Radiolabeling, docking studies, in silico ADME and biological evaluation of serotonin with 125I for 5-HTRs imaging  

作　　者：Dina M.El-Sharawy Marwa S.El Refaye H.Hussien Asmaa M.AboulMagd 

机构地区：[1]Labeled Compounds Department,Hot Lab.Center,Egyptian Atomic Energy Authority(EAEA),P.O.Box 13759,Cairo,Egypt [2]Radioactive Isotopes and Generators Department,Hot Lab.Center,Egyptian Atomic Energy Authority(EAEA),P.O.Box 13759,Cairo,Egypt [3]Cyclotron Project,Nuclear Research Center,Cairo,Egypt [4]Pharmaceutical Chemistry Department,Faculty of Pharmacy,Nahda University,Beni Suef,Egypt [5]Pharmaceutics and Clinical Pharmacy Department,Faculty of Pharmacy,Nahda University,Beni Suef,Egypt

出　　处：《Nuclear Science and Techniques》2020年第8期64-71,共8页核技术（英文）

摘　　要：Serotonin is one of the significant signaling molecules used by several neural systems in the gut and brain. This study aimed to develop a novel and potent tracer for targeting, detecting, and imaging serotonin receptors(5-HTRs), which is a promising tool in the determination of the receptor’s function and relationship with the diseases related to serotonin and its receptor dysfunction. Serotonin was effectively labeled via a direct electrophilic substitutional reaction using an oxidizing agent such as iodogen with 125I in a neutral medium, and 125I-serotonin was achieved with a maximum labeling yield of 91 ± 0.63% with in vitro stability up to 24 h. Molecular modeling was conducted to signify 125I-serotonin structure and confirm that the radiolabeling process did not affect serotonin binding ability to its receptors. Biodistribution studies show that the maximum gastro intestinal tract uptake of 125I-serotonin was 17.8 ± 0.93% ID/organ after 30 min postinjection and the tracer’s ability to pass the blood–brain barrier. Thus, 125I-serotonin is a promising single photon emission computed tomography tracer in the detection of 5 HTRs.

关 键 词：SEROTONIN Electrophilic substitution Molecular modeling 5HTRs 

分 类 号：R817[医药卫生—影像医学与核医学]