ABSTRACT
Tin-117m-labeled 23-(trimethylstannyl)-24-nor-5 alpha-cholan-3 beta-ol (2) has been prepared by reaction of trimethyl [117mSn]tin lithium with 3 beta-acetoxy-23-bromo-24-nor-5 alpha-cholane (1). Tin-117m (2) shows pronounced adrenal uptake (2.5% injected dose) in female rats 1 day after injection. Furthermore, the adrenal to liver (9.1:1) and adrenal to blood (33.7:1) ratios are high after this period. The absorbed radiation dose values from [117mSn]2 to human organs have also been estimated by using rat tissue distribution and excretion data. [117mSn]2 is the first reported tissue-specific organic radiopharmaceutical labeled with this nuclide and may have potential as an adrenal imaging agent.
Subject(s)
Cholanes/chemical synthesis , Radionuclide Imaging/methods , Trialkyltin Compounds/chemical synthesis , Trimethyltin Compounds/chemical synthesis , Adrenal Glands/metabolism , Animals , Cholanes/metabolism , Female , Indicators and Reagents , Kidney/metabolism , Kinetics , Liver/metabolism , Male , Mass Spectrometry , Ovary/metabolism , Radioisotopes , Rats , Spectrophotometry, Infrared , Tissue Distribution , Trimethyltin Compounds/metabolismABSTRACT
Selenium-75-labeled 24-(isopropylseleno)chol-5-en-3 beta-ol (4) has been prepared by reaction of sodium isopropyl-[75Se]selenol [( 75Se]2) with 3 beta-acetoxy-24-bromochol-5-ene (3). This new 75Se-labeled adrenal imaging agent shows pronounced adrenal uptake in rats. The concentration of radioactivity in rat adrenals increased steadily from 1 to 24 h after injection and then decreased slowly over the 21-day period. After 3 days the adrenal/blood and adrenal/liver ratios were 85:1 and 32:1, respectively, which are sufficient for adrenal imaging by single photon techniques. After 6 h the adrenal/blood ratio was 17:1 and the adrenal/liver ratio was 7:1. We propose that these ratios are sufficiently high for positron emission tomography of the adrenals. The absorbed radiation dose values to human organs have been estimated for the 75Se- and 73Se-labeled agent.
Subject(s)
Cholenes/chemical synthesis , Organoselenium Compounds , Radionuclide Imaging/methods , Selenium , Selenium/chemical synthesis , Adrenal Glands/metabolism , Animals , Cholenes/metabolism , Female , Indicators and Reagents , Kidney/metabolism , Kinetics , Liver/metabolism , Mass Spectrometry , Ovary/metabolism , Radioisotopes , Rats , Selenium/metabolism , Spectrophotometry, Infrared , Tissue DistributionABSTRACT
A polystyrene resin, suitable for semi-solid gastric emptying studies, was rapidly (less than 20 min) and conveniently prepared using commercially available reagents. Using the outlined procedure, Chelex-100 resin bound Tc-99m with greater than 98% labeling efficiency. The resulting Tc-99m Chelex-100 resin demonstrated excellent in vitro and in vivo stability. The clinical application of Tc-99m Chelex-100 resin, mixed with oatmeal, was tested in normal subjects and in various patient groups, including diabetic autonomic neuropathy, pyloric obstruction, postoperative dumping syndrome, and morbidly obese patients before and after gastroplasty.
