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  • 1
    Electronic Resource
    Electronic Resource
    Radiotherapy with a Radiolabeled Somatostatin Analogue, [111In-DTPA-d-Phe1]-Octreotide (1994)
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 733 (1994), S. 0 
    Details
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1749-6632.1994.tb17300.x
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  • 2
    Electronic Resource
    Electronic Resource
    Radiolabelled somatostatin analogue(s) for peptide receptor scintigraphy and radionuclide therapy (1999)
    Springer
    Annals of oncology 10 (1999), S. 23-29 
    Details
    ISSN: 1569-8041
    Keywords: octreotide ; peptide ; radionuclide ; scintigraphy ; somatostatin ; therapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Background: Peptide receptor scintigraphy with the radioactive somatostatin analogue, [111In-DTPA0]octreotide, is a sensitive and specific technique to show in vivo the presence and abundance of somatostatin receptors on various tumours. Aim: With this technique primary tumours and metastases of neuroendocrine cancers as well as of many other cancer-types can be localised. This technique is currently used to assess the possibility of peptide receptor radionuclide therapy (PRRT) with repeated administrations of high doses of [111In-DTPA0]octreotide. 111In emits Auger and conversion electrons having a tissue penetration of 0.02–10 µm and 200 to 500 µm, respectively. Patients and methods: Thirty end-stage patients with mostly neuroendocrine progressing tumours were treated with [111In-DTPA0]octreotide, up to a maximal cumulative patient dose of about 74 GBq, in a phase I trial. Results: There were no major clinical side effects after up to two years treatment, except that in a few patients a transient decline in platelets counts and lymphocyte subsets occurred. Promising beneficial effects on clinical symptoms, hormone production and tumour proliferation were found. Of the 21 patients who received a cumulative dose of more than 20 GBq, eight patients showed stabilisation of disease and six other patients a reduction in size of tumours. There is a tendency towards better results in patients whose tumours have a higher accumulation of the radioligand. Conclusions: PRRT is feasible, also with 111In as radionuclide. Depending on the homogeneity of distribution of tumour cells expressing peptide receptors and the size of the tumour, β-emitting radionuclides, e.g., 90Y, labelled to DOTA-chelated peptides, are also attractive candidates for PRRT. The first PRRT trials with [90Y-DOTA0,Tyr3]octreotide started recently.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1027396313397
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  • 3
    Electronic Resource
    Electronic Resource
    Octreotide scintigraphy localizes somatostatin receptor-positive islet cell carcinomas (1991)
    Springer
    European journal of nuclear medicine 18 (1991), S. 924-927 
    Details
    ISSN: 1619-7089
    Keywords: Iodine-123-Tyr-Octreotide ; Somatostatin receptors ; In vivo ; In vitro ; Pancreatic islet cell carcinoma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Tyr-3-Octreotide is a synthetic derivative of somatostatin and a somatostatin-receptor analogue. The iodine-123-labelled compound localizes somatostatin-receptor-positive tumours. In this paper two patients are reported in whom somatostatin receptors were demonstrated in vitro. In a 60-year-old female with an islet cell carcinoma of the pancreas, multiple liver metastases and previously unrecognized bone metastases in the right acetabulum could be diagnosed as the reason for a persistent hypoglycaemia. In a 60-year-old male an islet cell carcinoma of the pancreas was localized with123I-Tyr-3-octreotide. The somatostatin receptors were demonstrated in vitro and the tumour was successfully treated with somatostatin. These studies demonstrate that123I-Tyr-3-octreotide offers the possibility of localizing somatostatin-receptor-positive tumours and their metastases. Moreover the method makes it possible to determine the receptor status of a tumour in vivo.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02258458
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  • 4
    Electronic Resource
    Electronic Resource
    Radioiodinated somatostatin analogue RC-160: preparation, biological activity, in vivo application in rats and comparison with [123I-Tyr3]octreotide (1993)
    Springer
    European journal of nuclear medicine 20 (1993), S. 1089-1094 
    Details
    ISSN: 1619-7089
