title: Labeling and evaluation of (99m) Tc-tricarbonyl-meloxicam as a preferential COX-2 inhibitor for inflammation imaging.
abstract: Imaging of inflammation has an important role in dissolving problems in diagnosis and therapy of patients with inflammatory disorders. In this study meloxican as a nonsteroidal anti-inflammatory drug (NSAID) has been labeled with thechnetium-99m-tricarbonyl core ([(99m) Tc (CO)3 (H2 O)3 ](+) ) in order to evaluate its feasibility as an inflammation imaging agent for in vivo use. (99m) Tc-tricabonyl labeling of meloxicam was performed by its incubation with prepared precursor (99m) Tc-tricabonyl and heating in a boiling water bath for 30 min while various range of pH (1-9) was adjusted. The stability of (99m) Tc-tricarbonyl-Meloxicam was checked in human serum at 37 °C, and biodistribution was studied in mice. Labeling yield of 98.1 ± 0.4% was obtained corresponding to a specific activity of 0.14 GBq/µmol. The radioconjugate showed good stability in human serum. Our main achievement was high accumulation of (99m) Tc-tricarbonyl-Meloxicam in the inflammated muscle in mice (T/NT = 3.90 at 4 h post injection) which may diagnostically be beneficial for distinguish sites of inflammation.
authors.affiliation: Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box: 14395-836,, Tehran, Iran.
authors.forename: Mostafa
authors.initials: M
authors.lastname: Erfani
authors.affiliation: School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, P.O. Box: 61357-33184, Ahvaz, Iran.
authors.forename: Somayeh
authors.initials: S
authors.lastname: Sharifzadeh
authors.affiliation: School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, P.O. Box: 61357-33184, Ahvaz, Iran.
authors.forename: Alireza
authors.initials: A
authors.lastname: Doroudi
authors.affiliation: Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box: 14395-836,, Tehran, Iran.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Shafiei
mesh_terms: D000818:Animals; D001692:Biological Transport; D052246:Cyclooxygenase 2 Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D006801:Humans; D007249:Inflammation / Q000000981:diagnostic imaging; D007553:Isotope Labeling; D000077239:Meloxicam; D051379:Mice; D009132:Muscles / Q000000981:diagnostic imaging; D015609:Organotechnetium Compounds / Q000737:chemistry*; D011877:Radionuclide Imaging / Q000379:methods*; D013843:Thiazines / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D013844:Thiazoles / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D015609:Organotechnetium Compounds; D013843:Thiazines; D013844:Thiazoles; C000624966:technetium 99m tricarbonyl-meloxicam; D000077239:Meloxicam
keywords: 99mTc-tricarbonyl; Meloxicam; imaging; inflammation