دورية أكاديمية
Relative uptake, metabolism, and beta-receptor binding of (1R,2S)-4-(18)F-fluorometaraminol and (123)I-MIBG in normotensive and spontaneously hypertensive rats.
| العنوان: | Relative uptake, metabolism, and beta-receptor binding of (1R,2S)-4-(18)F-fluorometaraminol and (123)I-MIBG in normotensive and spontaneously hypertensive rats. |
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| المؤلفون: | Pissarek M; Institut für Nuklearchemie Forschungszentrum Jülich, Jülich, Germany. m.pissarek@fz-juelich.de, Ermert J, Oesterreich G, Bier D, Coenen HH |
| المصدر: | Journal of nuclear medicine : official publication, Society of Nuclear Medicine [J Nucl Med] 2002 Mar; Vol. 43 (3), pp. 366-73. |
| نوع المنشور: | Comparative Study; Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Society of Nuclear Medicine Country of Publication: United States NLM ID: 0217410 Publication Model: Print Cited Medium: Print ISSN: 0161-5505 (Print) Linking ISSN: 01615505 NLM ISO Abbreviation: J Nucl Med Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Reston, VA : Society of Nuclear Medicine Original Publication: [Chicago, Ill.] : S.N. Turiel & Assoc. |
| مواضيع طبية MeSH: | 3-Iodobenzylguanidine*/pharmacokinetics , Metaraminol*/analogs & derivatives , Metaraminol*/pharmacokinetics , Radiopharmaceuticals*/pharmacokinetics, Heart/*diagnostic imaging , Hypertension/*diagnostic imaging , Receptors, Adrenergic, beta/*metabolism, Adrenergic beta-Antagonists/metabolism ; Animals ; Autoradiography ; Cardiomyopathies/diagnostic imaging ; Hypertension/metabolism ; Iodine Radioisotopes/pharmacokinetics ; Iodocyanopindolol/pharmacokinetics ; Liver/metabolism ; Male ; Myocardium/metabolism ; Propranolol/metabolism ; Rats ; Rats, Inbred SHR ; Rats, Inbred WKY ; Spleen/metabolism ; Tomography, Emission-Computed ; Tomography, Emission-Computed, Single-Photon |
| مستخلص: | Unlabelled: The objective of the study was to compare relative uptake, metabolism, and beta-receptor affinity of the new positron-emitting uptake-1 tracer (1R,2S)-4-(18)F-fluorometaraminol (4-FM) with those of the SPECT pharmaceutical meta-(123)I-iodobenzylguanidine (MIBG) in Wistar Kyoto (WKY) rats and spontaneously hypertensive (SHR) rats. Methods: No-carrier-added 4-(18)F-FM was applied to SHR and WKY rats in vivo and to retrogradely perfused hearts in vitro. Cardiac and extracardiac distribution was assessed, and metabolite formation was determined by thin-layer chromatography. The in vivo experiments were repeated with no-carrier-added (123)I-MIBG. By means of autoradiography, the beta-receptor affinity of 4-FM was compared with that of MIBG and propranolol (10 micromol/L) through displacement of (125)I-iodocyanopindolol (1.5 pmol/L) in slices of heart and spleen. Results: Cardiomyopathic hearts showed heterogeneous 4-(18)F-FM uptake with gradients up to 3.6 in vivo and in vitro between different regions of the heart. Control hearts showed such gradients in 4-(18)F-FM uptake only in vitro. (123)I-MIBG exhibited a less heterogeneous in vivo distribution in SHR hearts. Extracardiac differences between WKY and SHR were found for uptake of 4-(18)F-FM in the spleen (63.3% plus minus 4% vs. 38.8% plus minus 5.7% of cardiac activity) and for renal uptake of (123)I-MIBG (373% plus minus 27% vs. 81.4% plus minus 17% of cardiac activity). Metabolites of 4-(18)F-FM were found only in the liver and those of (123)I-MIBG were found in the liver and kidney with a nearly equal relative fraction in both types of animals of about 20%, 60%, and 30%, respectively. 4-FM suppressed cardiac-specific beta-receptor binding of (125)I-iodocyanopindolol in heart and spleen of both types of animals significantly, whereas MIBG had almost no effect. Conclusion: The more heterogeneous cardiac distribution of 4-(18)F-FM suggests that it reflects alterations in uptake-1 better than (123)I-MIBG in addition to the possibility of quantification and higher spatial resolution by PET compared with SPECT. Altered biotransformation in cardiomyopathic diseases may also impair the evaluation of (123)I-MIBG-SPECT data. The beta-receptor binding of 4-(18)F-FM must be further elucidated. |
| المشرفين على المادة: | 0 (4-fluorometaraminol) 0 (Adrenergic beta-Antagonists) 0 (Iodine Radioisotopes) 0 (Radiopharmaceuticals) 0 (Receptors, Adrenergic, beta) 35MRW7B4AD (3-Iodobenzylguanidine) 818U2PZ2EH (Metaraminol) 83498-72-0 (Iodocyanopindolol) 9Y8NXQ24VQ (Propranolol) |
| تواريخ الأحداث: | Date Created: 20020309 Date Completed: 20020405 Latest Revision: 20161124 |
| رمز التحديث: | 20231215 |
| PMID: | 11884497 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 0161-5505 |
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