    Keywords: Radioiodinated RC-160 ; Somatostatin ; Specific binding ; Tumour imager ; Peptide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We have evaluated the potential usefulness of the radioiodinated octapeptide RC-160, a somatostatin analogue, which might serve as a radiopharmaceutical for the in vivo detection of somatostatin receptor-positive tumours. For this purpose, iodine-123 and iodine-125 labelled RC-160 was tested for biological activity and applied in vivo in rats bearing the transplantable rat pancreatic tumour CA20948, which expresses somatostatin receptors. Our group has recently described the in vivo visualization of such tumours in rats and in humans with the radioiodinated somatostatin analogue [Tyr3]octreotide. Like [123I-Tyr3]octreotide, 123I-RC-160 showed uptake in and specific binding in vivo to somatostatin receptor-positive organs and tumours. However, blood radioactivity (background) was higher, resulting in a lower tumour to blood (background) ratio. We therefore conclude that in this animal model 123I-RC-160 has no advantage over [123I-Tyr3]octreotide as a radiopharmaceutical for the in vivo use as a somatostatin receptor imager, although, like [123I-Tyr3]octreotide, 123I-RC-160 shows specific binding to different somatostatin receptor-positive organs. Recently differences were reported in affinity between somatostatin and its analogues for somatostatin receptors expressed in different human cancers, like those of the breast, ovary, exocrine pancreas, prostate and colon. Therefore 123I-RC-160 might be of interest for future use in humans as a radiopharmaceutical for imaging octreotide receptor-negative tumours.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00173488
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  • 5
    Electronic Resource
    Electronic Resource
    Somatostatin receptor scintigraphy with [111In-DTPA-d-Phe1]- and [123I-Tyr3]-octreotide: the Rotterdam experience with more than 1000 patients (1993)
    Springer
    European journal of nuclear medicine 20 (1993), S. 716-731 
    Details
    ISSN: 1619-7089
    Keywords: Somatostatin ; Octreotide ; Tumour targeting ; Receptor imaging ; Apudoma ; Lymphoma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Various tumours, classically specified as either neuroendocrine or non-neuroendocrine, contain high numbers of somatostatin receptors, which enable in vivo localization of the primary tumour and its metastases by scintigraphy with the radiolabelled somatostatin analogue octreotide. In addition granulomas and autoimmune processes can be visualized because of local accumulation of somatostatin receptor-positive activated mononuclear leucocytes. In many instances a positive scintigram predicts a favourable response to treatment with octreotide. It is tempting to speculate that octreotide labelled with an appropriate radionuclide might be used in cancer therapy. The successful application of radiolabelled octreotide in scintigraphy indicates the possible usefulness of other radiolabelled peptides, either native peptides or derivatives of these, in, for example, nuclear oncology. The small size of these peptides, e.g. bombesin and substance P, is of the utmost importance for a relatively fast blood clearance, thus leading to low background radioactivity. In this way peptides are powerful alternatives to (fragments of) monoclonal antibodies, the application of which to scintigraphic localization of specific cell surface antigen-bearing tumours is plagued by slow blood clearance and, hence, high background levels.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00181765
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  • 6
    Electronic Resource
    Electronic Resource
    Visualization of the thymus by substance P receptor scintigraphy in man (1996)
    Springer
    European journal of nuclear medicine 23 (1996), S. 1508-1513 
    Details
    ISSN: 1619-7089
    Keywords: Substance P ; Thymus ; Immune-mediated diseases ; Inflammatory bowel disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Substance P, an 11-amino acid neuropeptide, has an important role in modulating pain transmission through neurokinin 1 and 2 receptors. Substance P and other tachykinins may also play a role in the pathogenesis of inflammatory diseases. In this study we present the results concerning the metabolism of the substance P analogue [111In-DTPA-Arg1]-substance P in man, as well as the visualization of the thymus in patients with immune-mediated diseases. Twelve selected patients were investigated, comprising five with inflammatory bowel disease, one with ophthalmic Graves' disease, one with sclerosing cholangitis, one with Sjögren's syndrome, one with rheumatoid arthritis, one with systemic lupus erythematosus and two with myasthenia gravis. During and after intravenous administration of 150-250 MBq (2.5–5.0 μg) [111In-DTPA-Arg1]-substance P, blood pressure, heart rate and oxygen saturation were monitored. Radioactivity was measured in blood, urine and faeces during the 48 h after injection. Planar and single-photon emission tomographic images were obtained 4 and 24 h after injection. After administration of [111In-DTPA-Arg1]-substance P, a transient flush was observed in all patients. Degradation of [111In-DTPA-Arg1]-substance P started in the first minutes after administration, resulting in a half-life of 10 min for the total plasma radioactivity, and