Simple, Rapid and Reliable Preparation of [11C]-(+)-a-DTBZ of High Quality for Routine Applications 英文参考文献.docVIP

Molecules 2012, 17, 6697-6704; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Simple, Rapid and Reliable Preparation of [11C]-(+)-?-DTBZ of High Quality for Routine Applications Jinming Zhang *, Xiaojun Zhang, Yungang Li and Jiahe Tian * Department of Nuclear Medicine, the PLA General Hospital, Beijing 100853, China * Authors to whom correspondence should be addressed; E-Mails: zhangjm301@163.com (J.Z.); tianjh@ (J.T.). Received: 27 April 2012; in revised form: 28 April 2012 / Accepted: 30 April 2012 / Published: 1 June 2012 Abstract: [11C]-(+)-?-DTBZ has been used as a marker of dopaminergic terminal densities in human striatum and expressed in islet beta cells in the pancreas. We aimed to establish a fully automated and simple procedure for the synthesis of [11C]-(+)-?-DTBZ for routine applications. [11C]-(+)-?-DTBZ was synthesized from a 9-hydroxy precursor in acetone and potassium hydroxide with [11C]-methyl triflate and was purified by solid phase extraction using a Vac tC-18 cartridge. Radiochemical yields based on [11C]-methyl triflate (corrected for decay) were 82.3% ± 3.6%, with a specific radioactivity of 60 GBq/?mol. Time elapsed was less than 20 min from end of bombardment to release of the product for quality control. Keywords: [11C]-(+)-?-DTBZ; VMAT2; position emission tomography; automated synthesis 1. Introduction The vesicular monoamine transporter (VMAT) has two pharmacologically distinct isoforms, VMAT1 and VMAT2 [1]. In contrast to VMAT1, VMAT2 is primarily found in the central nervous system of rodents and humans. Over 95% of striatal VMAT2 binding sites are associated with dopaminergic terminals, and the striatal VMAT2 binding site density is a linear function of the mesencephalic nigrostriatal neuron number [2]. Type-2 vesicular monoamine transporter binding is predicted to be unaffected by dopamin