Metabolism of the new synthetic cannabinoid EG-018 in human hepatocytes by high-resolution mass spectrometry

Purpose

The present study aims to recommend appropriate urinary marker metabolites for documenting EG-018 consumption by investigating its metabolism in human hepatocytes.

Methods

For metabolite profiling, 10 µM EG-018 was incubated in human hepatocytes for 3 h. Metabolite identification in hepatocyte samples was accomplished with high-resolution mass spectrometry via information-dependent data acquisition.

Results

EG-018 was highly metabolized in human hepatocytes. A total of eight metabolites were characterized, mainly generated from hydroxylation and carbonylation on the pentyl chain. Dihydrodiol formation, N-dealkylation, and glucuronidation of hydroxylated metabolites were the other major pathways.

Conclusions

The primary metabolites of EG-018 in human hepatocyte incubation were pentyl hydroxylated EG-018 (M6) and pentyl carbonylated EG-018 (M8). These two metabolites are proposed as the best urinary markers for confirming EG-018 intake.

     

机械通气辅助及血压调控对重症颅脑损伤患者脑氧代谢的影响

目的观察机械通气辅助及血压调控对重症颅脑损伤患者脑氧代谢的影响。方法56例重症颅脑外伤患者(3相似文献   

Postnatal development of nicotinamide adenine dinucleotide phosphate-diaphorase-positive neurons in the retina of the golden hamster

The histochemical method was used to investigate the postnatal development of nicotinamide adenine dinucleotide phosphate-diaphorase (NADPH-d) -positive neurons in retinas of the golden hamster. NADPH-d-positive neurons were discernible in the retina at postnatal day (P)1. From P4 onward to adulthood, when the retina acquired its laminated characteristics, NADPH-d- positive neurons were observed in the inner nuclear layer (INL) and the ganglion cell layer (GCL). Results showed that NADPH-d-positive neurons in INL and GCL followed different time courses and patterns in their development. NADPH-d-positive neurons in INL underwent a sharp increase from P4 to P8 (3.6-fold), followed by a decrease to 46% of the maximum at P12. This value was maintained relatively constant to the adult level. The mean diameters of NADPH-d-positive neurons in INL, which were smaller than those in the GCL for all ages, increased from P8 to P12 and from P20 to adulthood. As for neurons in the GCL, the increase in cell number was not so apparent for the earlier postnatal days until P20; thereafter, an obvious increase to the adult level was observed. The mean diameters of the NADPH-d-positive cell bodies in the GCL increased with age, except for P16-P20, during which time there was a slight and insignificant decrease. The tendency of changes in cell density was basically similar to that of the total number for both the INL and the GCL. Between P12 and P20, the density distribution map of the NADPH-d-positive neurons underwent dramatic changes: The highest density shifted from the upper central retina at the earlier postnatal days to the lower central retina in the adult. The two waves of increase in NADPH-d-positive neurons coincide with the process of axonal elongation and synaptogenesis and the acquisition of visual function and experience. It is suggested that these NADPH-d-positive neurons are related to these two developmental events.     

高效液相色谱法测定血浆中洛美沙星浓度及其在人体内药代动力学

建立了人血浆洛美沙星的反相离子对高效液相色谱测定方法。该法简便易行,精密度好,方法回收率95～102%,日内、日间RSD为2.1～7.8%,血药浓度在0.125～5.012 μg/ml范围内呈线性关系,相关系数0.9998,当S/N=2时,最小检测浓度为25 ng/ml。健康志愿者口服400 mg洛美沙星,药代动力学过程符合一室模型,消除相半衰期为5.5 h。     

Cadmium Pollution in Paddy Soil as Affected by Different Rice (Oryza sativa L.) Cultivars

No abstract available.     

Use of mandelic acid condensation polymer (SAMMA), a new antimicrobial contraceptive agent,for vaginal prophylaxis

OBJECTIVE: To assess the contraceptive properties, antimicrobial activity, and safety of mandelic acid condensation polymer (SAMMA). DESIGN: Experimental study of SAMMA's in vitro and in vivo properties. SETTING: Academic research laboratories. PATIENT(S): Healthy volunteers for semen donation in an academic research environment. INTERVENTION(S): Inhibition of sperm function indicators, conception, sexually transmitted infection-causing pathogens (including HIV), and lactobacilli was evaluated. Safety indicators were studied. MAIN OUTCOME MEASURE(S): Quantitation of SAMMA's effect on microbial infectivity or multiplication and on sperm function in vitro; evaluation of contraceptive efficacy in vivo; assessment of safety in vitro and in vivo. RESULT(S): Mandelic acid condensation polymer is not cytotoxic toward lactobacilli, microbial host cells, and spermatozoa. The compound inhibits hyaluronidase and acrosin, induces sperm acrosomal loss, and is contraceptive in the rabbit model. Mandelic acid condensation polymer prevents infectivity of HIV and herpesviruses 1 and 2 and, to a lesser extent, of Chlamydia trachomatis. It inhibits the multiplication of Neisseria gonorrhoeae. Mandelic acid condensation polymer is not mutagenic, has low acute oral toxicity, and is safe in the rabbit vaginal irritation assay. CONCLUSION(S): Mandelic acid condensation polymer inhibits sperm function, is contraceptive, has broad-spectrum antimicrobial activity, and is highly safe. Further development as a microbicide is warranted.     

A型禽流感在人类中的年龄分布

截至2006年7月4日,在这之前的30个月内,从非洲、亚洲和欧洲报告给世界卫生组织(WHO)已经确诊的人感染A型禽流感(H5N1)病例为229例[1]。WHO注意到确诊病例集中分布于儿童和青壮年中,在大年龄组中病例相对较少[2]。尽管一系列的     

人文素质与妇产科专业教育精准融合的实践

本研究从医学院校人文素质教育现状展开,分析了人文素质与专业教育精准融合的必要性和可行性,列表归纳人文素质与妇产科知识的精准融合点。继而以妇产科典型教学为例,阐释了“珍爱生命”“抗挫折能力”等融合点的具体实施,以及对这种精准融合教学的反思。     

Effects of Exercise Training on Restless Legs Syndrome,Depression, Sleep Quality,and Fatigue Among Hemodialysis Patients: A Systematic Review and Meta-analysis

Context

Hemodialysis (HD) patients experience a heavy symptom burden that leads to a decreased quality of life. Pharmacological treatment is effective but costly and has adverse effects. Exercise is a promising approach for symptom management, but the effect of exercise on restless legs syndrome (RLS), depression, sleep quality, and fatigue in HD patients is still uncertain.

任脉与脑相关探析

目的:从祖国医学的角度探讨任脉与脑相关。方法:根据任脉循行,从督脉为阳脉之海、任脉为阴脉之海、阴阳平衡学说等理论,推测不仅督脉对脑缺血损伤有修复作用,任脉在脑缺血损伤中可能也起着非常重要的作用。结论:我们推测任脉与脑相关。