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At least 19 recordsLinked to original sources
PubMed1996

Characterization of the radioactive metabolites of the 5-HT1A receptor radioligand, [O-methyl-11C]WAY-100635, in monkey and human plasma by HPLC: comparison of the behaviour of an identified radioactive metabolite with parent radioligand in monkey using PET.

N-(2-(4-(2-Methoxy-phenyl)-1-piperazin-1-yl)ethyl)-N-(2-pyridyl) cyclohexanecarboxamide (WAY-100635), labelled in the O-methyl group with carbon-11 (t1/2 = 20.4 min), is a promising radioligand for application with positron emission tomography (PET) to the study of 5-HT1A receptors in living human brain. An understanding of the metabolism of this new radioligand is crucial to the development of a biomathematical model for the interpretation of the kinetics of radioactivity uptake in brain in terms of receptor-binding parameters. After intravenous injection of [O-methyl-11C]WAY-100635 into humans, radioactivity was found to clear rapidly from blood and plasma. By using established methods for the analysis of radioactivity in plasma, it was found that intravenously injected [O-methyl-11C]WAY-100635 is rapidly metabolised to more polar radioactive compounds in a cynomolgus monkey and in humans. Thus, at 60 min postinjection, parent radioligand represented 40% and 5% of the radioactivity in monkey and human plasma, respectively. In monkey and human, one of the radioactive metabolites was identified as the descyclohexanecarbonyl analogue of the parent radioligand, namely [O-methyl-11C]WAY-100634. This compound is known to have high affinity for 5-HT1A receptors and alpha 1-adrenoceptors. In a PET experiment it was demonstrated that, after IV injection of [O-methyl-11C]WAY-100634 into a cynomolgus monkey, radioactivity was avidly taken up by brain. Uptake of radioactivity was higher in 5-HT1A receptor-rich frontal cortex than in cerebellum, which is devoid of 5-HT1A receptors. Polar radioactive metabolites appeared in plasma. The results suggest that the use of WAY-100635 labelled with carbon-11 in its cyclohexanecarbonyl moiety may provide enhanced signal contrast in PET studies and a possibility to develop a simple biomathematical model for regional brain radioactivity uptake.

Animals↗
PubMed2000

Comparisons between radioactive and non-radioactive gas lantern mantles.

Gas lantern mantles containing radioactive thorium have been used for more than 100 years. Although thorium was once believed to be indispensable for giving a bright light, non-radioactive mantles are now available. From the radioactivities of the daughter nuclides, we estimated the levels of radioactivity of 232Th and 228Th in 11 mantles. The mantles contained various levels of radioactivity from background levels to 1410 +/- 140 Bq. Our finding that radioactive and non-radioactive mantles are equally bright suggests that there is no advantage in using radioactive mantles. A remaining problem is that gas lantern mantles are sold without any information about radioactivity.

Camping↗
PubMed1994

Using a radioactive and non-radioactive exchangeable labeling system for laboratory diagnosis.

In this communication a safe and simple molecular diagnosis strategy was described, which can be applied for the identification of pathogens or oncogenes in clinical studies. In Southern or Northern analysis, we demonstrated the feasibility to exchange labeling probes from non-radioactive to radioactive or vice versa in a single membrane simply by stripping. We chose non-radioactive labeling because it is safe and easy to operate, but when the sensitivity is insufficient, it can be replaced by radioactive labeling. Our data show that radioactive or non-radioactive labeling is exchangeable in a single membrane and the sensitivity was comparable by either method under optimal conditions. The clinical implication is that for general hybridization starts with non-radioactive labeling, radioactive labeling is not needed unless the signals cannot be detected by non-radioactive labeling. Moreover, one membrane can be labeled repeatedly by different probes.

Blotting, Northern↗
PubMed1976

[Distribution of radioactivity in the body and rate of incorporation of radioactivity into the tissue proteins of monogastric animals following intravenous injection of tracer amino acids].

