International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology最新文献

{"title":"Synthesis and biodistribution of a new radiotracer for in vivo labeling of serotonin uptake sites by PET, cis-N,N-[11C]dimethyl-3-(2′,4′-dichlorophenyl)-indanamine (cis-[11C]DDPI)","authors":"Makiko Suehiro,&nbsp;Ursula Scheffel,&nbsp;Robert F. Dannals,&nbsp;Alan A. Wilson,&nbsp;Hayden T. Ravert,&nbsp;Henry N. Wagner Jr","doi":"10.1016/0883-2897(92)90150-W","DOIUrl":"10.1016/0883-2897(92)90150-W","url":null,"abstract":"<div><p>A new PET radiotracer for <em>in vivo</em> labeling of serotonin (5-HT) uptake sites, <em>cis-N</em>, <em>N</em>-[¹¹C]dimethyl-3-(2′,4′-dichlorophenyl)-indanamine, <em>cis</em>-[¹¹C]DDPI, was synthesized and its biological behavior was studied. The radiosynthesis of <em>cis</em>-[¹¹C]DDPI was performed by <em>N</em>-methylation of <em>cis-N</em>-methyl-3-(2′,4′-dichlorophenyl)-indanamine with [¹¹C]iodomethane. The average radiochemical yield was approx. 8%, with an average specific activity of 600mCi/μmol. Following intravenous administration, <em>cis</em>-[¹¹C]DDPI accumulated in mouse brain regions rich in 5-HT uptake sites, such as olfactory tubercles, hypothalamus and frontal cortex. Following pre-injection of 1 mg/kg of paroxetine, a high affinity 5-HT uptake blocker, the binding of <em>cis</em>-[¹¹C]DDPI in the olfactory tubercles, hypothalamus and frontal cortex was decreased by 23, 25 and 16%; this corresponds to 73, 82 and 59% of the specific binding in these regions. These results suggest that the accumulation of <em>cis</em>-[¹¹C]DDPI in the tissues rich in 5-HT sites is a result of specific binding of <em>cis</em>-[¹¹C]DDPI to 5-HT uptake sites. Due to the relatively high non-specific uptake and slow clearance of this compound from non-specific binding sites, the ratio between specific and non-specific binding increased slowly with time, reaching 1.5:1 at 60 min after injection.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 549-553"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90150-W","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571253","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"[75Se]selenite and [75Se]selenate fluctuations during the development of murine hepatoma","authors":"Muhammad Ashraf Tariq ,&nbsp;Ivor L. Preiss","doi":"10.1016/0883-2897(92)90151-N","DOIUrl":"10.1016/0883-2897(92)90151-N","url":null,"abstract":"<div><p>The distribution of selenate and selenite selenium in C57L/J mice during the progression of BW7756 murine hepatoma was investigated using intra-ocular injection with the oxyanions labeled with ⁷⁵Se radioisotope. Comparison is made with the normal distribution of selenium studied by the RIXRF method. The trace elemental profiles, TEP, for the two oxidation states are compared in healthy and disease states. It has been found that the presence of tumor significantly changes the level of tracer in various uninvolved organs. These changes are prominent in the early growth phase of the tumor. The two oxidation states show differences in the TEP for kidney, spleen, stomach and testes.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 555-561"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90151-N","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation of 123I-labeled 2′-iodospiperone and imaging of D2 dopamine receptors in the human brain using SPECT","authors":"Hideo Saji ,&nbsp;Yasuhiko Iida ,&nbsp;Yasuhiro Magata ,&nbsp;Yoshiharu Yonekura ,&nbsp;Yasushi Iwasaki ,&nbsp;Satoshi Sasayama ,&nbsp;Junji Konishi ,&nbsp;Iwao Nakatsuka ,&nbsp;Kunio Shiba ,&nbsp;Akira Yoshitake ,&nbsp;Akira Yokoyama","doi":"10.1016/0883-2897(92)90147-Q","DOIUrl":"10.1016/0883-2897(92)90147-Q","url":null,"abstract":"<div><p>[¹²³I]2′-ISP was readily prepared using a radioiodine exchange reaction with a radiochemical yield of approx. 50% after HPLC purification. The radiochemical purity of the product was more than 98% and the specific activity was 5.55–11.1 GBq/μmol. Biodistribution studies performed in mice indicated that injection of [¹²³I]2′-ISP with albumin produced a higher gastric uptake and a lower brain uptake than injection of the radioligand in a weakly acidic solution. In addition, toxicity tests performed in mice demonstrated that acute toxic effects would be very unlikely to be encountered if 2′-ISP was used for diagnostic purposes. A preliminary imaging study with [¹²³I]2′-ISP in a healthy human volunteer showed its specific uptake by the basal ganglia, a region of the brain known to have a high density of D₂ dopamine receptors.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 523-525, 527-529"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90147-Q","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571250","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Accumulation of radioactivity in the pancreas after intravenous administration of [13N]ammonia","authors":"Hideo Saji ,&nbsp;Yuji Kuge ,&nbsp;Kazutaka Yamamoto ,&nbsp;Yasuhiro Magata ,&nbsp;Yoshiharu Yonekura ,&nbsp;Junji Konishi ,&nbsp;Akira Yokoyama","doi":"10.1016/0883-2897(92)90148-R","DOIUrl":"10.1016/0883-2897(92)90148-R","url":null,"abstract":"<div><p>A biodistribution study of [¹³N]ammonia in rats showed a high accumulation of radioactivity in the pancreas soon after the intravenous injection of this tracer. In humans, the pancreas was also clearly visualized by dynamic positron emission tomography soon after the intravenous injection of [¹³N]ammonia. To investigate the mechanism of the pancreatic accumulation of [¹³N]ammonia, <em>in vitro</em> studies with pancreatic slices and <em>in vivo</em> biodistribution and metabolism studies were carried out in rats. The results indicated that [¹³N]ammonia enters the pancreas from the blood by diffusion at a rate dependent on local blood flow, and then is rapidly incorporated into the amino acid fraction (mainly the glutamine fraction), followed by its incorporation into protein. These findings suggest that [¹³N]ammonia could be useful for diagnostic imaging of the pancreas.