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PubMed1999

In vitro studies on the cellular uptake of melanoma imaging aminoalkyl-iodobenzamide derivatives (ABA).

The cellular uptake of 11 radioiodinated aminoalkyl-iodobenzamides (ABA) was studied using cultivated murine melanoma cells (B16/C3). All derivatives showed a high uptake (up to about 80%) of radioactivity in melanotic melanoma cells; hence, accumulation of all compounds radioiodinated in the ortho position was reduced by approximately 30%. Using the compound para-[131I]iododiethyl-aminoethylbenzamide (p-131I-ABA-2-2) a close correlation of the cellular melanin content with the tracer uptake (R2 = 0.95) was verified. The presence of extracellular melanin, however, had no effect on the cellular tracer uptake. Because the accumulation was independent of the specific activity of p-131I-ABA-2-2, a significant contribution to the uptake process by binding to receptor sites could be excluded.

Benzamides↗

PubMed1992

[Metabolite of 15-p-iodophenyl-3(R,S)-pentadecanoic acid (123I) in blood and urine].

We analyzed metabolites of 123I-BMIPP in blood and urine using rats, rabbits and human, while human samples were obtained from normal volunteers of Phase I clinical study. We estimated metabolic pathway of 123I-BMIPP as a myocardial metabolic imaging agent. Radioactivity accumulated in heart after administration gradually decreased and was mainly excreted to bladder via kidneys. The main radioactive component in blood was 123I-PIPA for any species and the urinary components were metabolic conjugates of 123I-PIPA. As results of these studies, we considered that 123I-BMIPP was metabolized to 123I-PIPA by alpha-oxidation process for the first step, follow by beta-oxidation process, then 123I-PIPA was released to blood from tissues. Moreover, 123I-PIPA in blood was conjugated with other compounds and excreted to the bladder.

Animals↗

PubMed1999

Evaluation of a scheme for the pre-distribution of stable iodine (potassium iodate) to the civilian population residing within the immediate countermeasures zone of a nuclear submarine construction facility.

BACKGROUND: The Barrow-in-Furness stable iodine (potassium iodate) tablet pre-distribution scheme was the first of its kind to be introduced to protect the population living around a fixed site nuclear facility in the United Kingdom. Pre-distribution schemes have attracted critical comment principally because the certainty of availability of potassium iodate tablets was unknown. This study aimed to establish the reliability of such a scheme. METHOD: A structured interviewer-administered survey of a random sample of households served by the pre-distribution scheme was carried out using a standardized questionnaire. RESULTS: The ability of this scheme to provide stable iodine protection declined from 100 per cent to 60 per cent coverage over a period of two years for the designed worst-case demand (the ability to supply stable iodine tablets to all household residents normally living within the pre-distribution scheme zone). CONCLUSIONS: Pre-distribution has value in areas where evacuation to a centre where stable iodine tablets are available or post-accident distribution to sheltering households is difficult. The value of such a scheme must be calculated against a predictable decline in its effectiveness. In implementing such a scheme it should be noted that this decline in coverage can be reduced by calculating the frequency with which tablet packs are redistributed to take account of this factor.

Disaster Planning↗

PubMed1994

The use of competitive displacement agents to resolve albumin binding problems observed during the development of a radioimmunoassay for ICI 215001.

A radioimmunoassay has been developed for the analysis of ICI 215001, a carboxylic acid metabolite of ICI D7114. The level of binding and sensitivity of the assay were good in the absence of plasma. However, the addition of plasma to the incubation medium reduced the antibody binding of radiolabelled tracer (I) from 41 to 9%. This was attributed to the high (> 99%) plasma albumin binding of ICI 215001. A series of compounds (DL-tryptophan, octanoic acid, bilirubin, ponalrestat, warfarin, phenylbutazone and salicylic acid) which all bind to plasma albumin, were examined for their effect on the tracer-antibody interaction. Warfarin and phenylbutazone were the only compounds to specifically displace the iodinated tracer from albumin; warfarin was the only compound to restore antibody binding to control levels. The warfarin concentration and the pH of the incubation medium also had a substantial effect on the magnitude of the displacement. The optimized method for the analysis of ICI 215001 in human plasma (20 microliters) used phosphate buffer (pH 6.0, 0.1 M) containing warfarin (50 micrograms ml-1), which gave an assay with the desired specificity, precision and sensitivity.

