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化学进展 2008, Vol. 20 Issue (06): 869-877 前一篇   后一篇

• 综述与评论 •

5-羟色胺转运蛋白显像剂的研究进展*

郭运行 刘伯里**   

  1. （放射性药物教育部重点实验室 北京师范大学化学学院 北京 100875）
  • 收稿日期:2007-07-16 修回日期:2007-07-24 出版日期:2008-06-24 发布日期:2008-06-24
  • 通讯作者: 刘伯里
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Advances in the Serotonin Transporter Imaging Agents

Guo Yunxing; Liu Boli**

  

  1. (Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China)
  • Received:2007-07-16 Revised:2007-07-24 Online:2008-06-24 Published:2008-06-24
  • Contact: Boli Liu
中枢神经系统5-羟色胺神经元功能异常，特别是突触前膜的5-羟色胺转运蛋白（SERT）密度的变化常导致复杂的精神紊乱疾病。SERT的正电子发射断层（PET）和单光子发射断层（SPECT）活体显像剂有助于研究该系统的变化与精神紊乱疾病的关系，以及精神紊乱病人疗效的监测。本文综述了近年来SERT显像剂的最新研究进展，并指出了今后该类显像剂的发展趋势。
关键词： 5-羟色胺转运蛋白, 显像剂, 精神紊乱
Alterations of serotonergic neuronal function, particularly changes of density in the presynaptically located serotonin transporter (SERT) occur in psychiatric disorders. Imaging of SERT with positron emission tomography (PET) and single photon emission computed tomography (SPECT) in humans can provide an important tool for understanding the relationship of psychiatric disorders and the alterations in SERT density, as well as to monitor the treatment of patients. This review discusses the recent development of SERT imaging agents and the research trends for the future.
Key words: serotonin transporter, imaging agents, psychiatric disorders

