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At least 595 records · Page 33Linked to original sources
PubMed1975

The metabolism of the local anaesthetic fomocaine (1-morpholino-3-[p-phenoxymethylphenyl]propane) in the rat and dog after oral application.

1. The metabolism of fomocaine following its oral administration to male and female Wistar rats and male beagle dogs has been qualitatively investigated. 2. The drug is metabolized in both species by aromatic hydroxylation, N-oxidation, splitting of the ether link and, in the dog, by removal of the morpholine group. 3. The rat and dog excrete some unchanged fomocaine in the urine together with p-hydroxyfomocaine (free and conjugated), fomocaine-N-oxide, p-hydroxyfomocaine-N-oxide and p-(gamma-morpholinopropyl)benzoic acid. In addition, the dog excretes morpholine in the urine.

Administration, Oral↗
PubMed1981

Metabolism of the epoxy resin component 2,2-bis[4](2,3]epoxypropoxy)phenyl]propane, the diglycidyl ether of bisphenol A (DGEBPA) in the mouse. Part I. A comparison of the fate of a single dermal application and of a single oral dose of 14C-DGEBPA.

1. 14C-DGEBPA dermally applied to mice was only slowly eliminated in the feces (20% dose) and urine (3%), as a mixture of metabolites, over three days. Most of the applied radioactivity (66% dose) was extracted from the application area and its covering foil. 2. When 14C-DGEBPA was given orally to mice it was rapidly excreted; 80% of the administered 14C was eliminated in the feces and 11% in the urine 0-3 days after a single oral dose. 3. The urinary faecal metabolite profiles derived from dermal application and oral dosing were essentially similar.

Administration, Oral↗
PubMed1981

Metabolism of the epoxy resin component 2,2-bis[4-(2,3-epoxypropoxy)phenyl]propane, the diglycidyl ether of bisphenol A (DGEBPA) in the mouse. Part II. Identification of metabolites in urine and faeces following a single oral dose of 14C-DGEBPA.

1. The major metabolic transformation of orally ingested 14C-DGEBPA is by hydrolytic ring-opening of the two epoxide rings to form diols. This metabolite (the bis-diol of DGEBPA) is excreted in both free and conjugated forms and is further metabolized to various carboxylic acids, including two containing a methylsulphonyl moiety. 2. The product of oxidative dealkylation either of DGEBPA (with concomitant formation of glycidaldehyde) or of the bis-diol of DGEBPA (with concomitant formation of glyceraldehyde) is excreted in both free and conjugated forms in amounts representing 5% of the dose. 3. The high activity of epoxide hydratase towards DGEBPA suggests that glyceraldehyde and not glycidaldehyde is formed in vivo. 4. Hepatic epoxide hydratase activity towards DGEBPA measured in vitro decreased in the order rabbit greater than mouse greater than rat. 5. Two discrete epoxide hydratases are present in large amounts in the mouse. One is membrane-bound in the liver microsomal fraction and the other is a "soluble' enzyme located in the liver cytosol. This cytosolic enzyme was present in only very small amounts in the rat.

Administration, Oral↗
PubMed1998

Local health care system utilizing the LPG (liquid propane gas) network.

JAC's LPG monitoring network system is mainly provided in mountain villages. However, by using this system, it will be possible to start a Digital Network Program for the Elderly while maintaining superior economic feasibility and public benefit using existing information infrastructures. This project also has the capabilities for the creation of a fire/disaster monitoring system, as well as a health care system by using conventional LPG monitoring systems. Telemedicine is an option for the future, as well, by connecting medical equipment and a tele-conferencing system.

Aged↗
PubMed2000

Sulphur mustard induced oxidative stress and its prevention by sodium 2,3-dimercapto propane sulphonic acid (DMPS) in mice.

Sulphur mustard [bis(2-chloro ethyl) sulfide] (SM), a bifunctional alkylating agent has been frequently used as a chemical warfare agent. In the present study, the effects of sodium 2-3-dimercaptopropane sulphonic acid (DMPS) on some biochemical and histological parameters in mice, exposed to 1/4LC50 concentration of SM vapor (10.5 mg/m3) were examined over a period of seven days. Exposure of SM resulted in a significant loss of blood, hepatic and pulmonary glutathione (GSH) and an elevation of hepatic and pulmonary oxidized glutathione (GSSG). These biochemical changes were accompanied by a number of histopathological alterations. The most prominent was congestion and degeneration in viscera and obliteration of chromatin material. These biochemical and histopathological changes were less marked in animals pre-administered with DMPS followed by DMPS exposure indicating some protective value of the thiol (DMPS) against SM induced oxidative injury in mice.

Animals↗
PubMed2001

Interaction of 2,3-dimercapto-1-propane sulfonate with the human organic anion transporter hOAT1.

The kidney is the primary target organ in which inorganic mercury (Hg2+) accumulates and expresses its toxic effects. The chelating agent 2,3-dimercapto-1-propanesulfonic acid (DMPS) can rapidly reduce the renal burden of mercury and increase the urinary excretion of mercury. However, the cellular and molecular basis of its efficacy is still unknown. A number of previous studies implicated the "classical organic anion secretory pathway" in the secretion of DMPS and its chelation products. In this study we used the human ortholog of the organic anion transporter (hOAT1) expressed in the Xenopus oocyte expression system to study the interaction of DMPS and its mercury chelates with hOAT1. [3H]PAH was used to show the transport activity of hOAT1 (Km = 3.9 +/-1.3 microM). Uptake of [3H]para-aminohippuric acid (PAH) was inhibited by reduced DMPS (K(i) = 22.4 +/- 8.4 microM). We also investigated the interaction of oxidized DMPS with hOAT1 because it has been shown that at least 80% of DMPS in the blood is oxidized within 30 min. Oxidized DMPS also inhibited uptake of [3H]PAH (K(i) = 66 +/-13.6 microM). In contrast, we found no interaction of the DMPS-Hg chelate with hOAT1. To determine whether DMPS and oxidized DMPS are transported by hOAT1 we examined the effect of inwardly directed gradients these two compounds on efflux of [3H]PAH from HeLa cells transiently transfected with hOAT1. Gradients of both DMPS and oxidized DMPS significantly trans-stimulated efflux of [3H]PAH. These data suggest that hOAT1 can transport DMPS and oxidized DMPS, whereas the DMPS-Hg chelate has no significant affinity for the transporter.

Albumins↗