Zaihui Zhang , Donald M. Lyster , Gordon A. Webb , Chris Orvig
{"title":"Potential 67Ga radiopharmaceuticals for myocardial imaging: Tris(1-aryl-3-hydroxy-2-methyl-4-pyridinonato)gallium(III) complexes","authors":"Zaihui Zhang , Donald M. Lyster , Gordon A. Webb , Chris Orvig","doi":"10.1016/0883-2897(92)90118-I","DOIUrl":"10.1016/0883-2897(92)90118-I","url":null,"abstract":"<div><p>A series of highly lipophilic complexes of 1-aryl-3-hydroxy-2-methyl-4-pyridinones with gallium(III)-67 has been evaluated <em>in vitro</em> and <em>in vivo</em> as potential radiopharmaceuticals. The pyridinones have different substituents at the <em>para</em>-position of the phenyl ring: R = H, CH<sub>3</sub>, OCH<sub>3</sub> and NO<sub>2</sub>. Biodistribution studies of <sup>67</sup>Ga complexes have been carried out in rabbits, mice, rats and a dog. High heart uptake of the radionuclide has been shown in rabbits and the dog. The different biodistribution patterns in mice and rats indicate that there is a species difference in the biodistribution of these complexes. Rabbits and the dog show rapid heart uptake and blood clearance. The speciation of the Ga<sup>3+</sup> ion <em>in vivo</em> is simulated <em>in vitro</em> with a simple blood plasma model based on the available thermodynamic data.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 3","pages":"Pages 327-331, 333-335"},"PeriodicalIF":0.0,"publicationDate":"1992-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90118-I","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12794837","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":"4-Borono-2-[18F]fluoro-d,l-phenylalanine: a possible tracer for melanoma diagnosis with PET","authors":"Kiichi Ishiwata , Tatsuo Ido , Chihiro Honda , Mieko Kawamura , Masamitsu Ichihashi , Yutaka Mishima","doi":"10.1016/0883-2897(92)90116-G","DOIUrl":"10.1016/0883-2897(92)90116-G","url":null,"abstract":"<div><p>The potential of 4-borono-2-[<sup>18</sup>F]fluoro-<span>d,l</span>-phenylalanine ([<sup>18</sup>F]FBPA), a fluorinated derivative of a target compound for boron neutron capture therapy, for melanoma imaging by positron emission tomography (PET) was studied using animal models. A high uptake of [<sup>18</sup>F]FBPA was found in murine B16 melanoma or in Greene's melanoma No. 179, a melanotic cell line in hamsters, for the first 6 h after injection. Whole body autoradiography using [<sup>18</sup>F]FBPA gave a clear image of the B16 tumor. The acid-insoluble <sup>18</sup>F in the B16 increased to 27% by 6h, and most of the free <sup>18</sup>F was detected as [<sup>18</sup>F]FBPA in both B16 and plasma. In the hamster models, No. 179 showed a 1.7 times higher uptake than amelanotic Greene's melanoma No. 178 at 6 h post-injection, although both melanomas indicated similar metabolic activities when examined by a tracer uptake study using <span>l</span>-[<sup>14</sup>C]methionine, 2-deoxy-<span>d</span>-[<sup>14</sup>C]glucose and [<sup>3</sup>H]thymidine. [<sup>18</sup>F]FBPA may be a very promising PET tracer for melanoma imaging.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 3","pages":"Pages 311-315, 317-318"},"PeriodicalIF":0.0,"publicationDate":"1992-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90116-G","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12795591","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}
C.S. John , E.O. Schlemper , P. Hosain , C.H. Paik , R.C. Reba