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 531-533, 535-537"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90148-R","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571251","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"131I Therapy in diffuse goiters: Should we still use uptake free methods to Calculate activities?","authors":"J. Clerc,&nbsp;M. Izembart,&nbsp;L. Barritault","doi":"10.1016/0883-2897(92)90156-S","DOIUrl":"10.1016/0883-2897(92)90156-S","url":null,"abstract":"","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Page 601"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90156-S","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12570507","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A simple method for producing a technetium-99m-labeled liposome which is stable In Vivo","authors":"William T. Phillips ,&nbsp;Alan S. Rudolph ,&nbsp;Beth Goins ,&nbsp;James H. Timmons ,&nbsp;Robert Klipper,&nbsp;Ralph Blumhardt","doi":"10.1016/0883-2897(92)90149-S","DOIUrl":"10.1016/0883-2897(92)90149-S","url":null,"abstract":"<div><p>A new method for labeling preformed liposomes with technetium-99m (^99mTc) has been developed which is simple to perform and stable <em>in vivo</em>. Previous ^99mTc-liposome labels have had variable labeling efficiencies and stability. This method consistently achieves high labeling efficiencies (&gt; 90%) with excellent stability. A commercially available radiopharmaceutical kit—hexamethylpropyleneamine oxime (HM-PAO)—is reconstituted with ^99mTcO^−₄ and then incubated with preformed liposomes that encapsulate glutathione. The incubation takes only 30 min at room temperature. Liposomes that co-encapsulate other proteins such as hemoglobin or albumin, in addition to glutathione, also label with high efficiency. Both <em>in vitro</em> and <em>in vivo</em> studies indicate good stability of this label. Rabbit images show significant spleen and liver uptake at 2 and 20 h after liposome infusion without visualization of thyroid, stomach or bladder activity.</p><p>This labeling method can be used to study the biodistribution of a wide variety of liposome preparations that are being tested as novel drug delivery systems. This method of labeling liposomes with ^99mTc may also have applications in diagnostic imaging.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 539-543, 545-547"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90149-S","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571252","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation and in vivo binding of [11C]carazolol, a radiotracer for the beta-adrenergic receptor","authors":"Marc S. Berridge,&nbsp;Emily H. Cassidy,&nbsp;Andrew H. Terris,&nbsp;Jean-Marc Vesselle","doi":"10.1016/0883-2897(92)90152-O","DOIUrl":"10.1016/0883-2897(92)90152-O","url":null,"abstract":"<div><p>Carazolol is a high affinity beta-adrenergic receptor antagonist which is relatively non-specific for the receptor subtypes. The labeling of the two enantiomers of this compound with carbon-11, including the synthesis of the required labeling precursors, is reported. The yield and specific activity are sufficient for use in positron tomography. Biodistribution and specific receptor binding studies show the labeled material to be of interest for further investigation as a radiopharmaceutical for positron tomography.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 563-569"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90152-O","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12530438","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Radiolabeled products in rat liver and serum after administration of antibody—amide—DTPA—indium-111","authors":"C.H. Paik ,&nbsp;V.K. Sood ,&nbsp;N. Le ,&nbsp;L. Cioloca ,&nbsp;J.A. Carrasquillo ,&nbsp;J.C. Reynolds ,&nbsp;R.D. Neumann ,&nbsp;R.C. Reba","doi":"10.1016/0883-2897(92)90146-P","DOIUrl":"10.1016/0883-2897(92)90146-P","url":null,"abstract":"<div><p>Anti-human serum albumin antibody (Ab) was used as a model antibody. Ab was conjugated with DTPA using cyclic DTPA dianhydride reaction and radiolabeled with ¹¹¹In. The labeled Ab was purified by affinity chromatography. Size exclusion HPLC of this product showed 62% of ¹¹¹In bound to monomeric Ab and 38% of the activity bound to antibody oligomers with molecular weights ranging from 300,000 to 450,000. The labeled antibody preparation was injected into the tail vein of rats. The radioactive substances in serum and the supernatant from liver homogenates were analyzed for molecular weight and immunoreactivity. Size exclusion