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Biomedical subjects

E Ferguson

Publications and source records attributed to E Ferguson.

At least 73 records · Page 4Linked to original sources
PubMed1991

Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2 H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors.

A series of substituted quinoline mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase both in vitro and (cholesterol biosynthesis) in vivo. Since previous studies suggested that the 4-(4-fluorophenyl) and 2-(1-methylethyl) substituents afforded optimum potency, attention was focused on variations at position 6 of the quinoline ring. Biological evaluation of a small number of analogues bearing a variety of 6-substituents showed that modification at this position had little effect on potency. Several compounds (8b, 8e, and 11) were identified that showed comparable potency to compactin and mevinolin in both the in vitro and in vivo assays.

Animals↗
PubMed1990

Hep-G2 cells and primary rat hepatocytes differ in their response to inhibitors of HMG-CoA reductase.

CI-981, a novel synthetic inhibitor of HMG-CoA reductase, was previously reported to be highly liver-selective using an ex vivo approach. In order to determine liver-selectivity at the cellular level, CI-981 was evaluated in cell culture and compared to lovastatin, pravastatin, fluvastatin and BMY-21950. Using human cell lines, none of the compounds tested showed liver-selectivity, i.e. strong inhibition of cholesterol synthesis in Hep-G2 cells (liver model) but weak inhibition in human fibroblasts (peripheral cell model). In contrast, all drugs tested produced equal and potent inhibition of sterol synthesis in primary cultures of rat hepatocytes, and CI-981, pravastatin and BMY-21950 were more than 100-fold more potent in rat hepatocytes compared to human fibroblasts. Since all compounds were also equally potent at inhibiting sterol synthesis in a rat subcellular system and in vivo, the data suggest that the use of Hep-G2 cells may not be the cell system of choice in which to study inhibition of hepatic cholesterogenesis or to demonstrate liver selectivity of inhibitors of HMG-CoA reductase.

Animals↗
PubMed1990

Effects of single doses of alpidem, lorazepam, and placebo on memory and attention in healthy young and elderly volunteers.

The aim of the present study was to compare the effects of alpidem, a new imidazopyridine derivative with benzodiazepine-like anxiolytic effects, with those of lorazepam and placebo on memory and attention in two age groups of healthy volunteers. The study design was that of a randomized double-blind crossover trial with 12 young (18-30 years old) and 12 elderly (65-80) subjects. At weekly intervals, each subject was administered single oral doses of 25 mg alpidem, 50 mg alpidem, 1 mg lorazepam, and placebo in a randomized sequence. Computerized memory and attention tests were performed 90 minutes before and 320 minutes after drug administration. Lorazepam and alpidem 50 mg produced memory impairments: for verbal memory tests the difference against placebo was highly significant for both drugs, while for visual memory this impairment was significant for lorazepam only. No memory effects were seen with 25 mg alpidem. There were no significant drug effects on attention, suggesting a specific amnestic effect not explained by general sedation. Performance of the elderly subjects was much lower than that of the younger ones in both memory and attention tasks. It was not possible to observe any interaction effects between drug and age.

Adolescent↗
PubMed1984

Serum and muscle potassium in experimental alcoholic myopathy.

We investigated the possible role of potassium deficiency, a recognized cause of myopathy, in the pathogenesis of experimental acute alcoholic myopathy (EAM) in the rat. Alcohol-treated animals receiving the same dietary potassium as controls developed mild hypokalemia; however, muscle potassium was preserved or elevated even in the presence of scattered muscle fiber necrosis. Increasing dietary potassium raised serum potassium but did not prevent EAM. These data indicate that hypokalemia in EAM is due to potassium redistribution between intra- and extracellular compartments rather than potassium deficiency, and confirm clinical observations that alcohol-induced muscle injury occurs independently of potassium deficiency.

Acute Disease↗
PubMed1984

Operations of choice for cancers of the colon and rectum. An overview.

Despite proven guidelines, rational management proposals, and effective surgical therapies, surgical resections not in accord with national norms continue to be used. Refinement of existing knowledge can improve the marginal results of the past. A simple overview is presented. Management of cancer of the cecum, ascending colon, hepatic and splenic flexures, transverse colon, descending, sigmoid, and rectosigmoid colon are graphically presented. Multiple large bowel polyps, chronic ulcerative colitis with tendency to neoplasia, and multiple polyposis are briefly discussed as to proper surgical management. A similar succinct overview of individual polyp management is diagrammatically shown. Cancer management of the rectum including adenocarcinoma, squamous cell, cloacogenic and villous tumors are shown as well as the management of basal cell and squamous cell lesions of the anal verge.

Cecal Neoplasms↗
PubMed1982

Sensitivity to two-stage carcinogenesis of SENCAR mouse skin grafted to nude mice.

SENCAR mice are extremely susceptible to two-stage skin carcinogenesis, while BALB/c mice are relatively resistant. Skin grafts to BALB/c nude mice were performed with full-thickness skin from SENCAR and BALB/c donors, and tumor formation was monitored in grafted skin, surrounding host skin, and intact SENCAR, BALB/c and nude mice. Initiation was accomplished by exposure to 20 micrograms dimethylbenz(a)anthracene and promotion by repeated exposure to 12-O-tetradecanoylphorbol-13-acetate. SENCAR skin retained a high sensitivity to carcinogenesis when grafted to nude hosts, whereas BALB/c skin remained resistant. The donor type did not influence the tumor yield in surrounding nude host skin. The rate of tumor regression was not altered in SENCAR skin grafts on nude mice relative to intact SENCAR skin. These results indicate that the unusual sensitivity of SENCAR epidermis to chemical carcinogenesis is not due to altered systemic factors but is a property of the skin itself.

9,10-Dimethyl-1,2-benzanthracene↗
PubMed1976

A method for the estimation of total calcium in serum or heparinized plasma.

A simple titrimetric method for the determination of total calcium in serum or heparinized plasma is described. After removing interfering substances with an ion-exchange resin, calcium is reacted with glyoxalbis (2-hydroxyanil), GBA, and the resulting red colour titrated with ethylenediaminetetra-acetic acid in the presence of a methanol/glycerol mixture. No special equipment is used, deproteinization is not necessary and only 0.2 ml of sample is required.

Autoanalysis↗