The studies were carried out with pigs and rats. The radioactive animo acids (14C leucine and 3H lysine) were administered to the pigs by way of a catheter tube into the jugular vein. Subsequently, the time pattern of the distribution of the specific amino acid radioactivity was followed in the TCE soluble and Tce precipitable fractions of the blood plasma (TCE= trichloro-acetic acid). The radioactive labelling in rats was carried out by injecting 14C leucine into the portal vein. The animals were killed after incorporation periods from 2 to 60 mins, and the levels of specific radioactivity were estimated in the TCE soluble and TCE precipitable fractions of the blood plasma, in the liver and in the skeletal muscles. The experimental results clearly indicated that the specific radioactivity of the tracer amino acids and the rate of incorporation of radioactivity into tissue proteins were greatly influenced by the size of the free amino acid pool within the range of distribution of the tracer. An estimation of the magnitude of the pool of free amino acids within the distribution range of the tracer can be obtained from the curve pattern for the decline of specific radioactivity of the corresponding free amino acid in the blood plasma. This pool exhibits a high rate of turnover. In all studies made to evaluate in vivo processes of protein synthesis by use of radioactive tracer amino acids it will be particularly important that consideration should be given to the specific radioactivity of the amino acid in the precursor pool for protein synthesis.

Amino Acids↗
PubMed2001

"Edge Effect" of (32)p radioactive stents is caused by the combination of chronic stent injury and radioactive dose falloff.

BACKGROUND: Radioactive stents have been reported to reduce in-stent neointimal thickening. An unexpected increase in neointimal response was observed, however, at the stent-to-artery transitions, the so-called "edge effect." To investigate the factors involved in this edge effect, we studied stents with 1 radioactive half and 1 regular nonradioactive half, thereby creating a midstent radioactive dose-falloff zone next to a nonradioactive stent-artery transition at one side and a radioactive stent-artery transition at the other side. METHODS AND RESULTS: Half-radioactive stents (n=20) and nonradioactive control stents (n=10) were implanted in the coronary arteries of Yucatan micropigs. Animals received aspirin and clopidogrel as antithrombotics. After 4 weeks, a significant midstent stenosis was observed by angiography in the half-radioactive stents. Two animals died suddenly because of coronary occlusion at this mid zone at 8 and 10 weeks. At 12-week follow-up angiography, intravascular ultrasound and histomorphometry showed a significant neointimal thickening at the midstent dose-falloff zone of the half-radioactive stents, but not at the stent-to-artery transitions at both extremities. Such a midstent response (mean angiographic late loss 1.0 mm) was not observed in the nonradioactive stents (mean loss 0.4 to 0.6 mm; P< 0.01). CONCLUSIONS: The edge effect of high-dose radioactive stents in porcine coronary arteries is associated with the combination of stent injury and radioactive dose falloff.

Animals↗
PubMed1975

[Resorption and incorporation of radioactive-labeled amino acids during the administration of various protein carriers in rats. 2. Uptake of radioactivity by tissues of the gastrointestinal tract after intragastric administration of 14C-L-U-leucine and 3H-glycine].

Male Albino rats (weighing 90-100 gms) were fed ad libitum for 14 days with limited periods of access to food. Powdered whole egg (V), fish meal (F), yeats (H), and gelatine (10% protein in dry matter) used as protein sources. Additionally, one group of rats received a protein-free (e). Radioactive tracers were administered by intragastric infusion of 25 mu Ci 3H glycine and 5 mu Ci 14C L-leucine per 100 gm of body weight 2 hrs after the feeding of 2 gm of the experimental diet per 100 gms of body weight. The level of uptake of radioactive tracers from the different sections of the gastro-intestinal tract was measurels of 3H and 14C labelling in intestinal tissues were observed 3 hrs and 7 hrs after infusion. The level of 14C labelling was found to be negatively correlated and the level of 3H labelling was positively correlated with the biological value of the diet. Intestinal tissues are capable of storing considerable amounts of 14C radioactivity. So, 72 hrs after infusion, the following levels of 14C radioactivity (expressed as percentage of the total dose of radioactivity) were found in tissues of the gastro-intestinal tract: whole egg: 8.4%, fish meal: 9.6%, yeast: 13.1%, gelatine: 14.9%; protein-free diet; 14.2%. The quotients correlating the levels of radioactivity from the intestinal contents with that found in the intestinal wall suggest that the walls of the small intestine possess a high capacity for absorption. At all times of radioactive measurements the walls of the small intestine were found to contain higher levels of both 14C and 3H radioactivity than the contents of small intestine.

