. In this study, advantages and disadvantages of both techniques are discussed. For a qualitatively optimal contrast enhanced MRA (CE-MRA) timing parameters like injection delay, flow rate and the adjustment of sequence parameters have to be considered in relation to the fast venous return from the sinus to the jugular veins. First, the optimal time point of the data acquisition have been determined at a model and with a computer simulation in reference to the presence of CA in the arteries. As a result, 90 % of the contrast contribution is defined by 16 % of the symmetrically acquired central k-space lines. A measuring protocol for clinical use was obtained by a gradual variation of spacial resolution, measuring time and CA-injection parameters and was proved in normal volunteers and patients. An exact determination of the bolus-arrival-time by means of a test-bolus injection was acquired. The best qualitative results were achieved by a double-dose injection at 2 ml/s injection rate. The temporal reserves of ultra-fast sequences should be invested in the improvement of the spatial resolution. To date, further investigations related to the problem of optimal CA-application may improve the potentials of CE-MRA procedures.      

High-dose gadoteridol in MR imaging of intracranial neoplasms.

Twelve patients with a high suspicion of brain metastases by previous clinical or radiologic examinations were studied in a phase III investigation with magnetic resonance (MR) imaging at 1.5 T after a bolus intravenous injection of 0.1 mmol/kg gadoteridol followed at 30 minutes by a second bolus injection of 0.2 mmol/kg gadoteridol. All lesions were best demonstrated (showed greatest enhancement) at the 0.3-mmol/kg (cumulative) dose, with image analysis confirming signal intensity enhancement in the majority of cases after the second gadoteridol injection. More lesions were detected with the 0.3-mmol/kg dose than with the 0.1-mmol/kg dose, and more lesions were detected with the 0.1-mmol/kg dose than on precontrast images. In this limited clinical trial, high-dose gadoteridol injection (0.3-mmol/kg cumulative dose) provided improved lesion detection on MR images specifically in intracranial metastatic disease.     

纤维组织粘合剂的实验研究

本文应用“冷沉淀”法制备纤维组织粘合剂。对纤维组织粘合剂中主要成份和含量进行了测定,并测定了主要理化性质,建立了动物实验模型,观察了实验兔对纤维粘合剂的反应。