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Various asymmetric or cyclic ester derivatives of the phosphonic acid moiety in the calcium antagonist fostedil (KB-944) were synthesized. The coronary vasodilator activity of these compounds was assessed by Langendorff's method. Among them, the ethyl isopropyl ester 12 showed the most potent activity, which was comparable to that of fostedil.
A similar distribution of 99Tcm, 45Ca and 85Sr was obtained when injected in rats as 99Tcm-labelled pyrophosphate or ethylene-1-hydroxy-1,1-diphosphonate (EHDP), 45Ca-chloride and 85Sr-choloride respectively. The highest concentrations occurred in bone and teeth. In EHDP-treated rats, isotopes were accumulated at sites of ectopic calcifications in the lung, kidney and stomach wall as well as in mineralized tissues. These results indicate that 99Tcm, when administered as 99Tcm-labelled EHDP accumulates predominatly in the inorganic rather than organic tissue components.
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Microorganisms, which mineralize organophosphates (216 isolates) have been isolated for the chernozem soils of different regions of Ukraine. Sixteen most active strains referred to Bacillus genus have been identified and studied. These microorganisms grow (with different intensity) on the mineral medium with glucose and glycerophosphate or phytin, accumulating phosphate-ions in the medium. The most active strains mineralized glycerophosphate, accumulating about 280 micrograms/ml of PO4(3-) and phytin accumulating up to 130 micrograms/ml of PO4(3-) during 3 days. New strains of bacilli have been chosen for creation of combined bacterial preparations of the complex effect.
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