[1]潘明志.α受体及α受体显像[J].国际放射医学核医学杂志,2000,24(2):49-51.
　PAN Ming-zhi.Sigma receptor and sigma receptor imaging[J].International Journal of Radiation Medicine and Nuclear Medicine,2000,24(2):49-51.
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《国际放射医学核医学杂志》[ISSN:1673-4114/CN:12-1381/R]

卷:
24
期数:
2000年第2期
页码:
49-51
栏目:
综述
出版日期:
1900-01-01

文章信息/Info

Title:
Sigma receptor and sigma receptor imaging
作者:
潘明志
610041 四川 成都, 华西医科大学第一附属医院核医学科
Author(s):
PAN Ming-zhi
Department of Nuclear Medicine, The First Affiliated Hospital, WCUMS, Sichuan Chengdu 610041, China
关键词:
σ受体; 放射性配体; σ受体阳性肿瘤; 肿瘤受体显像
Keywords:
sigma receptor; radio-ligand; sigma receptor-positive tumors; tumor receptor imaging
分类号:
R817.4
摘要:
近年研究发现,α受体是一类非阿片1非多巴胺受体,其结构,生理与生化功能和药理学作用尚不十分清楚。许多肿瘤如恶性黑色素瘤、乳癌前列腺癌、非小细胞肺癌、结肠癌肾癌以及来自神经组织的肿瘤均含有高密度的α受体。因此,研制具有高亲和性,高选择性的α受体配体已成为分子核医学的热点之一。这不仅可以对α受体的生化和生理功能以及药理作用民可作为α受体阳性肿瘤的显像剂甚至治疗剂。
Abstract:
Recent studies indicate that sigma receptors are a class of non-opiate, non-dopaminergic proteins. The structure, physiological and biochemical functions, and the pharmacological significance of sigma receptors are not completely understood. A wide variety of human tumors, including malignant melanoma, non-small cell lung carcinoma,tumors of breast, prostate, colon, kidney, and neural origin contain a high density of sigma receptors. Therefore, the development of high affinity sigma receptor-specific radio-ligands has become an attractive target.The radio-ligands not only can be used to study the physiological and biochemical functions and pharmacology of sigma receptors, but also can be potentially used to image and treat sigma receptor-positive tumors.

参考文献/References:

[1] John CS, Vilner BJ,GuldeM E, et al.Synthesis and pharmacological characterization of 4-[125I]-N-(n-Benzylpiperidin-4yl)-4-iodobenzamide:A high affinity σ receptor ligand for potential imaging of breast cancer[J]. Cancer Res, 1995,55:3022~3027.
[2] Mach RH,Smith CR,Whirrett BR,et al.σ2 receptor as potential biom arkers of proliferation in breast cancer[J]. Cancer Res, 1997,57:156~161.
[3] John CS, Lim BB, Vilner BJ, et al.Substituted halogenated ary lsulfonamides:A new class of σ receptor binding tumorimaging agents[J]. J Med Chem,1998, 41:2445~2450.
[4] Seth P, Fei Y J,Huang FH, et al.Cloning and functional characterization of a sigmareceptor from rat brain[J]. JN eurochem,1998, 70:922~931.
[5] Vilder BJ,John CS and Bowen WD.Sigma-1 and Sigma-2 receptor are expressed in a wide variety of human and rodent tumor cell lines[J]. Cancer Res, 1995, 15:408~413.
[6] John CS,Gulden ME,Li JH,et al.Synthesis,in vitro binding, and tissue distribution of radio iodinated 2-[125I]N-(N-benzylpiperidin-4-yl)-2-iodobenzamide,2-[125I] BP:A potential marker for human prostate tumors[J]. Nucl Med Biol,1998,25:189~194.
[7] Watethouse RN, Mardon K and Brien JC. Synthesis and preliminary evaluation of [123I]1-(4-Cyanobenzl)-4-[[(trans-iodopropen-2-yl)oxy]-methyl]piperidine:A novel high affininty sigm a receptor radioligand for SPECT[J]. Nucl Med Biol,1997, 24:45~51.
[8] John CS,Bow en WD,Fisher SJ,et al.Synthesis,in vitro pharmacolog ic characterization, and preclinical evaluation of N-[2-(1’-piperdinyl)ethy l]-3-[125I] iodo-4-methoxybenza mide (P[125I]MBA) for imaging breast cancer[J]. Nucl Med Biol,1999, 26:377~382.
[9] John CS, Lim BB, Geyer BC, et al.99Tcm-labeled σ-receptor-binding complex:Synthesis,characterization, and specific binding to human ductal breast carcinoma (T47D) cells[J]. Bioconjugate Chem, 1997,8:304~309.

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备注/Memo

备注/Memo:
收稿日期:2000-03-14。
作者简介:潘明志(1955-),男,重庆市人,华西医科大学附属第一医院核医学科讲师,硕士,主要从事临床核医学显像研究。
更新日期/Last Update: 1900-01-01