Subject(s)
Chelating Agents , Gastric Emptying , Technetium , Administration, Oral , Humans , Resins, Synthetic , Sodium Pertechnetate Tc 99m , Technology, PharmaceuticalABSTRACT
Survival of Staphylococcus epidermidis (10(2) organisms/ml) in solutions containing various levels of radioactivity was assessed. Six test preparations contained nonbacteriostatic 0.9% sodium chloride solution; four of these contained technetium Tc 99m pertechnetate (99mTcO-4) in various quantities (80, 250, 500, and 750 mCi). A fifth contained technetium that had decayed to an essentially nonradioactive form, and a sixth contained 0.9% sodium chloride solution only. Each of the six 20-ml solutions was inoculated with 2 ml of single-strength trypticase soy broth (TSB) containing 10(3) organisms/ml. At various times up to 12 hours after inoculation, 1-ml aliquots of each test solution were withdrawn and passed through 0.22-micron filters, thereby preventing further irradiation of the filtered organisms. The filters were incubated in single-strength TSB at 37 degrees C, and samples were examined for turbidity at 24, 48, and 72 hours. After 24 hours, 25 of the 36 sample tubes showed turbidity; after 48 hours, the turbid samples totaled 28. Bacteria in the two nonradioactive solutions remained viable throughout the 12-hour sampling period. Accumulated doses of radiation obtained in the 250-, 500-, and 750-mCi samples inhibited bacterial growth. To be a valid quality-control measure, sterility monitoring of prepared radiopharmaceutical dosage forms may need to be performed concurrently with their preparation.
Subject(s)
Bacteria/radiation effects , Technetium , Drug Contamination , Nephelometry and Turbidimetry , Sodium Pertechnetate Tc 99m , Staphylococcus/growth & development , Staphylococcus/radiation effects , Time FactorsABSTRACT
The distribution of radioactivity in the myocardium of rats and dogs infarcted by ligation of the left anterior coronary artery has been determined after intravenous injection of 9-[Te-123m]telluraheptadecanoic acid (Te-123m HDA]. In rats the normal myocardium concentrated radioactivity (3.7% +/- 0.28 injected dose/g) to nearly three times that in the zones of infarction (1.12% +/- 0.18 dose/g0. The focal defects detected in the gamma-camera images of rats and dogs correspond well with areas of infarction identified in the excised hearts by staining with triphenyltetrazolium chloride. The distribution of radioactivity from Te- 123m HDA in dog hearts sectioned at autopsy showed a linear correlation (r = 0.94) with blood flow as determined with scandium-46-labeled microspheres.
Subject(s)
Fatty Acids , Heart/diagnostic imaging , Tellurium , Animals , Coronary Circulation , Dogs , Female , Male , Mice , Myocardium/metabolism , Radionuclide Imaging , Rats , Rats, Inbred Strains , Tissue DistributionABSTRACT
The absorbed radiation doses to humans from 23-(isopropyl[123mTe]telluro)-24-nor-5 alpha-cholan-3 beta-ol (Te-123m-23-ITC) and 24-(isopropyl[123mTe]telluro)-chol-5-en-3 beta-ol(Te-123m-24-ITC) have been calculated, based on rat biological data, to assess the relative radiation risks to humans from these two new adrenal-imaging agents. The estimated radiation doses to several critical organs have been compared with dose estimates for a variety of other radiolabeled steroids that have been designed as adrenal-imaging agents. Dose estimates to selected organs from Te-123m-23-ITC are as follows (rad/mCi): adrenals 98; ovaries 8.0; liver 1.6. Similar estimated values for Te-123m-24-ITC are: adrenals 210; ovaries 13; liver 2.0. The radiation dose estimates for these two agents are comparable to the calculated radiation doses from 6 beta-[(methyl[75Se]seleno)methyl]-19-nor-cholest-5(10)-en-3 beta-ol (Scintidren) and 19-[131I]iodocholest-5-en-3 beta-ol (NP-59), two agents currently in clinical use for the diagnosis of adrenal disease.
Subject(s)
Adrenal Glands/diagnostic imaging , Cholanes , Cholenes , Radioisotopes , Tellurium , Animals , Cholanes/metabolism , Cholenes/metabolism , Female , Radiation Dosage , Radionuclide Imaging , Rats , Tellurium/metabolismABSTRACT
Two methods for calculating the radiation dose from remaining body activity have been suggested. One requires correction of the cumulated activities so that they reflect the activity uniformly distributed in the total body. The other method requires correction of the S values so that a value of S for the target organ from the remainder of the body is obtained. These two methods give the same answer. We have examined these methods and the number of steps required to calculate the radiation dose in each case. Our results show that the method of correcting the cumulated activities is preferred, especially if the number of source and target organs is large and a computer equipped with the necessary software is not available.
