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PubMed1979

Cannabinols and feeding in sheep.

Marijuana, long used for the euphoria which results, recently has been found to stimulate hunger in humans but in several laboratory animals cannabinoids decrease food intake. Sheep, relatively more sensitive to chemicals that affect food intake, were injected IV with the d-and l-isomers of tetrahydrocannabinol and with a 9-aza-cannabinol) 9-AC) (8-(1,2-dimethylheptyl)-5,5-dimethyl-5H-[1]benzopyranol[3,4]pyridin-10-01, HCL) and feeding behavior was monitored. In the first 30 min, food intake was increased by the l-isomer and by 9-AC but not affected by d-delta 9-THC. After 24 h, feed intake was decreased by at least one dose of d-and l-delta 9-THC and 9-AC. The l-but not d-isomer was active at very low doses compared with doses used in many laboratory animals.

Animals↗
PubMed1978

Purine reutilization and synthesis de novo in long-term human lymphocyte cell lines deficient in adenine phosphoribosyltransferase activity.

Clonal lines, with either partial or total deficiency of adenine phosphoribosyltransferase (APRT) were derived from the WI-L2 long-term human lymphocyte line by selection for resistance to the adenine analogs 8-azaadenine or 2,6-diaminopurine. Resistance to 8-azaadenine also conferred resistance to 2,6 diaminopurine and vice versa. Cells with 30--40% of wild-type APRT activity were selected by resistance to 0.01 mM 2,6-diaminopurine or 1.40 mM 8-azaadenine. The APRT in the 8-azaadinine-resistant cells exhibited a four- to sevenfold increase in the apparent Km for adenine. Activities of three other purine reutilization and interconversion enzymes in the resistant cells, including hypoxanthine phosphoribosyltransferase (HPRT), adenosine kinase, and adenosine deaminase, were within the range of wild-type activities. The doubling times of the APRT-deficient cells in purine-free medium was not different from wild-type cells. The APRT in the 8-azaadenine-resistant cells did not have an altered mobility in glycerol gradients as compared to wild-type cells. The rate of purine synthesis de novo and intracellular levels of 5-phosphoribosyl-1-pyrophosphate were unchanged in the APRT-deficient cells as compared to WI-L2. The ability of the cells to reutilize exogenous adenine, however, was severely impaired.

Adenine↗
PubMed1998

Comparative in vitro activity of BAY 12-8039 and five other antimicrobial agents against anaerobic bacteria.

The in vitro activity of BAY 12-8039 against 360 anaerobic clinical isolates was determined by the agar dilution method and compared to that of five other antimicrobial agents. BAY 12-8039 and imipenem were the most active agents tested. The following MIC90 values were determined for BAY 12-8039: Peptostreptococcus spp. (50 isolates), 1 mg/l; Propionibacterium acnes (30 isolates). 0.25 mg/l; Clostridium perfringens (30 isolates), 0.5 mg/l; Clostridium difficile (50 isolates), 2 mg/l; Bacteroides fragilis (50 isolates), 1 mg/l; non-fragilis Bacteroides, Porphyromonas, and Prevotella spp. (100 isolates), 2 mg/l; and Fusobacterium spp. (50 isolates), 0.25 mg/l. The results of the present study show that BAY 12-8039 may be useful in the treatment and prophylaxis of anaerobic infections.

Anti-Infective Agents↗
PubMed1977

Electron spin resonance studies of an animal model of human congenital myotonia: increased erythrocyte membrane fluidity in rats with 20,25-diazacholesterol-induced myotonia.

Electron spin resonance experiments have been performed on erythrocyte membranes from rats with myotonia induced by treatment with 20,25-diazacholesterol. The results suggest that erythrocyte membranes in this animal model of human congenital myotonia possess a highly significantly increased surface membrane fluidity compared to that of controls. Alterations in the physical state of membrane proteins were not apparent. These findings, also present in human congenital myotonia [Butterfield, Chesnut, Roses & Appel, 1976, Nature (London) 263:159; Butterfield, 1977 (Submitted for publication)], strengthen the concepts that increased membrane fluidity is associated with the presence of myotonia and that congenital myotonia may be a diffuse membrane disease.

Amino Acids, Sulfur↗
PubMed1981

Inhibition of antigen-induced histamine release from rat mast cells by a cyclic GMP-phosphodiesterase inhibitor and sodium nitrite.

Antianaphylactic properties have been attributed to cyclic nucleotide phosphodiesterase inhibitors through increase of cyclic AMP levels, according to the concept that increases in cyclic AMP reduce release and increases in cyclic GMP enhance release. However, Coulson et al. [3] showed that the inhibition of histamine release from human lung is correlated to the inhibition of cyclic GMP hydrolysis. We studied the effect of specific inhibitors of cyclic AMP and cyclic GMP hydrolysis on the antigen-induced mediator release from rat mass cells and human basophils and on airways relaxation [4]. The results suggested that the modulation of mediator release was different from one cell type to the other, enhancement of cyclic AMP levels leading to the inhibition of release from basophils, while cyclic GMP appears to be predominantly involved in mast cells. The present paper shows that high concentrations of sodium nitrite, a stimulating agent of guanylate cyclase, inhibit histamine release from rat mast cells in the presence or absence of M&B 22948, a selective cyclic GMP phosphodiesterase inhibitor.