Animal Nutritional Physiological Phenomena↗
PubMed2003

[Design of radiolabeled antibody fragments for tumor-selective radioactivity localization--brush border enzyme-sensitive bond to decrease renal accumulation of radioactivity].

Nonspecific renal radioactivity localization constitutes a problem in targeted imaging and therapy with radiolabeled antibody fragments. Based on the idea that the renal radioactivity levels should be reduced if radiolabeled compounds excreted in the urine are released from antibody fragments by tubular brush border enzymes, 3'-iodohippuryl N epsilon-maleoyl-L-lysine (HML) was designed as a radioiodination reagent for antibody fragments; the glycyl-lysine sequence in HML is a substrate for a brush border enzyme and m-iodohippuric acid is released by cleavage of the linkage. In normal mice, HML-conjugated Fab demonstrated low renal radioactivity levels from early postinjection times. Directly radioiodinated Fab showed migration of radioactivity from the membrane to the lysosomal fraction of the renal cells from 10 to 30 min postinjection. On the other hand, the majority of the radioactivity was detected only in the membrane fraction after injection of HML-conjugated Fab. In tumor-bearing mice, HML-conjugated Fab showed a marked decrease in renal radioactivity localization without impairing the tumor accumulation. These findings indicate that HML is a useful reagent for reducing the renal radioactivity levels of antibody fragments.

Animals↗
PubMed2006

[Evil radioactivity. Subjective perception of radioactivity in patients with thyroid disease prior to treatment with radioiodine].

AIM: We assess the perspective of patients with thyroid disease towards radiation and radioactivity by means of a cultural-anthropological approach based on qualitative measures and quantitative scores. From the interviews with the patients we evaluate as to how much radioactivity is accepted as an abstract term or as a benefit within the medical context. PATIENTS, METHODS: 68 patients with autonomously functioning thyroid lesions (35 women, 33 men, 32-81 years) were included in this study. All patients were interviewed in an open dialogue with the principal investigator. Patients were asked to describe their attitude towards radioactivity in general and towards radioiodine therapy in particular. Patients were asked to use a scoring system (1 = positive, 5 = negative) to quantify their attitudes. RESULTS: The responses of all patients towards radioactivity in general were heterogeneous with most responses reflecting a negative perception. Many patients expressed their associated fears about atomic energy, malignant diseases and radioactive contamination. The scoring system reflected a mostly negative opinion base. However, patients became more positive once they assumed an immediate benefit of radioactivity for the treatment of their own disease (p = 0.01). CONCLUSIONS: Knowing about significant differences in patient's perception about radioactivity in general or in the clinical context may help to optimise and tailor the initial, pre-therapeutical interview towards the patient.

Adult↗
PubMed1996

Labeling of insulin with non-radioactive 127I and application to incorporation of radioactive 125I for use in receptor-binding experiments by high-performance liquid chromatography.

Conditions for the labeling of insulin with radioactive iodine isotopes were investigated by means of incorporation of non-radioactive 127I into the peptide. Either the chloramine-T (CT) or lactoperoxidase-hydrogen peroxide (LPO) technique was applied and reversed-phase high-performance liquid chromatography (RP-HPLC) was used for analysis of the reaction products. The LPO method provided the 127I-labeled peptide within 15-30 min, whereas the CT alternative yielded the labeled substrate even within 15 s. However, the latter reaction can only be controlled in a reproducible manner with difficulty and undesired side-reactions became increasingly prominent when the reaction time of 15 s was exceeded for only a few seconds. In another experiment, the LPO technique was applied for radiolabeling insulin with 125I. The product was first purified by size-exclusion chromatography (SEC) and then subjected to RP-HPLC. SEC yielded two peaks. The smaller one, which eluted at a slightly higher Kd value (accounting for about 14% of total radioactivity) predominantly consisted of material eluting at the column's void volume under the conditions of RP-HPLC, whereas the main SEC fraction (accounting for about 86% of total radioactivity) yielded a single peak, as shown by HPLC. The radioactive material attributable to the main SEC fraction revealed the expected receptor-binding properties, as evidenced by displacement experiments with non-radioactive insulin, as well as the action of tetradecanoyl phorbol acetate on the binding characteristics and thus indicating formation of a labeled hormone retaining biological activity.

