Synthesis and Radiolabeling of HYNIC-GPRPILE and HYNIC-GPLGAAD Peptides with 99mTc as fibrin imaging agent
- سال انتشار: 1397
- محل انتشار: بیست و دومین همایش سالیانه پزشکی هسته ای ایران
- کد COI اختصاصی: RINMMICMED22_041
- زبان مقاله: انگلیسی
- تعداد مشاهده: 459
نویسندگان
Pharmaceutical Chemistry and Radiopharmacy Department, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
Pharmaceutical Chemistry and Radiopharmacy Department, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
Department of Chemistry, North Tehran Branch of Islamic Azad University, Tehran, Iran
Pharmaceutical Chemistry and Radiopharmacy Department, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
چکیده
Background: Today, Thrombosis is a serious risk factor for both thromboembolic disease (such as DVT, PE) and cancer. Fibrin is a major constituent of clots and is present in all types of thrombi, but absent in circulation. Fibrin is a highly sensitive and specific target for molecular imaging of thrombi. In the present study, we have developed two linear fibrin-binding peptides for thrombus imaging. Peptides were synthesized, radiolabeled with 99mTc and their stability in normal saline and human plasma and LogP were determined.Methods: HYNIC-Gly-Pro-Arg-Pro-ILe-Leu-Glu and HYNIC-Gly-Pro-Lys-Gly-Ala-Ala-Asp peptides were synthesized using a standard Fmoc strategy and radiolabeled with 99mTc. The stability of the radiolabeled peptides in human plasma and normal saline as well as partition coefficient (LogP) was determined.Results: HYNIC-GPRPILE calculated for C41H65N13O11: 915.5; found m/z = 916.5 [M + H] +. Analytical RP-HPLC: Rt = 10min; 85 % A, 15 % B., LogP=-1.83±0.31 HYNIC- GPLGAAD calculated forC31H47N11O11:749.3; found m/z=750.3 [M + H] +. Analytical RP-HPLC: Rt = 8min; 85 % A, 15 % B, LogP=-2.58±0.51 The optimal labeling conditions were 20 μg peptide, 80° C, pH 5 - 6 and incubation time 30 min. The radiochemical purity of radiolabeled peptides was more than 95%. The stability of peptides in human plasma at 37°C was 95 % after 6 h.Conclusions: The results indicate that peptides are promising agents for in vitro and in vivo studies.کلیدواژه ها
Thrombosis, HYNIC, Fibrin, 99mTc, DVTمقالات مرتبط جدید
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