Adrenergic beta-Agonists↗

PubMed1994

Maleimidoethyl 3-(tri-n-butylstannyl)hippurate: a useful radioiodination reagent for protein radiopharmaceuticals to enhance target selective radioactivity localization.

In pursuit of radiolabeled monoclonal antibodies (mAbs) with rapid urinary excretion of radioactivity from nontarget tissues, radioiodinated mAbs releasing a m-iodohippuric acid from the mAbs in nontarget tissues were designed. A novel reagent, maleimidoethyl 3-(tri-n-butylstannyl)hippurate (MIH), was synthesized by reacting N-(hydroxyethyl)maleimide with N-Boc-glycine before coupling with N-succinimidyl 3-(tri-n-butylstannyl)benzoate (ATE). MIH possessed a maleimide group for mAb conjugation and a butylstannyl moiety for high-yield and site-specific radioiodination, and the two functional groups were linked via an ester bond to release m-iodohippuric acid. To investigate the fate of radiolabels after lysosomal proteolysis, hepatic parenchymal cells were used as a model nontarget tissue and 131I-labeled MIH was conjugated with galactosyl-neoglycoalbumin (NGA). Further conjugation of [131I]MIH with a mAb against osteogenic sarcoma (OST7) after reduction of its disulfide bonds was followed up. In murine biodistribution studies, [131I]MIH-NGA exhibited rapid accumulation in the liver followed by radioactivity elimination from the liver at a rate that was identical to and faster than those of 131I-labeled NGA via direct iodination ([131I]NGA) and [131I]ATE-labeled NGA, respectively. While [131I]NGA indicated high radioactivity levels in the murine neck, stomach, and blood, such increases in the radioactivity count were not detectable by the administration of either [131I]MIH-NGA or [131I]ATE-NGA. At 6 h postinjection of [131I]MIH-NGA, 80% of the injected radioactivity was recovered in the urine. Analyses of urine samples indicated that m-iodohippuric acid was the sole radiolabeled metabolite. In biodistribution studies using [131I]-MIH-OST7 and [131I]ATE-OST7, while both 131I-labeled OST7s registered almost identical radioactivity levels in the blood up to 6 h postinjection, the former demonstrated a lower radioactivity level than [131I]ATE-OST7 in nontarget tissues throughout the experiment. Such chemical and biological characteristics of MIH would enable high target/nontarget ratios in diagnostic and therapeutic nuclear medicine using mAbs and other polypeptides.

Albumins↗

PubMed1995

Lipophilic metabolite of [123I]beta-CIT in human plasma may obstruct quantitation of the dopamine transporter.

I-123 or C-11 labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane (beta-CIT) is a recently developed radioligand for the study of dopamine and serotonin reuptake sites in humans with single photon emission tomography (SPET) or positron emission tomography (PET). Determination of the radioligand metabolite pattern is fundamental for a quantitative analysis of radioligand binding. The metabolism of [123I]beta-CIT was determined by a gradient HPLC method in plasma samples of six human subjects. Two metabolites of [123I]beta-CIT were found, a polar and a lipophilic. At 4 h after [123I]beta-CIT injection the percentages of parent compound and polar and lipophilic metabolites were 23 +/- 3% (mean +/- SD), 33 +/- 11%, and 44 +/- 8%, respectively. The lipophilic metabolite might pass the blood-brain barrier and account for a fraction of free and nonspecifically bound radioactivity in brain. The existence of a lipophilic metabolite of [123I]beta-CIT may obstruct the use of simple ratio methods for quantitation of the dopamine transporter in brain.

Adult↗

PubMed2004

Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.