of 4 min for the intact radiopharmaceutical, as identified with high-performance liquid chromatography. Urinary excretion accounted for 〉95% of the radioactivity within 24 h post injection, and up to 0.05% was found in the faeces up to 60 h. In all patients uptake of radioactivity was found in the areolae mammae (in women), liver, spleen, kidneys and urinary bladder. In eight patients a high uptake of [111In-DTPA-Arg1]-substance P was observed in the thymus. We conclude that, despite its short half-life, [111In-DTPA-Arg1]-substance P, a new radio-pharmaceutical, can be used to visualize the thymus. This may contribute to the investigation of the role of thymus in immune-mediated diseases. In addition, inflammatory sites in various diseases could be visualized.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01254476
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  • 7
    Electronic Resource
    Electronic Resource
    A new radiolabelled somatostatin analogue [111In-DTPA-D-Phe1]RC-160: preparation, biological activity, receptor scintigraphy in rats and comparison with [111In-DTPA-D-Phe1]octreotide (1994)
    Springer
    European journal of nuclear medicine 21 (1994), S. 328-335 
    Details
    ISSN: 1619-7089
    Keywords: Radioindium labelled RC-160 ; Somatostatin ; Specific binding ; Tumour imager ; Radiopharmaceutical ; Peptide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We have evaluated the potential usefulness of indium-111 labelled [DTPA-D-Phe1]RC-160, derived from the octapeptide somatostatin analogue RC-160, as a radiopharmaceutical for the in vivo detection of somatostatin receptor-positive tumours. For this purpose 111In-and 111In-labelled [DTPA-D-Phe1]RC-160 was tested for its biological activity, and applied for somatostatin receptor scintigraphy in vivo to rats bearing the transplantable rat pancreatic tumour CA20948, which expresses somatostatin receptors. We previously described the development of the 111In-labelled somatostatin analogue [DTPA-D-Phe1]octreotide and its use in the in vivo visualization of somatostatin receptor-positive tumours in rats and in humans. Like [111In-DTPA-D-Phe1]octreotide, [111In-DTPA-D-Phe1]RC-160 showed uptake in and specific binding in vivo to somatostatin receptor-positive organs and tumours, and the tumours were clearly visualized by gamma camera scintigraphy. However, as compared to [111In-DTPA-D-Phe1]octreotide, blood radioactivity (background) was higher, resulting in a lower tumour to blood (background) ratio. Using this animal model we therefore conclude that [111In-DTPA-DPhe1]RC-160 has no advantage over [111In-DTPA-DPhe1]octreotide as a radiopharmaceutical in the visualization of somatostatin receptors which bind both analogues. However, recent reports suggest the existence of different somatostatin receptor subtypes on some human cancers, which differentially bind RC-160 and not octreotide. These tumours include cancers of the breast, ovary, exocrine pancreas, prostate and colon. [111In-DTPA-D-Phe1]RC-160 might be of interest for future use in such cancer patients as a radiopharmaceutical for imaging somatostatin receptor-positive tumours, which do not bind octreotide.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00176572
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  • 8
    Electronic Resource
    Electronic Resource
    A new radiolabelled somatostatin analogue [111In-DTPA-D-Phe1]RC-160: preparation, biological activity, receptor scintigraphy in rats and comparison with [111In-DTPA-D-Phe1]octreotide (1994)
    Springer
    European journal of nuclear medicine 21 (1994), S. 328-335 
    Details
    ISSN: 1619-7089
    Keywords: Radioindium labelled RC-160 ; Somatostatin ; Specific binding ; Tumour imager ; Radiopharmaceutical ; Peptide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We have evaluated the potential usefulness of indium-111 labelled [DTPA-D-Phe1]RC-160, derived from the octapeptide somatostatin analogue RC-160, as a radiopharmaceutical for the in vivo detection of somatostatin receptor-positive tumours. For this purpose111In-and111In-labelled [DTPA-D-Phe1]RC-160 was tested for its biological activity, and applied for somatostatin receptor scintigraphy in vivo to rats bearing the transplantable rat pancreatic tumour CA20948, which expresses somatostatin receptors. We previously described the development of the111In-labelled somatostatin analogue [DTPA-D-Phe1]octreotide and its use in the in vivo visualization of somatostatin receptor-positive tumours in rats and in humans. Like [111In-DTPA-D-Phe1]octreotide, [111In-DTPA-D-Phe1]RC-160 showed uptake in and specific binding in vivo to somatostatin receptor-positive organs and tumours, and the tumours were clearly visualized by gamma camera scintigraphy. However, as compared to [111In-DTPA-D-Phe1]octreotide, blood radioactivity (background) was higher, resulting in a lower tumour to blood (background) ratio. Using this animal model we therefore conclude that [111In-DTPA-DPhe1]RC-160 has no advantage over [111In-DTPA-DPhe1]octreotide as a radiopharmaceutical in the visualization of somatostatin receptors which bind both analogues. However, recent reports suggest the existence of different somatostatin receptor subtypes on some human cancers, which differentially bind RC-160 and not octreotide. These tumours include cancers of the breast, ovary, exocrine pancreas, prostate and colon. [111In-DTPA-D-Phe1]RC-160 might be of interest for future use in such cancer patients as a radiopharmaceutical for imaging somatostatin receptor-positive tumours, which do not bind octreotide.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00947968
