Radiosynthesis of the diastereomerically pure (E)-[11C]ABP688

被引：0
作者：
Bdair, Hussein [1 ,4 ]
Tsai, I-Huang [2 ]
Smart, Kelly [3 ]
Benkelfat, Chawki [4 ]
Leyton, Marco [4 ]
Kostikov, Alexey [1 ,2 ,5 ]
机构：
[1] McGill Univ, Montreal Neurol Inst, Montreal, PQ, Canada
[2] McGill Univ, McConnell Brain Imaging Ctr, Montreal Neurol Inst, Montreal, PQ, Canada
[3] Yale Univ, Sch Med, Yale PET Ctr, New Haven, CT USA
[4] McGill Univ, Dept Psychiat, Montreal, PQ, Canada
[5] McGill Univ, Dept Neurol & Neurosurg, Montreal, PQ, Canada
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2019年 / 62卷 / 12期
关键词：
mGlu5; receptors; PET tracers; radiosynthesis; (E)-[C-11]ABP688; RECEPTOR SUBTYPE 5; PHARMACOLOGY; PET;
D O I：
10.1002/jlcr.3802
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
We report an efficient protocol for the radiosynthesis of diastereomerically pure (E)-[C-11]ABP688, a positron emission tomography (PET) tracer for metabotropic glutamate type 5 (mGlu5) receptor imaging. The protocol reliably provides sterile and pyrogen-free formulation of (E)-[C-11]ABP688 suitable for preclinical and clinical PET imaging with >99% diastereomeric excess (d.e.), >99% overall radiochemical purity (RCP), 14.9 +/- 4.3% decay-corrected radiochemical yield (RCY), and 148.86 +/- 79.8 GBq/mu mol molar activity in 40 minutes from the end of bombardment.
引用
收藏
页码：860 / 864
页数：5
相关论文
共 19 条
  • [1] Ametamey SM, 2007, J NUCL MED, V48, P247
  • [2] Ametamey SM, 2006, J NUCL MED, V47, P698
  • [3] In Vivo Imaging of mGluR5 Changes during Epileptogenesis Using [11C]ABP688 PET in Pilocarpine-Induced Epilepsy Rat Model
    Choi, Hongyoon
    Kim, Yu Kyeong
    Oh, So Won
    Im, Hyung-Jun
    Hwang, Do Won
    Kang, Hyejin
    Lee, Boeun
    Lee, Yun-Sang
    Jeong, Jae Min
    Kim, E. Edmund
    Chung, June-Key
    Lee, Dong Soo
    [J]. PLOS ONE, 2014, 9 (03):
  • [4] In vivo variation in same-day estimates of metabotropic glutamate receptor subtype 5 binding using [11C]ABP688 and [18F]FPEB
    DeLorenzo, Christine
    Gallezot, Jean-Dominique
    Gardus, John
    Yang, Jie
    Planeta, Beata
    Nabulsi, Nabeel
    Ogden, R. Todd
    Labaree, David C.
    Huang, Yiyun H.
    Mann, J. John
    Gasparini, Fabrizio
    Lin, Xin
    Javitch, Jonathan A.
    Parsey, Ramin V.
    Carson, Richard E.
    Esterlis, Irina
    [J]. JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM, 2017, 37 (08) : 2716 - 2727
  • [5] Ketamine-induced reduction in mGluR5 availability is associated with an antidepressant response: an [11C]ABP688 and PET imaging study in depression
    Esterlis, I.
    DellaGioia, N.
    Pietrzak, R. H.
    Matuskey, D.
    Nabulsi, N.
    Abdallah, C. G.
    Yang, J.
    Pittenger, C.
    Sanacora, G.
    Krystal, J. H.
    Parsey, R. V.
    Carson, R. E.
    DeLorenzo, C.
    [J]. MOLECULAR PSYCHIATRY, 2018, 23 (04) : 824 - 832
  • [6] Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers
    Hamill, TG
    Krause, S
    Ryan, C
    Bonnefous, C
    Govek, S
    Seiders, TJ
    Cosford, NDP
    Roppe, J
    Kamenecka, T
    Patel, S
    Gibson, RE
    Sanabria, S
    Riffel, K
    Eng, WS
    King, C
    Yang, XQ
    Green, MD
    O'Malley, SS
    Hargreaves, R
    Burns, HD
    [J]. SYNAPSE, 2005, 56 (04) : 205 - 216
  • [7] ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors:: Identification, in vitro pharmacology, pharmacokinetic and biodistribution studies
    Hintermann, Samuel
    Vranesic, Ivo
    Allgeier, Hans
    Bruelisauer, Armin
    Hoyer, Daniel
    Lemaire, Michel
    Moenius, Thomas
    Urwyler, Stephan
    Whitebread, Steven
    Gasparini, Fabrizio
    Auberson, Yves P.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (02) : 903 - 914
  • [8] Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression
    Hughes, Z. A.
    Neal, S. J.
    Smith, D. L.
    Rizzo, S. J. Sukoff
    Pulicicchio, C. M.
    Lotarski, S.
    Lu, S.
    Dwyer, J. M.
    Brennan, J.
    Olsen, M.
    Bender, C. N.
    Kouranova, E.
    Andree, T. H.
    Harrison, J. E.
    Whiteside, G. T.
    Springer, D.
    O'Neil, S. V.
    Leonard, S. K.
    Schechter, L. E.
    Dunlop, J.
    Rosenzweig-Lipson, S.
    Ring, R. H.
    [J]. NEUROPHARMACOLOGY, 2013, 66 : 202 - 214
  • [9] Binding potential of (E)-[11C]ABP688 to metabotropic glutamate receptor subtype 5 is decreased by the inclusion of its 11C-labelled Z-isomer
    Kawamura, Kazunori
    Yamasaki, Tomoteru
    Kumata, Katsushi
    Furutsuka, Kenji
    Takei, Makoto
    Wakizaka, Hidekatsu
    Fujinaga, Masayuki
    Kariya, Kaori
    Yui, Joji
    Hatori, Akiko
    Xie, Lin
    Shimoda, Yoko
    Hashimoto, Hiroki
    Hayashi, Kazutaka
    Zhang, Ming-Rong
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2014, 41 (01) : 17 - 23
  • [10] In vivo metabotropic glutamate receptor 5 availability-associated functional connectivity alterations in drug-naive young adults with major depression
    Kim, Jong-Hoon
    Joo, Yo-Han
    Son, Young-Don
    Kim, Jeong-Hee
    Kim, Yun-Kwan
    Kim, Hang-Keun
    Lee, Sang-Yoon
    Ido, Tatsuo
    [J]. EUROPEAN NEUROPSYCHOPHARMACOLOGY, 2019, 29 (02) : 278 - 290
12