2beta-Carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]tropane (ZIET) and 2beta-carbomethoxy-3beta-[4'-((Z)-2-bromoethenyl)phenyl]tropane (ZBrET) were synthesized as well as their nortropane congeners ZIENT and ZBrENT. Binding affinities of these compounds were determined in cells transfected to express human SERT, DAT, and NET using [3H]citalopram, [125I]RTI-55, and [3H]nisoxetine, respectively. Both ZIET and ZBrET displayed high affinity for the SERT (Ki = 0.11 and 0.08 nM, respectively). The affinities of ZIET and ZBrET for the DAT were 200 and 38-fold lower, respectively, than for the SERT. [11C]ZIET and [11C]ZBrET were prepared by alkylation of their corresponding nortropanes with [11C]methyl iodide in approximately 30% radiochemical yield (decay-corrected to end of bombardment, EOB). High specific activity [123I]ZIET was synthesized in 33% radiochemical yield (decay-corrected) by treating the 2beta-carbomethoxy-3beta-[4'-((Z)-2-trimethylstannylethenyl)phenyl]tropane (3) with no carrier-added sodium [123I]iodide and hydrogen peroxide in ethanolic HCl. Biodistribution studies in rats indicated that [123I]ZIET enters the brain readily and accumulates in SERT-rich regions. Blocking studies performed in rats demonstrated that [123I]ZIET was selective and specific for SERT-rich regions (e.g. thalamus, brainstem, and striatum). MicroPET brain imaging studies in monkeys demonstrated that [11C]ZIET and [11C]ZBrET uptakes were selectivity localized in the putamen, midbrain, caudate, thalamus, pons, and medulla. Radioactivity in the regions of high SERT density of monkey brain was displaceable with citalopram except in the putamen and caudate. Radioactivity uptake in these DAT-rich regions was significantly displaceable either by preadministration of citalopram followed by injection of RTI-113 (or vice-versa) or by administration of a mixture of DAT and SERT ligands. In conclusion, the high yield, high specific activity, one-step radiolabeling method, high selectivity and favorable kinetics, and the good results obtained with [123I]ZIET in rats support the candidacy of [11C]ZIET for in vivo visualization and quantification of brain SERT.

Animals↗

PubMed1981

Human serum albumin labelled with 99Tcm and 131I for total blood volume determination: A critical and comparative analysis in vivo and in vitro.

The increased plasma volume or total blood volume determined with radioactive tracers often have no physical or pathologic explanation. The plasma volume and blood dilution were simultaneously measured in 5 patients who had received human serum albumin labelled with 99Tcm or 131I. In each case and for each tracer, a biexponential dilution curve was obtained. The measured plasma volume was consistently higher after 99Tcm-labelled albumin. The results are correlated with the presence of non-protein artifacts arising from the labelling process and proteinaceous compounds arising from denaturation.

Blood Volume Determination↗

PubMed1979

Reincorporation of iodinated peptides in vivo and the comparative effectiveness of tungstic and trichloroacetic acids in peptide separation.

The absorption of 125I-bovine IgG after oral administration to young rats has been followed by gel filtration and quantitatively by TCA precipitation. The wide spectrum of protein derivatives crossing the gut wall have been utilised to compare the relative effectiveness of 10% TCA, and 1% tungstic acid, as reagents for the quantitative assessment of radioactive proteins and peptides. Radioactive iodide was the chief radioactive metabolite when 125I-labelled bovine IgG was fed to young rats, there was no significant incorporation of small radioactive metabolites into protein during a second exposure to the gut wall.

Acids↗

PubMed2006

High-activity radio-iodine labeling of conventional and stealth liposomes.

A new method to label preformed liposomes with high activities of radiohalogenated compounds has been developed. It uses activated esters of simple synthetic molecules that may be readily halogenated, such as Bolton-Hunter reagent (BH), and arginine-containing liposomes. BH, in the form of an activated ester, crosses the liposome membrane to react with arginine inside the liposomes, as demonstrated by thin-layer chromatography and by the fact that saline-containing liposomes, or hydrolyzed BH or the water soluble sulfo-BH afforded only marginal encapsulation yields. Under optimized conditions, between 37 and 55 degrees C, 62 +/- 4% (mean +/- SD) of radiolabeled BH were consistently encapsulated in the liposomes within 30 min. In molar amounts, this corresponds to a mean of 56 nmol of BH per micromol of lipids. Based on achievable specific activity, up to 2.8 GBq of iodine-131 could be entrapped per micromol of lipids. Leakage of radioactivity was very low, with less than 5% of the encapsulated activity released within 6 days at 4 degrees C in phosphate-buffered saline and less than 50% within 24 h in human serum at 37 degrees C. The labeling stability, and the fact that both conventional and PEGylated liposomes can be readily labeled with high doses of radioactivity, will make this technique useful for in vivo targeting applications, such as tumor detection (using iodine-123 or iodine-124) or therapy (with iodine-131 or astatine-211).