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[ 1 ] Blakely R D , Berson H E , Fremeau J , et al . Nature , 1991 , 353(6348) : 66 —70
[ 2 ] Miller G M, Yatin S M, de La Garza Ⅱ R , et al . Mol . Brain Res. , 2001 , 87(1) : 124 —143
[ 3 ] Maron E , Kuikka J T , Shlik J , et al . Psychiatry Res. , 2004 ,132(2) : 173 —181
[ 4 ] Stengler-Wenzke K, Muller U , Angermeyer M C , et al . Eur.Arch. Psychiatry Clin. Neurosci . , 2004 , 254 : 252 —255
[ 5 ] Ichimiya T , Suhara T , Sudo Y, et al . Biol . Psychiatry , 2002 , 51(9) : 715 —722
[ 6 ] Malison R T , Price L H , Berman R , et al . Biol . Psychiatry ,1998 , 44(11) : 1090 —1098
[ 7 ] Thomas A J , Hendriksen M, Piggott M, et al . Neuropathol .Appl . Neurobiol . , 2006 , 32(3) : 296 —303
[ 8 ] Kuikka J T , Tammela L , Karhunen L , et al .Psychopharmacology , 2001 , 155 (3) : 310 —314
[ 9 ] Hesse S , Barthel H , Schwarz J , et al . Neurosci . Biobehav.Rev. , 2004 , 28(6) : 547 —563
[10] McCann U D , Szabo Z , Seckin E , et al .Neuropsychopharmacology , 2005 , 30(9) : 1741 —1750
[11] Suehiro M, Scheffel U , Dannals R F , et al . J . Nucl . Med. ,1993 , 34(1) : 120 —127
[12] Suehiro M, Wilson A A , Scheffel U , et al . Int . J . Rad. Appl .Instrum. B , 1991 , 18(7) : 791 —796
[13] Mathis C A , Gerdes J M, Enas J D , et al . J . Nucl . Med. ,1991 , 32 (suppl . ) : 965 —965
[14] Kilboum M R. J . Nucl . Med. , 1988 , 29(suppl . ) : 932 —932
[15] Mukherjee J , Das M K, Yang Z Y, et al . Nucl . Med. Biol . ,1998 , 25(7) : 605 —610
[16] Dannals R F , Ravert H T , Wilson A A , et al . Int . J . Rad.Appl . Instrum. A , 1990 , 41(6) : 541 —543
[17] Suehiro M, Ravert H T , Dannals R F , et al . J . Label . Compd.Radiopharm. , 1992 , 31(10) : 841 —848
[18] Suehiro M, Scheffel U , Ravert H T , et al . Life Sci . , 1993 , 53(11) : 883 —892
[19] Suehiro M, Scheffel U , Dannals R F , et al . J . Nucl . Med. ,1993 , 34(1) : 120 —127
[20] Szabo Z , Scheffel U , Suehiro M, et al . J . Cereb. Blood Flow Metab. , 1995 , 15(5) : 798 —805
[21] Suehiro M, Greenberg J H , Shiue C Y, et al . Nucl . Med. Biol . ,1996 , 23(4) : 407 —412
[22] Zessin J , Eskola O , Brust P , et al . Nucl . Med. Biol . , 2001 , 28(7) : 857 —863
[23] Neumeyer J L , Wang S Y, Milius R A , et al . J . Med. Chem. ,1991 , 34(10) : 3144 —3146
[24] Laruelle M, Baldwin R M, Malison R T , et al . Synapse , 1993 ,13(4) : 295 —309
[25] Brucke T , Kornhuber J , Angelberger P , et al . J . Neural .Transm. Gen. Sect . , 1993 , 94(2) : 137 —146
[26] de Win M M, Habraken J B , Reneman L , et al .Neuropsychopharmacology , 2005 , 30(5) : 996 —1005
[27] Bergstrêm K A , Halldin C , Hall H , et al . Eur. J . Nucl . Med. ,1997 , 24(6) : 596 —601
[28] Reneman L , Booij J , Lavalaye J , et al . Synapse , 1999 , 34(1) :77 —80
[29] Helfenbein J , Sandell J , Halldin C , et al . Nucl . Med. Biol . ,1999 , 26(5) : 491 —499
[30] Goodman M M, Chen P , Plisson C , et al . J . Med. Chem. ,2003 , 46(6) : 925 —935
[31] Plisson C , McConathy J , Martarello L , et al . J . Med. Chem. ,2004 , 47(5) : 1122 —1135
[32] Stehouwer J S , Plisson C , Jarkas N , et al . J . Med. Chem. ,2005 , 48(22) : 7080 —7083
[33] Jensen S B , Bender D , Smith D F , et al . J . Label . Compd.Radiopharm. , 2002 , 45(3) : 181 —189
[34] Jensen S B , Smith D F , Bender D , et al . Synapse , 2003 , 49(3) : 170 —177
[35] Audrain H , Bender D , Cumming P , et al . J . Label . Compd.Radiopharm. , 2003 , 46(9) : 873 —882
[36] Quinlivan M, Mattner F , Papazian V , et al . Nucl . Med. Biol . ,2003 , 30(7) : 741 —746
[37] Hashimoto K, Goromaru T. Radioisotopes , 1990 , 39 (4) : 168 —169
[38] Hashimoto K, Goromaru T. J . Pharmacol . Exp. Ther. , 1990 ,255(1) : 146 —153
[39] Mathis C A , Taylor S E , Biegon A , et al . Brain Res. , 1993 ,619(1/2) : 229 —235
[40] Biegon A , Mathis C A , Hanrahan SM, et al . Brain Res. , 1993 ,619(1/2) : 236 —246
[41] Jagust W J , Eberling J L , Roberts J A , et al . Eur. J .Pharmacol . , 1993 , 242 (2) : 189 —193
[42] Lundkvist C , Loc’h C , Halldin C , et al . Nucl . Med. Biol . ,1999 , 26(5) : 501 —507
[43] Sandell J , Halldin C , Sovago J , et al . Nucl . Med. Biol . , 2002 ,29(6) : 651 —656
[44] Karramkam M, DolléF , Valette H , et al . Bioorg. Med. Chem. ,2002 , 10(8) : 2611 —2623
[45] Lee B S , Chu S , Lee K C , et al . Bioorg. Med. Chem. , 2003 ,11(23) : 4949 —4958
[46] In M Y, Chi D Y, Choi S J , et al . Bull . Korean Chem. Soc. ,2002 , 23(10) : 1439 —1444
