Synthesis and Preliminary Evaluation of a New <sup>99m</sup>Tc Labeled Substance P Analogue as a Potential Tumor Imaging Agent
| Author | Saeed Mozaffari | en |
| Author | Mostafa Erfani | en |
| Author | Davood Beiki | en |
| Author | Fariba Johari Daha | en |
| Author | Farzad Kobarfard | en |
| Author | Saeed Balalaie | en |
| Author | Babak Fallahi | en |
| Issued Date | 2015-01-31 | en |
| Abstract | Neurokinin 1 receptors (NK1R) are overexpressed on several types of important human cancer cells. Substance P (SP) is the most specific endogenous ligand known for NK1Rs. Accordingly,a new SP analogue was synthesized and evaluated for detection of NK1R positive tumors.[6-hydrazinopyridine-3-carboxylic acid (HYNIC)-Tyr8-Met(O)11-SP] was synthesized and radiolabeled with 99mTc using ethylenediamine-N,N'-diacetic acid (EDDA)and Tricine as coligands. Common physicochemical properties of radioconjugate were studied and in-vitro cell line biological tests were accomplished to determine the receptor mediated characteristics. In-vivo biodistribution in normal and tumor bearingnude mice was also assessed. The cold peptide was prepared in high purity (>99%) and radiolabeled with 99mTc at high specific activities (84-112GBq/µmol) with an acceptable labeling yield (>95%). The radioconjugate was stable in-vitro in the presence of human serum and showed 44% protein binding to human serumalbumin. In-vitro cell line studies on U373MG cells showed an acceptable uptake up to 4.91 ± 0.22% with the ratio of 60.21 ± 1.19% for its specific fraction and increasing specific internalization during 4 h. Receptor binding assays on U373MG cells indicated a mean Kd of 2.46 ± 0.43 nM and Bmax of 128925 ± 8145 sites/cell. In-vivo investigations determined the specific tumor uptake in 3.36 percent of injected dose per gram (%ID/g) for U373MG cells and noticeable accumulations of activity in the intestines and lung. Predominant renal excretion pathway was demonstrated. | en |
| DOI | https://doi.org/10.22037/ijpr.2015.1603 | en |
| URI | https://brieflands.com/journals/ijpr/articles/125290 | en |
| Keyword | NK<sub>1</sub>R | en |
| Keyword | Substance P analogue | en |
| Keyword | <sup> 99m</sup>Tc | en |
| Keyword | HYNIC | en |
| Keyword | U373MG cells | en |
| Publisher | Brieflands | en |
| Title | Synthesis and Preliminary Evaluation of a New <sup>99m</sup>Tc Labeled Substance P Analogue as a Potential Tumor Imaging Agent | en |
| Type | Original Article | en |
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