Chromatography, Thin Layer↗

PubMedDate not supplied

The metabolism and kinetics of 125I-labeled human intravenous IgG preparation (C-425) in rats and rabbits. I. Blood clearance, excretion into urine and feces, and brain uptake.

The metabolism of intravenous human IgG preparation (C-425) was studied by the use of 125I-C-425 in rats and rabbits after intravenous injection of the compound particularly with regard to changes in the levels of radioactive compound or metabolites in the blood as a function of time as well as levels excreted in urine and feces. Brain uptake index of 125I-C-425 was estimated by a slightly modified Oldendorf's method. 125I-Polyglobin was used as the control compound. The half-life of blood clearance of 125I-C-425 radioactivity after the 2nd day was about 8 days in rats and about 5 days in rabbits, respectively. Within a relatively short period of 1 hour, a rapid decrease of blood concentration of radioactivity was recorded. This was due to the transfer of labelled compound from blood into the extravascular compartment. A high concentration of radioactivity in the blood was maintained for one week after intravenous injection of the labelled compound in both rats and in rabbits. Most of the radioactive compound or metabolites were excreted in the urine and relatively little in feces. Excretion in urine of rats reached about 22% for 125I-C-425 and about 17% for 125I-Polyglobin. The excretion rate slowed down over 24 hours. The total recovery rates in rats were about 40% for 125I-C-425 and 125I-Polyglobin and about 55% in rabbits for both drugs. The permeability through the blood-brain barrier was found to be negligible for both drugs.

Animals↗

PubMedDate not supplied

Bis(hydroxamamide)-based bifunctional chelating agent for 99mTc labeling of polypeptides.

To develop chelating molecules that provide 99mTc-labeled polypeptides of high in vivo stability and high specific activities under mild reaction conditions, an asymmetrical bis(benzohydroxamamide) compound with an amine group, 4'-aminomethyl-N,N'-trimethylenedibenzohydroxamamide [NH2-C3(BHam)2], was designed and synthesized. The amine residue of NH2-C3(BHam)2 was converted to a maleimide group by reaction with N-succinimidyl-6-maleimidohexanoate, and the conjugation product was coupled to thiol groups of a monoclonal antibody against osteogenic sarcoma (OST7, IgG1) pretreated with 2-iminothiolane to prepare C3(BHam)2-OST7. 99mTc radiolabeling of C3(BHam)2-OST7 was performed by the exchange reaction with [99mTc]glucoheptonate. [99mTc]C3(BHam)2-OST7 was further characterized using directly radioiodinated OST7 ([125I]OST7) and [111In]labeled OST7 with 1-[4-[(5-maleimidopentyl)amidobenzyl]ethylenediamine-N,N, N'N'-tetraacetic acid (EMCS-Bz-EDTA) as references. [99mTc]C3(BHam)2-OST7 was obtained with radiochemical yields of over 94% at protein concentrations as low as 0.2 mg/mL at room temperature for 1 h. [99mTc]C3(BHam)2-OST7 remained stable after incubation in freshly prepared murine plasma and in the presence of cysteine. Similar binding affinities to tumor cells were observed between [99mTc]C3(BHam)2-OST7 and [125I]OST7. When injected into normal mice, [99mTc]C3(BHam)2-OST7 exhibited radioactivity levels in the blood similar to [111In]-EMCS-Bz-EDTA-OST7 up to 24 h postinjection with significantly faster elimination rate of the radioactivity from the liver. In nude mice bearing osteogenic sarcoma, no significant differences were observed in the radioactivity levels in the blood and the tumor between [99mTc]C3(BHam)2-OST7 and [125I]OST7 at 24 h postinjection. These findings indicated that C3(BHam)2 provided 99mTc chelate of high stability at low concentrations even when conjugated to an intact antibody. Such characteristics render bis(hydroxamamide) compounds useful as chelating molecules for preparation of 99mTc-labeled polypeptides.

