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作者： SUN Xun, AN Rui, LI Shuo, HE Yong, WU Jun Department of Nuclear Medicine, Union Hospital, Huazhong University of Science and Technology,Wuhan 430022, China

To study the biological characteristics of 99mTc labeled somatostatin analogue 99mTc-HYNIC-TOCA in tumor cell and tumor model, and to discuss the possibility of diagnosing tumors with 99mTc-HYNIC-TOCA. Methods TOCA was labeled with 99mTc using HYNIC as bifunctional chelator, EDDA and tricine as coligand. The cell uptake, retention and internalization studies of 99mTc-HYNIC-TOCA were operated

关键词： somatostatin receptor imaging tumor TOCA HYNIC

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^(99m)Tc-YIGSR as a receptor Tracer in imaging the Ehrlich Ascites Tumor-bearing Mice as Compared with ^(99m)Tc-MIBI

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2007年第4期27卷 471-474页

作者：胡佳秦光明张永学安锐兰小莉 Department of Nuclear Medicine Union Hospital Tongji Medical College Huazhong University of Science and Technology Department of Nuclear Medicine Shenzhen Second People's Hospital

The validity of ^99mTc-YIGSR, a novel receptor radio-tracer, in imaging the Ehrlich ascites tumor was evaluated. YIGSR, a pentapeptide of laminin, was labeled with ^99mTc by using a bifunctional chelator S-Acetly-NH3-MAG3. The MIBI was labeled with ^99mTc by following the kit instruction. The mice of tumor group were intravenously injected 1-2 mCi of ^99mTc-YIGSR or ^99mTc-MIBI via caudal vein, immobilized and imaged under a Gamma camera. The same procedure was performed in mice of blockade group, in which the unlabeled YIGSR was previously injected to block the receptor-recognition sites, and inflammation group serving as control. The reverse-phase Sep-Pak C18 chromatogram was found to have an essentially complete conjugation between YIGSR and S-Acetly-NH3-MAG3. The conjugated YIGSR could be radio-labeled successfully with ^99mTC at room temperature and neutral pH, with a radio-labeling yield of 62%. Without the chelator S-Acetly-NH3-MAG3, the YIGSR was labeled with ^99mTc at an efficiency of 4%. The imagological study revealed obvious tumor accumulation of ^99mTc-YIGSR 15 min after the injection, and the uptake peaked after 3 h with a tumor-to-muscle ratio （T/M） of 11.36. The radio-tracer was slowly cleared up and resulted in a T/M of 3.01 at the 8th h after the injection. As for blocked group, the tumor uptake of radiotracer was significantly lower, with the highest T/M being 4.61 after 3 h and 0.89 after 8 h. The T/M was 3.72 at the 3rd h and 1.29 at the 8th h after the ^99mTc-YIGSR injection in the inflammatory group. The T/M was significantly higher in tumor group than in inflammatory group or control group （P〈0.001）. In the ^99mTc-MIBI group, the T/M was 1.40 at the 3rd h and 0.55 at the 8th h after the injection, which showed a significant difference as compared with ^99mTc-YIGSR （P〈0.001）. It is concluded that YIGSR can be successfully radiolabelled by using S-Acetly-NH3-MAG3. ^99mTc-YIGSR has many advantages in tumor imaging, such as quick and clear visual

关键词： laminin-YIGSR tumor receptor imaging radio-labeling ^99mTC S-Acetly-NH3-MAG3

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PET imaging for receptor occupancy: meditations on calculation and simplification

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The Journal of Biomedical Research 2012年第2期26卷 69-76页

作者： Yumin Zhang Gerard B.Fox Translational Sciences Global Pharmaceutical R&DAbbott LaboratoriesAbbott ParkIL 60064USA.

This invited mini-review briefly summarizes procedures and challenges of measuring receptor occupancy with positron emission tomography. Instead of describing the detailed analytic procedures of in vivo ligand-receptor imaging, the authors provide a pragmatic alJproach, along with personal perspectives, for conducting positron emission tomography imaging for receptor occupancy, and systematically elucidate the mathematics of receptor occupancy calculations in practical ways that can be understood with elementary algebra. The authors also share insights regarding positron emission tomography imaging for receptor occupancy to facilitate applications for the development of drugs targeting receptors in the central nervous system.

关键词： positron emission tomography receptor imaging receptor occupancy drug development centralnervous system

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History of the dopamine hypothesis of antipsychotic action

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World Journal of Psychiatry 2021年第7期11卷 355-364页

作者： Mary V Seeman Department of Psychiatry University of TorontoToronto M5P 3L6OntarioCanada

The dopamine hypothesis of how antipsychotic drugs exert their beneficial effect in psychotic illness has an interesting history that dates back to *** hypothesis is not to be confused with the dopamine hypothesis of schizophrenia;the aim of the latter is to explain the etiology of *** present review does not deal with schizophrenia but,rather,with the historical development of our current understanding of the dopamine-associated actions of the drugs that reduce the symptoms of *** historical review begins with the serendipitous discovery of chlorpromazine,a drug synthesized around a chemical core that initially served to produce man-made *** molecular core subsequently contributed to the chemistry of *** was with the aim of producing a superior antihistamine that chlorpromazine was synthesized;instead,it revolutionized the treatment of *** first hypothesis of how this drug worked was that it induced hypothermia,a cooling of the body that led to a tranquilization of the *** new,at the time,discoveries of the presence of chemical transmitters in the brain soon steered investigations away from a temperature-related hypothesis toward questioning how this drug,and other drugs with similar properties and effects,modulated endogenous *** a result,over the years,researchers from around the world have begun to progressively learn what antipsychotic drugs do in the brain.

关键词： Chlorpromazine Haloperidol G-Protein coupled receptors Binding assays receptor imaging High affinity states

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Feasibility on Systemic Delivery of Asialoorosomucoid Complex to Hepatic Origin Cells Mediated by Asialoglycoprotein receptor

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2005年第3期25卷 234-235,239页

作者：孙军夏劲松王玉王宇哲宗义强屈伸 Department of Biochemistry and Molecular Biology School of Basic Medical Sciences Tongji Medical CollegeHuazhong University of Science and Technology

receptor mediated gene delivery is a new gene transfer strategy. Asialoglycoprotein receptor (ASGP-R), the receptor of asialoorosomucoid (Asor), is specially expressed on the surface of hepatocyte. In this paper, the nuclide 131I was combined with Asor to form a kind of soluble nuclide-protein complex, which can be specifically endocytosed into hepatocyte by ASGP-R. After intravenous injection of the complex into experimental animals, the deposition of Asor in vivo and the targeting quality of hepatocyte was detected by ECT. This research testified the feasibility of targeting Asor complex delivery to hepatocyte mediated by ASGP-R in vivo, and provided foundation for the genetic diagnosis and gene therapy of hepatic cell-related diseases.

关键词： asialoglycoprotein receptor receptor imaging vp3 gene hepatocellular carcinoma

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