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At least 1,333 records · Page 74Linked to original sources
PubMed2000

[Application of radionuclides in pharmaceutical fields].

Application studies of radionuclides in pharmaceutical fields are described concerning two major categories, such as the use of gamma-emitter in nuclear medicine and beta-emitter in tracer investigation. In the former radionuclide an effort has been made to develop radioactive new diagnostic agents in the nephro-urology field. Of several agents examined two new radiopharmaceuticals, 99mTc-malic acid and 99mTc-dimercaptopropionic acid proved to be sufficient for renal imaging with adequate concentration in experimental animals and humans. Useful information was obtained for diagnosis of renal diseases using both the labeled agents. Identification and purity tests of radiopharmaceuticals also set forth for official compendia such as the Japanese pharmacopoeia and so on. In the latter one the fates of two medicines, thalidomide and norphenylephrine, were studied and the safety evaluation of some xenobiotics including food additives, plasticizers and domestic chemical products, etc. was carried out in animals using synthesized 14C- or 3H-labeled compounds. In addition, the metabolism of n-propyl-N-nitrosourea, a carcinogen, in rats, and chemical modification of high molecular substances such as DNA, RNA and proteins by 1,1'-ethylene-bis(1-nitrosourea) (EBNU), a carcinostatic agent, were studied in vitro by the use of the tracer technique.

Animals↗
PubMedDate not supplied

High performance liquid chromatography coupled with radioactivity detection: a powerful tool for determining drug metabolite profiles in biological fluids.

High performance liquid chromatography coupled with continuous radioactivity detection represents an advancement in drug metabolism research. Using radioactive substances labelled in biologically stable positions, all metabolites can be specifically detected by radioactivity measurement. Thus no clean-up of biological fluids is required prior to HPLC. This can prevent artefact formation from unstable metabolites, reduces recovery problems and facilitates quantitation. Separation of highly polar and unpolar metabolites is possible in a single chromatographic run using gradient elution and reversed phase materials. This technique is also well-suited for preparative isolation and purification of metabolites for subsequent structure elucidation. Various metabolite profiles of drugs labelled with carbon-14 or tritium are shown. Metabolites of the following drugs are presented: norfenefrine, etozolin, thymoxamine, naloxone, and levobunolol. We review the general methodology and report our experience with this technique. In principle, this technique may be useful for all biological systems in which tracer techniques are applied.

2-Hydroxyphenethylamine↗
PubMedDate not supplied

Involvement of reactive oxygen species in the induction of (S)-N-p-coumaroyloctopamine accumulation by beta-1,3-glucooligosaccharide elicitors in potato tuber tissues.

Treatment of potato tuber tissues with beta-1,3-glucooligosaccharide induces accumulation of (S)-N-p-coumaroyloctopamine (p-CO). We examined the role of reactive oxygen species (ROS) and nitric oxide (NO) in the signal transduction leading to p-CO accumulation. Induction was suppressed by an NADPH-oxidase inhibitor, diphenyleneiodonium chloride, and oxygen radical scavengers. H2O2 was generated in the tuber tissue within a few minutes of treatment with beta-1,3-glucooligosaccharide. On the other hand, treatment with NO specific scavenger, nitric oxide synthase inhibitor, and serine protease inhibitor did not inhibit p-CO induction. Our findings suggest that ROS generated by the action of NADPH-oxidase play an important role in this system, while NO and serine protease are unlikely to be involved in this process.

1,2-Dihydroxybenzene-3,5-Disulfonic Acid Disodium ↗
PubMed2004

Properties of descending dorsal unpaired median (DUM) neurons of the locust suboesophageal ganglion.

A group of six dorsal unpaired median (DUM) neurons of the suboesophageal ganglion (SOG) of locusts was studied with neuroanatomical and electrophysiological techniques. The neurons are located posteriorly in the SOG and have axons that descend into the ganglia of the ventral nerve cord, some as far as the terminal abdominal ganglion. Within thoracic ganglia the neurons have profuse dendritic ramifications in many neuropiles, including ventral sensory neuropiles. Based on their projection patterns three different morphological types of neurons can be distinguished. These neurons receive excitatory inputs through sensory pathways that ascend from the thoracic ganglia and are activated by limb movements. They may be involved in the modulation of synaptic transmission in thoracic ganglia.

Animals↗
PubMed1986

Drug- and temperature-induced changes in peripheral circulation measured by laser-Doppler flowmetry and digital-pulse plethysmography.

We measured the effects of a new transdermal nitroglycerin patch (25 mg, 10 cm2) applied for 24 h, norphenephrine (6 mg), prazosin (1 mg) as well as local heat and cold provocation on blood pressure, heart rate, skin blood flow (measured by laser-Doppler flowmetry, L-D) and peripheral arterial resistance (assessed by digital pulse plethysmography, D-P) in 15 healthy volunteers (aged 21-31 years). Heat provocation induced a three-fold increase in skin blood flow in the hand (p less than 0.001) and cold provocation a decrease in flow (p less than 0.05) of about 20%. Forehead skin blood flow did not change. Peripheral arterial resistance showed less consistent changes during the provocation tests. Prazosin increased the forehead skin blood flow (p less than 0.01) and decreased peripheral arterial resistance, while norphenephrine showed an opposite effect. Transdermal nitroglycerin induced an increase of 25% in forehead skin blood flow (p less than 0.05) which persisted for 24 h and a decrease in peripheral arterial resistance (p less than 0.02), but this effect was evident up to 8 h only. We conclude that (1) local heat and cold provocation mainly affected skin blood flow, (2) vasodilative and vasoconstrictive drugs showed marked changes in peripheral arterial resistance, but at different points in time from subject to subject, and (3) transdermal nitroglycerin patches induced haemodynamic changes persisting for up to 8-24 h.

2-Hydroxyphenethylamine↗
PubMed1985

Defective responsiveness of adenylate cyclase to forskolin in the Drosophila memory mutant rutabaga.

The Drosophila memory mutant rutabaga (rut) has been previously shown to have a defective subpopulation (or functional state) of the enzyme adenylate cyclase. We report here that the reduced adenylate cyclase activity is also associated with a defective responsiveness of the enzyme to forskolin. Forskolin activation isotherms of the enzyme in normal membranes reveal low- and high-affinity forskolin-interacting components; the residual enzyme in the mutant shows a smaller proportion of the high-affinity response. In addition, in mutant membrane preparations, forskolin fails to shift the Km of the enzyme for free Mg2+ and for MgATP, in contrast to the situation in the normal tissue. The defect in the responsiveness to forskolin in rut is even more pronounced in a Lubrol-solubilized enzyme preparation, and is due to intrinsic properties of the cyclase system rather than to the absence (or presence) of a soluble, or detergent solubilized, factor in rut. The reduced forskolin responsiveness maps to the X chromosomal segment 12F5-6 to 13A1-5, within the region previously reported to span the locus that controls both the abortive memory and the lack of Ca2+-stimulation of adenylate cyclase in rut17. The possible relevance of the findings to postulated molecular mechanisms of short-term memory formation is discussed.

Adenylyl Cyclases↗