Amides↗

PubMed1976

Localization of radiolabeled enzyme inhibitors in the adrenal gland.

Tissue distribution studies were performed in rats and dogs at five time intervals between 10 min and 24 hr after the intravenous injection of one of the following radiolabeled adrenocortical enzyme inhibitors: 3H-amino-glutethimide, 125I-3-iodoaminoglutethimide, 3H-SKF-12185, 125I-3-SKF-12185, 3H-metyrapone. 3H-metyrapol. 3H-amphenone B, and 3H-SU-10603. In rats, 3H-SKF-12185 showed the highest uptake in the whole adrenal (3.5% kg dose/gm at 1 hr). In dogs, 3H-metyrapol showed the highest uptake in the adrenal cortex (9% kg dose/gm at 1 hr), and the peak cortex-to-liver concentration ratio was 57 at 2 hr. These peaks uptakes were comparable to those obtained with the conventional iodocholesterols, but they were reached much earlier, with elimination of most of the adrenal radioactivity by 24 hr. These properties would permit the use of 123I as the label and a higher tracer dose, resulting in a higher photon flux. Thus, the radiolabeled enzyme inhibitors show promise as adrenal-scanning agents, with a markedly shortened scanning procedure, a lower absorbed radiation dose, and better resolution.

Adrenal Gland Diseases↗

PubMed1985

Radionuclide imaging of ovarian tumours with a radiolabelled (123I) monoclonal antibody (NDOG2).

The biodistribution of a radiolabelled monoclonal antibody (123I-NDOG2) was studied in patients with ovarian tumour. It was found that the uptake patterns in known tumour sites was variable and that the clearance of the agent from the vascular pool was due to renal excretion of the radionuclide and the redistribution of the radioactively labelled compound into other compartments. The mean (+/- SD) plasma clearance time was 20.8 (+/- 2.3) h and the ratios of target (tumour) to background (thigh) ranged between 1.4 and 4.8. The ratio between the plasma radioactivity at either 3.5 or 20 h after administration was calculated relative to the initial plasma radioactivity. These values (0.79 and 0.48, respectively) were incorporated into an image-subtraction technique that allowed for redistribution outside the vascular pool. A whole-body dose equivalent to 16.3 mu Sv MBq-1 (60.4 mrem.mCi-1) was calculated.

Antibodies, Monoclonal↗

PubMed2007

Pharmacokinetic study of darbepoetin alfa: absorption, distribution, and excretion after a single intravenous and subcutaneous administration to rats.

KRN321 is a hyperglycosylated analogue of recombinant human erythropoietin (rHuEPO, epoetin alfa), and its absorption, distribution, and excretion have been studied after a single intravenous and subcutaneous administration of 125I-KRN321 at a dose of 0.5 microg kg-1 to male rats. The half-lives of immunoreactive radioactivity in the terminal phase after intravenous and subcutaneous administration were 14.05 and 14.36 h, respectively, and the bioavailability rate after subcutaneous administration was 47%. The total radioactivity in tissues was lower than that in the serum in all tissues excluding the thyroid gland and skin at the injection site (subcutaneous administration). The maximum concentrations were observed in the bone marrow or skin at the injection site followed by the thyroid gland, kidneys, adrenal glands, spleen, lungs, stomach and bladder. The radioactivity found in trichloroacetic acid-precipitated fractions suggested that a high-molecular weight compound, unchanged or mixed with endogenous protein, distributed to the tissues after administration. The whole-body autoradiographic findings in both groups were in agreement with the tissue distribution mentioned above. The blood cell uptake of KRN321 was low for both groups. The excretion ratios of radioactivity into urine and faeces up to 168 h were 71.4 and 14.1% after the intravenous administration and 74.9 and 12.0% after the subcutaneous administration. There was no difference in the excretion profile of radioactivity between the two groups.

