Synthesis, radiolabeling and baboon SPECT imaging of 2β-carbomethoxy-3β-(3′-[123I]iodophenyl)tropane ([123I]YP256) as a serotonin transporter radiotracer

Bois, Frederic; Baldwin, Ronald M.; Amici, Louis; Al-Tikriti, Mohammed S.; Kula, Nora; Baldessarini, Ross; Innis, Robert B.; Staley, Julie K.; Tamagnan, Gilles D.

doi:10.1016/j.nucmedbio.2007.09.002

« Previous Next »Nuclear Medicine and Biology
Volume 35, Issue 1 , Pages 53-59, January 2008

Synthesis, radiolabeling and baboon SPECT imaging of 2β-carbomethoxy-3β-(3′-[¹²³I]iodophenyl)tropane ([¹²³I]YP256) as a serotonin transporter radiotracer

Frederic Bois
- Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA
Ronald M. Baldwin
- Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA
Louis Amici
- Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA
Mohammed S. Al-Tikriti
- Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA
Nora Kula
- Department of Psychiatry and Neuroscience Program, Harvard Medical School, Mailman Research Center McLean Division of Massachusetts General Hospital, Belmont, MA 02478, USA
Ross Baldessarini
- Department of Psychiatry and Neuroscience Program, Harvard Medical School, Mailman Research Center McLean Division of Massachusetts General Hospital, Belmont, MA 02478, USA
Robert B. Innis
- Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA
Julie K. Staley
- Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA
Gilles D. Tamagnan
- Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA
- Institute for Neurodegenerative Disorders, New Haven, CT 06510, USA
- Corresponding author. Tel.: +1 203 401 4309; fax: +1 203 789 2119.

Received 18 May 2006; received in revised form 5 September 2007; accepted 7 September 2007.

Abstract

To develop a potential SPECT probe to evaluate the integrity of the serotoninergic system (5-HTT) whose dysfunction is linked to several disease conditions such as Parkinson's disease, Alzheimer's disease and depression, we report the synthesis, radiolabeling and in vivo baboon imaging of 2β-carbomethoxy-3β-(3′-[¹²³I]iodophenyl) tropane (YP256, 6). The radiolabeling was performed by iododestannylation using sodium [¹²³I]iodide and peracetic acid. Although the ligand displayed high selectivity for 5-HTT over dopamine transporter in vitro, SPECT imaging in baboons did not reveal selective 5-HTT accumulation in brain in vivo.

Keywords: Radiolabeling, Serotonin transporter, Monkey study, Brain imaging, SPECT