{"title":"Synthesis, characterization and biodistribution of a new hexadentate aminethiol ligand labeled with Tc-99m","authors":"C.S. John , E.O. Schlemper , P. Hosain , C.H. Paik , R.C. Reba","doi":"10.1016/0883-2897(92)90110-K","DOIUrl":"10.1016/0883-2897(92)90110-K","url":null,"abstract":"<div><p>A new hexadentate aminethiol ligand (TACNS) derived from triazacyclononane was synthesized and characterized for the development of technetium radiopharmaceuticals. The ligand formed a neutral, lipophilic and stable complex with [<sup>99m</sup>Tc]pertechnetate in the presence of tin(II)tartarate as a reducing agent. The biodistribution of [<sup>99m</sup>Tc]TACNS indicates slight uptake in brain (0.23% ID/organ at 5 min) with a washout at 30 min to 0.14% ID/organ. A small uptake in heart (0.48% ID at 5 min) was also observed.</p><p>The characterization of [<sup>99m</sup>Tc]TACNS complex using single crystal x-ray analysis and mass spectroscopy has shown that an Sn-N<sub>3</sub>S<sub>3</sub> complex was formed in which tin is oxidized from Sn(II) to Sn(IV). Pertechnetate was incorporated into the complex as counter anion. The nature of the species formed with Tc-99 and “no-carrier-added” [<sup>99m</sup>Tc]pertechnetate is different as confirmed by ratio TLC. From these results, it is demonstrated that sometimes it may be difficult to predict the structure of new technetium radiopharmaceuticals, especially when stannous ion is used as a reducing agent. Moreover, the nature of the chemical species may not be the same at millimolar and at nanomolar levels.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 3","pages":"Pages 269-274"},"PeriodicalIF":0.0,"publicationDate":"1992-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90110-K","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12494664","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":"Announcementiol.","authors":"","doi":"10.1016/0883-2897(92)90014-P","DOIUrl":"https://doi.org/10.1016/0883-2897(92)90014-P","url":null,"abstract":"","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Page I"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90014-P","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136492040","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
G.J. Beyer, R. Bergmann, G. Kampf, P. Mäding, F. Rösch
{"title":"Simultaneous study of the biodistribution of radio-yttrium complexed with EDTMP and citrate ligands in tumour-bearing rats","authors":"G.J. Beyer, R. Bergmann, G. Kampf, P. Mäding, F. Rösch","doi":"10.1016/0883-2897(92)90008-M","DOIUrl":"10.1016/0883-2897(92)90008-M","url":null,"abstract":"<div><p>The influence of the ligands ethylenediaminetetramethylene phosphonic acid (EDTMP) and citrate (CIT) on the biodistribution of radio-yttrium in rats bearing a DS-carcinosarcoma was compared. <sup>88</sup>Y-EDTMP and <sup>87</sup>Y-CIT were i.v. injected into the same animals. Faster blood clearance and higher renal excretion were observed for the EDTMP-ligand. Of high practical interest is the reduced liver uptake of radio-yttrium (by one order of magnitude) with the EDTMP complex. Since bone and tumour accumulation is only weakly influenced, high tumour-to-liver ratios (up to 14) were observed. We propose to use EDTMP or similar complex ligands for liver blocking when radionuclides like <sup>90</sup>Y, <sup>169</sup>Yb, <sup>225</sup>Ac or other group 3 elements are to be applied in endoradionuclide therapy technique.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 201-203"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90008-M","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768631","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":"Investigations of N-linked macrocycles for 111in and 90Y labeling of proteins","authors":"C. Wu, F. Virzi, D.J. Hnatowich","doi":"10.1016/0883-2897(92)90012-N","DOIUrl":"10.1016/0883-2897(92)90012-N","url":null,"abstract":"<div><p>To simplify the synthesis of macrocyclic chelators, commercially available macrocyclic amines were condensed with halogenated acetic acid to prepare the five chelators 12N4 (DOTA), 14N4 (TETA), 15N4, 9N3 and 12N3. Only 12N4 and 9N3 showed efficient labeling of the free chelator with <sup>111</sup>In and <sup>90</sup>Y. Serum stability studies at 37 °C with In-labeled DTPA, 12N4 and 9N3 showed no loss of label over 2 days whereas, with <sup>90</sup>Y, only 12N4 showed stabilities comparable to DTPA. The 12N4 chelator was derivatized by attaching biotin on one N-acetate group to simulate the attachment to protein. The serum stability for both <sup>111</sup>In and <sup>90</sup>Y was identical to that of biotin derivatized