Absorption↗

PubMed1994

LH-RH analogue carrying a cytotoxic radical is internalized by rat pituitary cells in vitro.

The binding and internalization of a cytotoxic analogue of luteinizing hormone-releasing hormone (LH-RH), T-98 (agonist [D-Lys6]LH-RH linked to glutaryl-2-(hydroxymethyl)anthraquinone), by rat anterior pituitary cells was investigated. Analogue T-98 was bound to pituitary membrane binding sites for LH-RH with a high affinity (Kd = 1.2 nM) and was 17 times more potent in releasing luteinizing hormone (LH) from superfused rat pituitary cells than LH-RH. The labeling of this cytotoxic LH-RH analogue was carried out both with radioactive (125I) and nonradioactive iodine. Monoiodination of the Tyr5 residue of T-98 did not significantly affect its binding affinity but greatly decreased its LH-releasing activity to about 3% of the original value. Di-iodination in the same position lowered binding affinity twenty-threefold and further diminished LH-releasing potency. [125I]T-98 was found to bind very strongly to polystyrene, which precluded the use of regular tissue culture plasticware in our experiments. In pituitary cells cultured in glass vials, binding and internalization of [125I]T-98 were observed, which were time and temperature dependent, and which could be inhibited by excess unlabeled analogue. No enzymatic degradation of labeled T-98 was detected in the culture medium during the incubation. Our results indicate that T-98 is internalized by pituitary gonadotropes through receptor-mediated endocytosis. Because this new class of compounds was designed as anticancer drugs, our findings also suggest that this cytotoxic LH-RH agonist may also be internalized by LH-RH receptors present in breast, prostate, ovarian, and other tumors.

Animals↗

PubMed2004

Synthesis and preliminary biological evaluation of new radioiodinated MMP inhibitors for imaging MMP activity in vivo.

Non-invasive measurement of matrix metalloproteinase (MMP) activity in vivo is a clinical challenge in many disease processes such as inflammation, tumor metastasis and atherosclerosis. Therefore, radioiodinated analogues of the non-peptidyl broad-spectrum MMP inhibitor (MMPI) CGS 27023A 1a were synthesized for non-invasive detection of MMP activity in vivo using single photon emission computed tomography (SPECT). The compounds Br-CGS 27023A 1b and HO-CGS 27023A 1d were synthesized from the amino acid D-valine and used as precursors for radioiodinated derivatives of CGS 27023A and their non-radioactive references I-CGS 27023A 1c and HO-I-CGS 27023A 1e. Radioiodination of the precursors with [(123)I]NaI or [(125)I]NaI produced the no-carrier-added MMP inhibitors [(123)I]I-CGS 27023A 1f, [(125)I]I-CGS 27023A 1g, HO-[(123)I]I-CGS27023A 1h, and HO-[(125)I]I-CGS 27023A 1i. In vitro studies showed that the non-radioactive analogues of the MMP inhibitors exhibited affinities against gelatinase A (MMP-2) and gelatinase B (MMP-9) in the nanomolar range, comparable to the parent compound CGS 27023A. In vivo biodistribution using HO-[(125)I]I-CGS 27023A 1i in CL57 Bl6 mice showed rapid blood and plasma clearance and low retention in normal tissues. The preliminary biological evaluation warrant further studies of these radioiodinated MMP inhibitors as potential new radiotracers for imaging MMP activity in vivo.

Animals↗

PubMed1985

Radiotracers for functional brain imaging.

The rapid growth of nuclear medicine 25 years ago was in large part related to the success of brain tumor imaging using radiopharmaceuticals designed to detect changes in the blood-brain barrier (BBB). The success of computed tomography, and more recently nuclear magnetic resonance, in imaging these lesions has all but eliminated the use of radioactive agents for brain tumor detection. But, in recent years there has been a new wave of interest in isotope studies of the brain. The recent emphasis has been on agents which enter the brain across the BBB and are designed to provide functional data ranging from regional perfusion and metabolism to the distribution of binding sites for neuroactive compounds. While none of these new radiopharmaceuticals has yet come into widespread clinical application, the research results already achieved clearly indicate that brain imaging will again be an important aspect of nuclear medicine practice.

Amphetamines↗