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Information Journal Paper

Title

Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent

Pages

  97-110

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. Invivo 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/μ mol) 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. Invitro 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. Therefore, this new radiolabeled peptide could be a promising radiotracer for detection of NK1R positive primary or secondary tumors.

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    APA: Copy

    MOZAFFARI, SAEED, ERFANI, MOSTAFA, BEIKI, DAVOOD, JOHARI DAHA, FARIBA, KOBARFARD, FARZAD, BALALAIE, SAEED, & FALLAHI, BABAK. (2015). Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 14(1), 97-110. SID. https://sid.ir/paper/288513/en

    Vancouver: Copy

    MOZAFFARI SAEED, ERFANI MOSTAFA, BEIKI DAVOOD, JOHARI DAHA FARIBA, KOBARFARD FARZAD, BALALAIE SAEED, FALLAHI BABAK. Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2015;14(1):97-110. Available from: https://sid.ir/paper/288513/en

    IEEE: Copy

    SAEED MOZAFFARI, MOSTAFA ERFANI, DAVOOD BEIKI, FARIBA JOHARI DAHA, FARZAD KOBARFARD, SAEED BALALAIE, and BABAK FALLAHI, “Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 14, no. 1, pp. 97–110, 2015, [Online]. Available: https://sid.ir/paper/288513/en

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