3',5'-Cyclic-GMP Phosphodiesterases↗
PubMedDate not supplied

Antibacterial activity of the fourth-generation fluoroquinolones gatifloxacin and moxifloxacin against ocular pathogens.

The ideal ophthalmic anti-infective exhibits broad-spectrum activity against gram-positive, gram-negative, and atypical bacterial species. These pathogens can cause potentially blinding infections such as keratitis and endophthalmitis, both of which are associated with ophthalmic surgery or traumatic injury. These infections often require aggressive antibacterial therapy, preferably with newer generations of antibiotics. In this study, minimal inhibitory concentration (MIC) values for gatifloxacin and moxifloxacin were determined in vitro against bacterial strains that were isolated from suspected cases of bacterial keratitis and endophthalmitis. The ocular isolates included 7 gram-positive, 4 gram-negative, and 3 atypical bacterial species. Gatifloxacin and moxifloxacin exhibited similar activity against 6 gram-positive organisms: Staphylococcus epidermidis, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Bacillus cereus, and Enterococcus faecalis. MIC90 values for the drugs against these isolates ranged from 0.08 mg/mL to 0.57 mg/mL and were comparable to previously published values against isolates from patients with systemic infections. The MIC90 for gatifloxacin against Streptococcus viridans was 0.22 mg/mL compared with 0.73 mg/mL for moxifloxacin (P = .011). Among the gram-negative isolates, the mean MIC90 for gatifloxacin against Pseudomonas aeruginosa was 1.28 mg/mL compared with 2.60 mg/ mL for moxifloxacin (P = .023). MIC90 values for gatifloxacin against Klebsiella pneumoniae and Enterobacter aerogenes were one fourth to one fifth the values for moxifloxacin. For the atypicals, the MIC90 values for gatifloxacin against Nocardia asteroides and Mycobacterium chelonae were one fourth the corresponding values for moxifloxacin. Gatifloxacin demonstrated a broad spectrum of activity against several key ocular pathogens tested in this study and was at least as effective as moxifloxacin against these pathogens.

Anti-Bacterial Agents↗
PubMed2001

Ciprofloxacin- and methicillin-resistant staphylococcus aureus susceptible to moxifloxacin, levofloxacin, teicoplanin, vancomycin and linezolid.

In order to determine the comparative efficacy of vancomycin, teicoplanin, levofloxacin, moxifloxacin, and linezolid against methicillin- and ciprofloxacin-resistant Staphylococcus aureus, each agent was tested against 65 genetically different strains using the microbroth dilution method. All of the isolates were typed using the enterobacterial repetitive intergenic consensus polymerase chain reaction to exclude multiple isolates of epidemic clones. Susceptibility testing revealed that all of the isolates were susceptible to vancomycin and teicoplanin. Linezolid exhibited minimum inhibitory concentration (MIC) levels ranging from 1 to 4 mg/l (MIC90, 4 mg/l). The MICs of moxifloxacin and levofloxacin ranged from 0.01 to 8 mg/l (MIC90, 8 mg/l) and 0.25 to 32 mg/l (MIC90. 16 mg/l), respectively. Thus, linezolid is active against methicillin- and ciprofloxacin-resistant Staphylococcus aureus, whereas moxifloxacin may need to be administered at a dose higher than recommended in order to successfully treat serious infections.

Acetamides↗
PubMed2006

[Pathogenesis, diagnosis and therapy of Legionella infections].

Legionella species are ubiquitous in aquatic environments. About 50 years ago they entered the engineered (technical) environment, i.e. warm water systems with zones of stagnation. Since that time they represent a hygienic problem. After transmission to humans via aerosols legionellae might cause Legionella pneumonia (legionnaires' disease) or influenza-like respiratory infections (Pontiac fever). Epidemiological data suggest that Legionella strains might differ substantially in their virulence properties. Although the molecular basis is not understood L. pneumophila serogroup 1 especially MAb 3/1-positive strains cause the majority of infections. The main virulence feature is the ability to multiply intracellularly. After uptake into macrophages legionellae multiply in a specialized vacuole and finally lyse their host cells. Several bacterial factors like surface components, secretion systems and iron uptake systems are involved in this process. Since the clinical picture of Legionella pneumonia does not allow differentiation from pneumoniae caused by other pathogens, microbiological diagnostic methods are needed to establish the diagnosis. Cultivation of legionellae from clinical specimens, detection of antigens and DNA in patients' samples and detection of antibodies in serum samples are suitable methods. However, none of the diagnostic tests presently available offers the desired quality with respect to sensitivity and specificity. Therefore, the standard technique is to use several diagnostic tests in parallel. Advantages and disadvantages of the diagnostic procedures are discussed. Therapeutic options for Legionella infections are newer macrolides like azithromycin and chinolones (ciprofloxacin, levofloxacin and moxifloxacin).

Anti-Bacterial Agents↗