DTPA and lower than that of the free chelators. Biodistribution studies in normal mice of a model protein (avidin) labeled with <sup>90</sup>Y via biotinylated 12N4 and biotinylated DTPA showed identical distribution at 1 day except in bone where the %ID/g for the macrocyclic-conjugated protein (3.4 ± 0.5, <em>N</em> = 8) was significantly (<em>P</em> < 0.001) lower than that of the DTPA-conjugated protein (9.4 ± 0.9, <em>N</em> = 7). In conclusion, macrocycles may be readily synthesized from the macrocyclic amines and several show useful stabilities with In and Y. When N-linked to a protein, the Y biodistribution was found to be superior to that of the corresponding DTPA-coupled protein.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 239-244"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90012-N","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768634","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}
Irene Virgolini , J. O'Grady , Graziana Lupattelli , F. Rauscha , P. Angelberger , S. Ventura , H. Sinzinger
{"title":"In vivo quantification of cholesterol content in human carotid arteries by quantitative Gamma-camera imaging after injection of autologous low density lipoproteins (LDL)","authors":"Irene Virgolini , J. O'Grady , Graziana Lupattelli , F. Rauscha , P. Angelberger , S. Ventura , H. Sinzinger","doi":"10.1016/0883-2897(92)90013-O","DOIUrl":"10.1016/0883-2897(92)90013-O","url":null,"abstract":"<div><p>Low density lipoprotiens (LDL) were isolated by immunoaffinity chromatography from 18 patients (31–70 years) suffering from primary hypercholesterolemia with angiographically proven atherosclerosis of either one or both carotid arteries. LDL were labeled with <sup>123</sup>I (1 mCi/mg LDL) by the iodine monochloride method followed by purification with dialysis and immediately reinjected thereafer. Gamma-camera serial controls over carotid regions allowed visual detection of uptake of the radiocompound uptake in 12 out of the 18 patients. The lipid entry ratio (LER; counts over the vascular region/pixel as compared to the contralateral side after background subtraction) confirmed the visual findings. Whole body images performed until 20 h after reinjection showed 3 different kinetic types of LDL-influx into the vessel wall: decreasing (type I), increasing and then decreasing (type II) and continuously increasing (type III) with time. Four patients underwent endarterectomy within 2–7 weeks after gamma-camera imaging. Histological control revealed an extensive amount of “foam cells” in tissue samples derived during surgery and an absence of endothelial lining in samples belonging to patients with type II kinetics.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 245-247, 249-250"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90013-O","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768635","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":"Radioimmunotherapy: Clinical results and dosimetric considerations","authors":"Virginia K. Langmuir","doi":"10.1016/0883-2897(92)90010-V","DOIUrl":"10.1016/0883-2897(92)90010-V","url":null,"abstract":"<div><p>Radiolabeled antibodies for cancer therapy are being investigated in clinical trials in more than 30 centers. <sup>131</sup>Iodine-labeled antibody (Ab) therapy of solid tumors has produced few responses when given alone. When given in conjunction with chemotherapy and external beam therapy in hepatoma patients, objective responses have occurred. Because of the short range of <sup>131</sup>I, <sup>90</sup>Y and <sup>186</sup>Re are being studied and objective responses have occurred in patients without the addition of other therapies. <sup>131</sup>I-labeled Ab therapy of lymphoma, a radioresponsive tumor, has produced a much higher objective response rate than in other solid tumors. Regional RIT has not been shown to offer a definite advantage over the intravenous route. Tumor doses have generally been less than 2000 cGy per treatment with some tumors receiving higher doses. The bone marrow is the dose-limiting organ for RIT and marrow cryopreservation with subsequent reinfusion may prove useful.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 213-225"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90010-V","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12703527","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}
