| چکیده انگلیسی مقاله |
Introduction: Bombesin (BN), a 14-amino acid neuropeptide, shows high affinity for the human GRP (gastrin releasing peptide) receptors, which are overexpressed by a variety of cancers, including prostate, breast, pancreas, gastrointestinal, and small cell lung cancer. Aim was to prepare [6-hydrazinopyridine-3-carboxylic acid (HYNIC0), D-Tyr6, D-Trp8] - BN [6-14] NH2 that could be easily labeled with 99mTc and evaluation of its potential as an imaging agent. Methods: Synthesis of the peptide amide was carried out onto Rink Amide MBHA (4-Methylbenzhydrylamine) resin. A bifunctional chelating agent (BFCA) was attached to the N terminal peptide in solid-phase. 99mTc labeling was performed by addition of sodium pertechnetate to solution that include [HYNIC0, D-Tyr6, D-Trp8] Bombesin [6-14] NH2, tricine, ethylenediamine-N,N′-diacetic acid (EDDA) and SnCl2. Radiochemical evaluation was carried out by reverse phase high-performance liquid chromatography (HPLC) and instant thin layer chromatography (ITLC). In-vitro internalization was tested using human prostate cancer cells (PC-3) with blocked and non-blocked receptors. Biodistribution was determined in rats. Results:[99mTc/tricine/EDDA-HYNIC0, D-Tyr6, D-Trp8] bombesin [6-14] NH2 was obtained with radiochemical purities >98%. Results of in-vitro studies demonstrated a high stability in serum and suitable internalization. Biodistribution data showed a rapid blood clearance, with renal excretion and specific binding towards GRP receptor-positive tissues such as pancreas. Conclusion: In this study, labeling of this novel conjugate with 99mTc easily was performed using coligand. The prepared 99mTc-HYNIC-BN conjugate has promising characteristics for the diagnosis of malignant tumors. |
| کلیدواژههای انگلیسی مقاله |
Iran, meta-analysis, trend of infertilityGated myocardial perfusion SPECT, Quantification, segmental scoring, Meckel’s scan, Meckel’s diverticulum, Gastrointestinal bleeding, Technetium Pertechnetate scintigraphy, Thiosemicarbazone, 191Os, Radiolabeling, Biodistribution, RBBB, Myocardial perfusion, Gated SPECT, Coronary artery disease, Effective dose, Nuclear medicine procedures, Collective effective dose, Tc99m MIBI parathyroid scintigraphy, Myocardium perfusion gated SPECT, Parathyroid adenoma, Skeletal scintigraphy, Fluid restriction, Tc-99m MDP, Image quality, Bone to soft tissue ratio, Radiology, Nuclear medicine, Medical imaging, Bibliometric study, Iran, Hyperthyroidism, Radioactive iodine, Sexual hormones, Semen analysis, Attenuation correction, Artifact, Color intensity, SPECT, Thyroid, I-131, Absorbed ratio, Monte-Carlo, Absorbed dose, MCNP-4A, Carcinoid Tumor, Liver metastases, ¹³¹I-MIBG scintigraphy, Quality Control, PET, 82mRb, 82Kr, Myocardial perfusion, Drug delivery systems, Gamma-scintigraphy, Neutron activation, Pharmacoscintigraphy, Post stroke dementia, Cerebral perfusion SPECT, ECD, 99mTc-DTPA, Renography, Deconvolution, Renal transit time parameters, Nuclear medicine, PET tracer, Gallium, Copper, Tc-94m, Minimally invasive radio-guided surgery, Hyperparathyroidism, Tc-99m sestamibi, Parathyroid
adenoma, Parathyroid hyperplasia, Bombesin, 99mTc, Tumor, HYNIC, |