Binding, Competitive↗
PubMed1993

Localization of calretinin mRNA in rat and guinea pig inner ear by in situ hybridization using radioactive and non-radioactive probes.

The localization of calretinin mRNA was studied in the rat and guinea pig inner ear by in situ hybridization, and compared to the distribution of the protein previously examined by immunocytochemistry. Radioactive and non-radioactive in situ hybridization (ISH) were performed using oligonucleotide probes labelled with 35S or digoxigenin. Radioactive ISH was more sensitive than non-radioactive ISH. In cochlear and vestibular ganglia, calretinin mRNA was localized in subpopulations of neurons with patterns of distribution similar to those shown by immunocytochemistry. By contrast, the observations in the sensory epithelia differed with the two techniques, ISH revealing less positive structures than immunocytochemistry. Rat inner hair cells and guinea pig inner hair cells, Hensen's cells and Deiters cells, which had been described strongly immunoreactive, appeared positive with radioactive but not with non-radioactive ISH. On the other hand, rat vestibular type II hair cells and guinea pig interdental cells of the spiral limbus which were faintly immunoreactive were not positive with both ISH techniques.

Animals↗
PubMed2004

Radioactive waste disposal implications of extending Part IIA of the Environmental Protection Act to cover radioactively contaminated land.

A short study has been carried out of the potential radioactive waste disposal issues associated with the proposed extension of Part IIA of the Environmental Protection Act 1990 to include radioactively contaminated land, where there is no other suitable existing legislation. It was found that there is likely to be an availability problem with respect to disposal at landfills of the radioactive wastes arising from remediation. This is expected to be principally wastes of high volume and low activity (categorised as low level waste (LLW) and very low level waste (VLLW)). The availability problem results from a lack of applications by landfill operators for authorisation to accept LLW wastes for disposal. This is apparently due to perceived adverse publicity associated with the consultation process for authorisation coupled with uncertainty over future liabilities. Disposal of waste as VLLW is limited both by questions over volumes that may be acceptable and, more fundamentally, by the likely alpha activity of wastes (originating from radium and thorium operations). Authorised on-site disposal has had little attention in policy and guidance in recent years, but may have a part to play, especially if considered commercially attractive. Disposal at BNFL's near surface disposal facility for LLW at Drigg is limited to wastes for which there are no practical alternative disposal options (and preference has been given to operational type wastes). Therefore, wastes from the radioactively contaminated land (RCL) regime are not obviously attractive for disposal to Drigg. Illustrative calculations have been performed based on possible volumes and activities of RCL arisings (and assuming Drigg's future volumetric disposal capacity is 950,000 m3). These suggest that wastes arising from implementing the RCL regime, if all disposed to Drigg, would not represent a significant fraction of the volumetric capacity of Drigg, but could have a significant impact on the radiological capacity with respect to 226Ra plus 232Th. The government's decision-making programme for managing solid radioactive wastes in the UK may possibly achieve a general consensus that the use of landfill for LLW from the RCL regime has a fundamental role to play. However, this is unlikely to change the situation within the next few years. No new national facility arising from this programme is likely to be available during the first decade of the operation of a new RCL regime. Hence it appears that Drigg will need to play an important role for some years to come.

Humans↗
PubMed2004

[Investigation of radioactivity measurement of medical radioactive waste].

To explore the possibility of which medical radioactive wastes could be disposed as general wastes after keeping them a certain period of time and confirming that their radioactivity reach a background level (BGL), we made a survey of these wastes in several nuclear medicine facilities. The radioactive wastes were collected for one week, packed in a box according to its half-life, and measured its radioactivity by scintillation survey meter with time. Some wastes could reach a BGL within 10 times of half-life, but 19% of the short half-life group (group 1) including 99mTc and 123I, and 8% of the middle half-life group (group 2) including 67Ga, (111)In, and 201Tl did not reach a BGL within 20 times of half-life. A reason for delaying the time of reaching a BGL might be partially attributed to high initial radiation dose rate or heavy package weight. However, mixing with the nuclides of longer half-life was estimated to be the biggest factor affecting this result. When disposing medical radioactive wastes as general wastes, it is necessary to avoid mixing with radionuclide of longer half-life and confirm that it reaches a BGL by actual measurement.

Half-Life↗