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At least 19 recordsLinked to original sources
PubMed1999

Studies of technetium-99m nitridobisdithiocarboxylate leucocyte specific radiopharmaceutical: [99mTcN(DTCX)2], DTCX = CH3(CH2)8CS2. The cellular and subcellular distribution in human blood cells, and chemical behaviour. Synthesis of the analogous rhenium-188 radiopharmaceutical.

The distribution of the radiopharmaceutical ([99mTcN(DTCX)2], DTCX = CH3(CH2)8CS2) in the leucocyte population determined by a density separation with double gradient Polymorphprep was studied. Microautoradiographic analysis showed a subcellular distribution of the radiomarker in human blood cells. This technique confirmed the observed lymphocyte selectivity (69%) and revealed that the uptake was predominantly cytoplasmic around the nucleus. A labeling mechanism by passive endocytosis could be proposed involving a required lipophilicity of the radiopharmaceutical for lymphocyte targeting. Finally, we describe the new synthesis with an efficient yield and radiochemical purity of the analogous radiopharmaceutical [188ReN(DTCX)2].

Autoradiography↗
PubMed1995

Radiopharmaceuticals 1994. Nil desperandum. European Association of Nuclear Medicine Committees on Radiopharmaceuticals and Positron Emission Tomography.

On the basis of the discussions at a symposium held in Düsseldorf and attended by representatives of various interested bodies, European legislation as it affects radiopharmaceuticals is reviewed. Due consideration is given to the new, centralised and decentralised, registration procedures, effective since 1 January 1995. The dossier required to support an application for marketing authorisation is discussed, separate consideration being given to single-photon emitters, therapeutic radio-nuclides and positron-emitting radiopharmaceuticals. The role of the European Pharmacopoiea is also considered. It is concluded that the new, modified procedures for the registration of medicinal products in the European Union may actually inhibit free availability of radio-pharmaceuticals within the Community, and that there is a strong case for modification of the European Directives so that radiopharmaceuticals are placed in a separate category to therapeutic drugs, with less stringent registration requirements.

Cost-Benefit Analysis↗
PubMed1993

EEC directives and guidelines applicable to radiopharmaceuticals--1993. Status quo with particular emphasis on the registration of radiopharmaceuticals which were on the market prior to January 1992.

The manufacture, scale and supply of radiopharmaceuticals in the EEC is regulated by directives that are incorporated into the national laws of the member states. The situation as of 1 January 1993 was not too optimistic, however, as the processing of licensing applications had been completely misjudged. Not one product had been registered as of 1 January. The costs involved are also high and since the European market for radiopharmaceuticals is relatively small, the market cannot afford this. It would appear that the EEC directives are inadequate and too non-specific, so revision is indicated.

Chemistry, Pharmaceutical↗
PubMed1986

[Detection of endotoxins in radiopharmaceutical preparations--III. Limulus test assessment using radiopharmaceutical preparations; correlation with the rabbit pyrogen test].

Experiments using 17 radiopharmaceuticals containing known amounts of added endotoxin show that none of them inhibits the pyrogenic reaction of the rabbit. Gelation of the Limulus amoebocyte lysate (LAL) is inhibited by 4 of them: colloidal erbium 169Er citrate, colloidal rhenium 186Re sulfide, colloidal technetium 99mTc (Re) sulfide for liver scintigraphy and the colloidal technetium 99mTc (Re) sulfide for lymphography. This inhibition is cancelled, either by dilution or after neutral pH adjustment. Both controls were performed on 313 batches of various radiopharmaceuticals, 95% of results were identical (93% negative, 2% positive). The remaining 5% correspond to positive LAL tests vs negative rabbit tests on the same batches. No negative LAL test vs positive rabbit test was observed.

Animals↗
PubMed1990

Cysteine, a chelating moiety for synthesis of technetium-99m radiopharmaceuticals: II. Attempt to synthesize renal tubular radiopharmaceuticals.

N-acyl glycine residue is known to interact with renal tubular transport enzymes and thereby promotes renal tubular secretion. Recently, a similar renal property was also observed with dioxotechnetium aminocarboxy chelates. Therefore, a radiopharmaceutical was designed containing both the above groups with the expectation that an efficient 99mTc labelled renal tubular agent could be developed by this process with which evaluation of various renal parameters will be possible. The synthesized compound, though secreted through the renal tubular pathway, did not show the expected efficiency. It was indicated that the renal property of the molecule was entirely due to chelated dioxotechnetium moiety and the expected effect of the acyl glycine residue was not observed in the molecule.

Animals↗
PubMed1983

Quantitative autoradiography with radiopharmaceuticals, Part 2: Applications in radiopharmaceutical research: concise communication.

We describe the application of macroautoradiography, a relatively simple, quantifiable method for the evaluation of positron-emitting and gamma-emitting radiopharmaceuticals. We have investigated the response properties of two types of film to positron (F-18) and negatron (C-14) emitters. Variations in the response of film to increasing film-to-source distance are described, along with the effects of different intensifying screens and mounting tape. Digitization of whole-body autoradiograms (WBARG) in small animals was performed by using a videodensitometry system (videocamera interfaced to a computer). Quantitation was derived from analysis of a series of step-wedge standards that covered the range of radioactivities in the sample. By using a close-up lens on the videocamera, a 2- by 2-cm field is digitized as a 128 X 128 array, each pixel representing 156 X 156 micron. The effect of chlorpromazine (CPZ) on glucose metabolism in mice was studied by giving C-14 2DG followed by CPZ and F-18 FDG in the same animal. Muscle activity decreased and brown-fat activity increased. The high spatial resolution of this technique enables quantification in structures as small as the basal ganglia in mice. The use of dual-nuclide ARG permits each animal to be its own control, which greatly increases the utility of this method.

Animals↗