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PubMed2002

[Na and Mg K-edge XANES study in silicate glasses].

The structural role of Na in Na2-O-SiO2 and Na2O-SiO2-P2O5 glasses was studied using Na K-edge XANES (X-ray near edge structure) spectra. The Na K-edge XANES shows little change with increase in the content of Na2O in Na2O-SiO2 glasses. However, the addition of P into the Na2O-SiO2 system causes dramatic change of the Na K-edge XANES, and the Na K-edge spectra of Na2O-SiO2-P2O5 glasses also change with the increase of P2O5 content. The structural role of Mg in CaMgSi2O6 (Di)--NaAlSi3O8 (Ab) glasses was studied using Mg K-edge XANES spectra. The Mg-O bond distance in these glasses is estimated to be 2.00 +/- 0.04 A. Thus, Mg in these glasses may be five coordinated with oxygen, or Mg may have multiple structural sites, MgIV, MgV and MgVI. The Di-Ab glasses may possess a medium-range ordering structure.

Glass↗
PubMed1982

Accumulation of cimetidine by kidney cortex slices.

The mechanisms involved in the excretion of the histamine H2-receptor antagonist cimetidine are as yet incompletely understood. The purpose of this study was to examine the interaction of cimetidine with incubated slices of dog kidney cortex. The results of time and concentration-dependent experiments by using 3H-labeled cimetidine demonstrated that the drug was accumulated without metabolism against a concentration gradient by a saturable process. Inhibition of uptake by cyanide and by incubation under a nitrogen atmosphere indicated energy dependence. Uptake of cimetidine by active cationic transport was likely inasmuch as both cyanine 863 and quinine blocked accumulation. However, a probenecid-sensitive component, accounting for about 20% of steady-state accumulation, also was identified. The lack of inhibitory action of p-aminohippuric acid and the cationic nature of the cimetidine molecule suggest the probenecid-sensitivity was not related to the renal organic anion mechanism. Further, probenecid inhibition was not due to a generalized cellular toxicity because maximally inhibitory concentrations of probenecid did not interfere with uptake of the cation tetraethylammonium.

Animals↗
PubMed1975

Inhibition of the ocular effects of sodium arachidonate by anti-inflammatory compounds.

Topical administration of aqueous solutions of sodium arachidonate to the eyes of rabbits increases intraocular pressure, constricts the pupil and increases both the protein and prostaglandin content of aqueous humor. Arachidonic acid itself dissolved in arachis oil is less effective than sodium arachidonate, although addition of polysorbate mono-oleate greatly increases the effects produced by arachidonic acid. Pretreatment with topically applied non-steroidal anti-inflammatory agents prevents the ocular effects of sodium arachidonate, indomethacin being 2-4 times as potent as either indoxole or pirprofen. Dexamethasone was without effect in these experiments. The results suggested that nonsteroidal anti-inflammatory agents deserve serious consideration for topical use in the treatment of ocular inflammation.

Administration, Topical↗
PubMed1990

No-carrier-added (NCA) N-(3-[18F]fluoropropyl)-N-norbuprenorphine and N-(3-[18F]fluoropropyl)-N-nordiprenorphine--synthesis, anatomical distribution in mice and rats, and tomographic studies in a baboon.

N-(3-Fluoropropyl)-N-norbuprenorphine (3a) and N-(3-fluoropropyl)-N-nordiprenorphine (4a) were synthesized by N-alkylation of norbuprenorphine (1) and nordiprenorphine (2) with 1-bromo-3-fluoropropane. The corresponding no-carrier-added (NCA) N-(3-[18F]fluoropropyl)-N-norbuprenorphine (3b) and N-(3-[18F]fluoropropyl)-N-nordiprenorphine (4b) were synthesized by N-alkylation of 1 and 2 with NCA 1-[18F]fluoro-3-iodopropane in a synthesis time of approximately 100 min from end of bombardment (EOB) with an overall radiochemical yield of approximately 15% (EOB) and a mass of 2-3 nmol. In vitro studies indicate that in the absence of sodium chloride, compounds 3a, 4a, N-propyl-N-norbuprenorphine (5), buprenorphine and diprenorphine are reasonably comparable in binding affinity for opioid receptors. In the presence of 100 mM sodium chloride, however, compounds 3a, 4a and 5, are clearly less potent than buprenorphine and diprenorphine. The anatomical distribution study of compound 3b in mice shows radioactivity accumulating in bone, indicating that in vivo defluorination may have occurred. Rat studies of both compounds 3b and 4b indicate the specific distribution of these two radioligands within certain cortical and subcortical regions of rat brain. However, the absolute uptake of compound 4b in rat brain was only half that of compound 3b. PET studies of 3b in a baboon revealed specific binding of compound 3b in striatum and cerebellum. At 1 h after injection, ratios of specific/non-specific binding of 3b in striatum and cerebellum of a baboon were 1.9 and 1.7 respectively.

Animals↗