James F. Kronauge , Mary L. Chiu , Jeffrey S. Cone , Alan Davison , B.Leonard Holman , Alun G. Jones , David Piwnica-Worms
{"title":"Comparison of neutral and cationic myocardial perfusion agents: Characteristics of accumulation in cultured cells","authors":"James F. Kronauge , Mary L. Chiu , Jeffrey S. Cone , Alan Davison , B.Leonard Holman , Alun G. Jones , David Piwnica-Worms","doi":"10.1016/0883-2897(92)90001-F","DOIUrl":"10.1016/0883-2897(92)90001-F","url":null,"abstract":"<div><p>Uptake and washout kinetics of two new neutral lipophilic technetium-99m-labeled boronic acid adducts of technetium tris(dioxime) (BATO complexes) were studied in monolayers of contractile chick heart cells and compared to the cationic myocardial perfusion agents, <sup>99m</sup>Tc(CNCH<sub>2</sub>C(CH<sub>3</sub>)<sub>2</sub>OCH<sub>3</sub>)<sup>+</sup><sub>6</sub> (Tc-MIBI) and <sup>201</sup>Tl<sup>+</sup>. <sup>99m</sup>TcCl(CDOH)<sub>2</sub>(CDO)(BCH<sub>3</sub>), where CDO = cyclohexanedione dioxime (CDO-MeB), had a 7-fold greater net accumulation than Tc-MIBI and the most rapid unidirectional washout with a fast initial phase and a slower secondary component. Incubation with cationic membrane transport inhibitors or metabolic inhibitors had little or modest influence, respectively, on uptake of these BATO complexes. Studies with NIH 3T3 fibroblasts indicated that the neutral complexes did not show myocyte specific accumulation.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 141-148"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90001-F","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768715","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":"The distribution of radioactivity in brains of rats given [N-methyl-11C]PK 11195 in vivo after induction of a cortical ischaemic lesion","authors":"J.E. Cremer, S.P. Hume, B.M. Cullen, R. Myers, L.G. Manjil, D.R. Turton, S.K. Luthra, D.M. Bateman, V.W. Pike","doi":"10.1016/0883-2897(92)90003-H","DOIUrl":"10.1016/0883-2897(92)90003-H","url":null,"abstract":"<div><p>PK 11195 is a selective ligand for the peripheral-type benzodiazepine binding site (PTBBS). There are few such sites in normal brain but their number increases in association with tissue necrosis. The time-course of appearance of PTBBS around a focally induced ischaemic lesion in frontal cortex of rat brain was established by autoradiography using [<em>N</em>-methyl-<sup>3</sup>H]PK 11195. Using this information and the same experimental model of ischaemia, the distribution of radioactivity after injection of carbon-11 (<span><math><mtext>t</mtext><msub><mi></mi><mn><mtext>1</mtext><mtext>2</mtext></mn></msub><mtext> = 20.3 </mtext><mtext>min</mtext></math></span>, β<sup>+</sup> = 99.8%) labelled PK 11195 was studied. The purpose was to synthesize [<em>N</em>-methyl-<sup>11</sup>C]PK 11195 and to test its suitability as a tracer for depicting the presence of PTBBS in ischaemic lesions. The time-profiles of distribution of radioactivity in brain regions after intravenous injection of tracer and the ratio of radioactivity in lesioned compared with unlesioned cortex were determined. Data for the temporal (days after lesion induction) and for the regional retention of radioactivity were consistent with independent evidence (autoradiographic and immunohistochemical) for the occurrence of increased numbers of PTBBS, predominantly in association with macrophages, in areas undergoing necrosis.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 159-161, 163-166"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90003-H","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768717","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}