HPLC of the serum samples indicated that the monomeric and dimeric Abs disappeared from the serum at a similar rate over a 48 h period. In addition, a new radioactive substance with an estimated molecular weight of 35,000 appeared in the serum. The immunoreactive fraction of the circulating ¹¹¹In substances decreased slowly, somewhat proportional to the appearance of the metabolite. On the other hand, the immunoreactivity of the ¹¹¹In substances in the supernatant from the liver homogenate decreased rapidly and no appreciable immunoreactivity was observed after 48 h. The labeled antibody was catabolized very rapidly in the liver and the major activity in the supernatant was associated with a small molecular weight metabolite which had a HPLC retention time identical to that of DTPA-¹¹¹In. The second metabolite had an estimated molecular weight of 35,000. No radioactivity was associated with transferrin.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 517-522"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90146-P","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571249","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and evaluation of high affinity, aryl-substituted [18F]fluoropropylbenzamides for dopamine D-2 receptor studies","authors":"Chester A. Mathis ,&nbsp;John E. Bishop ,&nbsp;John M. Gerdes ,&nbsp;John M. Whitney ,&nbsp;Kathleen M. Brennan ,&nbsp;William J. Jagust","doi":"10.1016/0883-2897(92)90153-P","DOIUrl":"10.1016/0883-2897(92)90153-P","url":null,"abstract":"<div><p>The potent dopamine D-2 ligands (<em>S</em>)-2,3-dimethoxy-<em>N</em>-[(1-ethyl-2-pyrrolidinyl)methyl]-5-(3-[¹⁸F]fluoropropyl)benzamide (¹⁸<strong>F-1</strong>) and (<em>S</em>)-2,3-dimethoxy-<em>N</em>-[(1 -ethyl-2-pyrrolidinyl)methyl]-5-(3-[¹⁸F]fluoropropyl)-6-hydroxybenzamide (¹⁸<strong>F-2</strong>) were prepared in high specific activity and 5–25% overall radiochemical yields. Benzamide <strong>1</strong> possessed a lower <em>in vitro</em> binding affinity for the D-2 receptor than salicylamide <strong>2</strong>, but the <em>in vivo</em> striatal-to-cerebellar radioactivity concentration ratios (<span><math><mtext>St</mtext><mtext>Cb</mtext></math></span>) in rats and dogs were nearly identical for the two compounds. Compound ¹⁸<strong>F-2</strong> was more lipophilic than ¹⁸<strong>F-1</strong>, and its increased penetration into and retention by striatal tissue was matched by an increase in non-specific binding in the cerebellum. Cerebral cortex radioactivity concentration levels in dogs were similar to cerebellum levels. The binding of ¹⁸F-labelled <strong>1</strong> and <strong>2</strong> displayed regional brain distribution patterns consistent with known dopamine D-2 receptor densities and was selectively blocked in the striatum of rats by dopamine D-2 antagonists. The binding of ¹⁸<strong>F-1</strong> was found to be stereoselective, as the ¹⁸F-labelled (<em>R</em>)-enantiomer displayed no selective retention in the striatum of dogs. High levels of radioactivity were found in the bones of rats following the injection of ¹⁸<strong>F-1</strong> and ¹⁸<strong>F-2</strong>, indicating that <em>in vivo</em> defluorination had occurred; however, no bone radioactivity was observed in dogs following the injection of these radioligands. Compound ¹⁸<strong>F-1</strong> was displaced from the striatum of dogs by both <em>d</em>-amphetamine-stimulated dopamine release and haloperidol at doses of 1 and 0.5 mg/kg, respectively, while compound ¹⁸<strong>F-2</strong> was displaced from the dog striatum only by haloperidol at these doses. The radioligand ¹⁸<strong>F-2</strong> holds promise for positron emission tomography studies of the dopamine D-2 receptor system based upon its selective, potent binding and resistance to displacement by endogenous dopamine.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 571-583, 585-588"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90153-P","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571255","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Use of ex vivo binding to measure the brain concentrations of putative radioligands","authors":"Jesse Baumgold,&nbsp;Pei-Ying Ling,&nbsp;Richard C. Reba","doi":"10.1016/0883-2897(92)90145-O","DOIUrl":"10.1016/0883-2897(92)90145-O","url":null,"abstract":"<div><p>The development of radioligands capable of imaging brain receptors depends on, amongst other factors, the ability of such compounds to penetrate the blood-brain barrier. We describe an <em>ex vivo</em> binding technique for measuring the brain concentration of peripherally administered unlabeled compounds. This technique can be used early in the development of putative radioligands. The pharmacokinetics of brain penetration of three muscarinic antagonists are described: QNB, BrQNB and the 2-thienyl derivative of BrQNB and were found to compare favorably to previous studies using [³H]QNB. These studies demonstrate the effectiveness of <em>ex vivo</em> binding in assessing the brain concentration of peripherally administered unlabeled compounds.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 513-516"},"PeriodicalIF":0.0,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90145-O","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12571248","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}