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  • 9
    Electronic Resource
    Electronic Resource
    Myocardial substrate utilization and hemodynamics following repeated coronary flow reduction in pigs (1979)
    Springer
    Basic research in cardiology 74 (1979), S. 477-493 
    Details
    ISSN: 1435-1803
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Der Effekt von wiederholter lokaler Ischämie und Reperfusion auf den myokardialen Energiestoffwechsel und Ventrikelfunktion wurde bei 12 narkotisierten Schweinen mit geöffnetem Thorax studiert. Die Schweine hatten 24 Stunden gefastet. Die myokardiale Ischämie wurde verursacht durch eine Reduktion der Blutdurchströmung in der linken Anterior Descending Koronar Arterie bis 40% vom Anfangswert während 30 Minuten. Eine zweite Reduktion wurde nach 35 Minuten Reperfusion angefangen. Die zweite Reduktion folgte wieder durch eine 35 Minuten dauernde Reperfusion. Am Ende der beiden Reperfusionen der Koronardurchströmung und Koronarwiderstand hatten sie wieder Anfangswerte angenommen. Während der Kontrolle gab es Laktat-Aufnahme, aber keine Aufnahme von Glukose, Freie Fettsäure (FFA), Triglyzeride, Glyzerol und Inosine. Während der ersten Okklusions-Periode wurde aus dem Herzen Lactat und Inosine freigemacht, es wurde Glukose und FFA aufgenommen. Am Ende der ersten Reperfusion wurde Laktat wieder aufgenommen, aber Inosine wurde noch immer an 10 von 12 Schweinen freigemacht. In der zweiten Okklusions-Periode gab es wieder Glukose und FFA-Aufnahme. Laktat und Inosine wurden freigemacht, aber die Produktion war viel kleiner als in der ersten Okklusions-Periode. Erschöpfung von myokardialen Glykogen und energiereichen Phosphaten können dafür verantwortlich sein. Nekrose könnte auch eine Rolle gespielt haben, obschon Enzym-Abgaben sehr gering waren und nur nach der zweiten Okklusions-Periode gefunden wurden. Herzfrequenz, Peripherewiderstand und ventrikulärer Füllungsdruck blieben so gut wie unverändert. Während der Experimente wurde die maximale Druckabfallgeschwindigkeit (minLVdP/dt) weniger, während Ischämie sich bei Reperfusion nicht herstellte. Veränderungen in minLVdP/dt und Herzminutenvolumen hatten einen höheren Korrelations-Koeffizient, als maxLVdP/dt und Herzminutenvolumen. Dieses Modell kann nicht für die Studien von Interventionen während myokardialer Ischämie benutzt werden.
    Notes: Summary The effect of repeated local ischemia and reperfusion on myocardial metabolism and ventricular performance was studied in 12 open-chested pigs fasted overnight. Myocardial ischemia was induced by reduction of the flow in the left anterior descending coronary artery to 40% of control during 30 min. After 35 min of reperfusion a second 30-min occlusion period was started, again followed by a 35-min reperfusion period. At the end of both reperfusion periods coronary flow and coronary resistance had returned to control values. During control there was lactate uptake, but no significant uptake of glucose, free fatty acids (FFA), triglycerides, glycerol and inosine. During the first occlusion period the heart released lactate and inosine, and used glucose and FFA. At the end of the first reperfusion period lactate uptake approached control values, but inosine was still released by 10 of the 12 animals. In the second ischemic period, glucose and FFA were again taken up. Lactate and inosine were released, but the production was much smaller than during the first occlusion period. Depletion of myocardial glycogen and high-energy phosphates could be responsible for this quantitatively different response. Necrosis may have played a role, although enzyme release was minimal and only observed after the second occlusion period. Heart rate, peripheral resistance and ventricular filling pressure were virtually unchanged throughout the course of the experiments. Maximum rate of fall of left ventricular pressure (min LVdP/dt) decreased during ischemia and did not recover during reperfusion. Changes in min LVdP/dt and cardiac output were more closely related than changes in max LVdP/dt and cardiac output. This model cannot be used for the study of interventions during myocardial ischemia in which the animal serves as its own control.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01907642
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