[47] Gerdes J M, O’Neil J P , Bolstad D B , et al . NeuroImage , 2004 ,22(Suppl . 2) : T147 —T147
[48] Ferris R M, BrieaddyL , Mehta N , et al . J . Pharm. Pharmacol . ,1995 , 47(9) : 775 —781
[49] Oya S , Kung M P , Acton P D , et al . J . Med. Chem. , 1999 , 42(3) : 333 —335
[50] Kung M P , Hou C , Oya S , et al . Eur. J . Nucl . Med. , 1999 ,26(8) : 844 —853
[51] Acton P D , Kung M P , Mu M, et al . Eur. J . Nucl . Med. ,1999 , 26(8) : 854 —861
[52] Zhuang Z , Choi S , Hou C , et al . Nucl . Med. Biol . , 2000 , 27(2) : 169 —175
[53] Acton P D , Mu M, Plossl K, et al . Eur. J . Nucl . Med. , 1999 ,26(10) : 1359 —1362
[54] Oya S , Choi S R , Hou C , et al . Nucl . Med. Biol . , 2000 , 27(3) : 249 —254
[55] Kauppinen T A , Bergstrêm K A , Heikman P , et al . Eur. J .Nucl . Med. Mol . Imaging , 2003 , 30(1) : 132 —136
[56] Catafau A M, Pérez V , Penengo M M, et al . J . Nucl . Med. ,2005 , 46(8) : 1301 —1309
[57] Newberg A B , Plossl K, Mozley P D , et al . J . Nucl . Med. ,2004 , 45(5) : 834 —841
[58] Newberg A B , Amsterdam J D , Wintering N , et al . J . Nucl .Med. , 2005 , 46(6) : 973 —977
[59] Kung H F , Newman S , Choi S R , et al . J . Med. Chem. , 2004 ,47(21) : 5258 —5264
[60] 蒋泉福(Jiang Q F) , 陆春雄(Lu C X) , 吴春英(Wu C Y) 等.核技术(Nuclear Techniques) , 2005 , 28(10) : 766 —770
[61] Oya S , Choi S R , Kung M P , et al . Nucl . Med. Biol . , 2007 ,34(2) : 129 —139
[62] Guo Y H , Chen X J , Jia H M, et al . J . Label . Compd.Radiopharm. , 2007 , 50 : S328 —S328
[63] Wilson A A , Houle S. J . Label . Compd. Radiopharm. , 1999 ,42(13) : 1277 —1288
[64] Wilson A A , Ginovart N , Schmidt M, et al . J . Med. Chem. ,2000 , 43(16) : 3103 —3110
[65] Houle S , Ginovart N , Hussey D , et al . Eur. J . Nucl . Med. ,2000 , 27(11) : 1719 —1722
[66] Huang Y, Hwang D R , Narendran R , et al . J . Cereb. Blood Flow Metab. , 2002 , 22(11) : 1377 —1398
[67] Ginovart N , Wilson A A , Meyer J H , et al . J . Cereb. Blood Flow Metab. , 2001 , 21(11) : 1342 —1353
[68] Wilson A A , Ginovart N , Hussey D , et al . Nucl . Med. Biol . ,2002 , 29(5) : 509 —515
[69] Tarkiainen J , Vercouillie J , Emond P , et al . J . Label . Compd.Radiopharm. , 2001 , 44(14) : 1013 —1023
[70] Huang Y, Hwang D R , Zhu Z , Bae S A , et al . Nucl . Med.Biol . , 2002 , 29(7) : 741 —751
[71] Huang Y, Narendran R , Bae S A , et al . Nucl . Med. Biol . ,2004 , 31(6) : 727 —738
[72] Jarkas N , McConathy J , Votaw J R , et al . Nucl . Med. Biol . ,2005 , 32(1) : 75 —86
[73] Zhu Z , Guo N , Narendran R , Erritzoe D , et al . Nucl . Med.Biol . , 2004 , 31(8) : 983 —994
[74] Huang Y, Hwang D R , Bae S A , et al . Nucl . Med. Biol . ,2004 , 31(5) : 543 —556
[75] Jarkas N , Votaw J R , Voll R J , et al . Nucl . Med. Biol . , 2005 ,32(3) : 211 —224
[76] Zessin J , Deuther-Conrad W, Kretzschmar M, et al . Nucl . Med.Biol . , 2006 , 33(1) : 53 —63
[77] Halldin C , Lundberg J , SóvágóJ , et al . Synapse , 2005 , 58(3) :173 —183
[78] Lundberg J , Odano I , Olsson H , et al . J . Nucl . Med. , 2005 ,46(9) : 1505 —1515
[79] Tarkiainen J , Vercoulillie J , Guilloteau D , et al . Label . Compd.Radiopharm. , 2001 , 44(suppl) : 193 —195
[80] Laruelle M, Slifstein M, Huang Y. Mol . Imaging Biol . , 2003 , 5(6) : 363 —375
[81] Vercouillie J , Mavel S , Galineau L , et al . Bioorg. Med. Chem.Lett . , 2006 , 16(5) : 1297 —1300
[82] Choi S R , Hou C , Oya S , et al . Synapse , 2000 , 38(4) : 403 —412
[83] KungM P , Hou C , Oya S , Mu M, et al . J . Label . Compd.Radiopharm. , 2001 , 44(suppl . ) : 15 —17
[84] Oya S , Choi S R , Coenen H , et al . J . Med. Chem. , 2002 , 45(21) : 4716 —4723
[85] Shiue G G, Fang P , Shiue C Y. Appl . Radiat . Isot . , 2003 , 58(2) : 183 —191
[86] Shiue G G, Choi S R , Fang P , et al . J . Nucl . Med. , 2003 , 44(12) : 1890 —1897
[87] Fang P , Shiue G G, Shiue C Y, et al . Appl . Radiat . Isot . ,2004 , 61(6) : 1247 —1254
[88] Huang Y, Bae S A , Zhu Z , et al . J . Med. Chem. , 2005 , 48(7) : 2559 —2570
[89] Oya S , Choi S R , Parhi A K, et al . J . Med. Chem. , 2007 , 50 :6673 —6684
[90] Oya S , Choi S R , Kung H F. 226th ACS National Meeting(Division of Medicinal Chemistry) , 2003 , 178 —178
[91] Eersels J L , Klok R P , Verbeek J , et al . Nucl . Med. Biol . ,2004 , 31(5) : 563 —569
[92] Perrone R , Berardi F , Colabufo N A , et al . J . Pharm.Pharmacol . , 2005 , 57(10) : 1319 —1327
[93] Meegalla S K, Plossl K, Kung M P , et al . J . Med. Chem. ,1997 , 40(1) : 9 —17
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