Methods for preparing standardized glycol methacrylate (GMA) based embedding media for use in light microscopy in a rational, precise and reproducible manner are described . The application of these procedures resulted in a versatile, low toxicity GMA embedding medium. GMA embedding medium and resin blocks were tested utilizing a variety of physico-chemical techniques, namely: gas chromatograph...

Glucokinase (GK) has a major role in the control of blood glucose homeostasis and is a strong potential target for the pharmacological treatment of type 2 diabetes. We report here the mechanism of action of two novel and potent direct activators of GK: 6-[(3-isobutoxy-5-isopropoxybenzoyl)amino]nicotinic acid(GKA1) and 5-([3-isopropoxy-5-[2-(3-thienyl)ethoxy]benzoyl]amino)-1,3,4-thiadiazole-2-ca...

The natural product rapamycin has been used to provide temporal and quantitative control of gene expression in animals through its ability to interact with two proteins simultaneously. A shortcoming of this approach is that rapamycin is an inhibitor of cell proliferation, the result of binding to FKBP12-rapamycin-associated protein (FRAP). To overcome this limitation, nontoxic derivatives of ra...

The benzannulation reaction of Fischer carbene complexes is investigated under conditions where the reaction of the carbene complex is occurring in the presence of two different alkynes. A series of competition experiments are examined where the effects of various structural factors are explored by pitting 10 different carbene complexes with 11 different alkynes. Terminal alkynes will react sel...

The reproductive toxicity of propoxur (2-isopropoxy-phenyl-N-methylcarbamate), a carbamate pesticide, was investigated in adult male Wistar rats exposed to 0, 1.73, 2.6, and 5.2 mg/kg body weight/day for 90 successive days. Results obtained from this study showed a significant (p < 0.05) concentration-dependent increase in food consumption, relative weights of testis, epididymis and kidneys wit...

Protease-activated receptors (PARs) are widely expressed throughout the respiratory tract, and PAR(2) has been investigated as a potential drug target for inflammatory airway diseases. The primary focus of this study was to determine the extent to which PAR(2)-activating peptides modulate lipopolysaccharide (LPS)-induced airway neutrophilia in mice and establish the underlying mechanisms. Intra...

BACKGROUND The rapid desensitization of the human prostacyclin (IP) in response to agonist binding has been shown in cell culture. Phosphorylation of the IP receptor by protein kinase C (PKC) has been suggested to be involved in this process. METHODS AND RESULTS In this study we investigated the vasodilatory effects of iloprost, a stable prostacyclin analogue, in perfused rabbit lungs. Contin...

It might be seen as reckless to challenge to create single-agents for the treatment of both type 1 diabetes caused by the destruction of the Langerhans β cells in pancreas by excessive autoimmunity, and type 2 diabetes caused by the obesity. However, we hypothesized that retinoid X receptor (RXR) agonists, which are researched for the treatment of type 2 diabetes, will also be useful like metfo...

The current study belongs to a series of investigations of polycyclic aromatic compounds containing intramolecular hydrogen bonds. Close proximity of the coupled aromatic system and hydrogen bridges gives rise to resonance-assisted hydrogen bonding phenomena. Substituted naphthols are ideally suited for this kind of investigation. The parent compound, 1-hydroxy-8-methoxy-3-methylnaphthalene, an...

A series of second-generation ruthenium olefin metathesis catalysts was investigated using a combination of reaction kinetics, X-ray crystallography, NMR spectroscopy, and DFT calculations in order to determine the relationship between the structure of the chelating o-alkoxybenzylidene and the observed initiation rate. Included in this series were previously reported catalysts containing a vari...