ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors:: Identification, in vitro pharmacology, pharmacokinetic and biodistribution studies

被引：70

作者：

Hintermann, Samuel

Vranesic, Ivo

Allgeier, Hans

Bruelisauer, Armin

Hoyer, Daniel

Lemaire, Michel

Moenius, Thomas

Urwyler, Stephan

Whitebread, Steven

Gasparini, Fabrizio ^{[1
]}

Auberson, Yves P.

机构：

[1] Novartis Inst BioMed Res, CH-4002 Basel, Switzerland

[2] Novartis Pharma AG, CH-4002 Basel, Switzerland

[3] Novartis Inst BioMed Res, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 02期

关键词：

metabotropic glutamate receptor subtype 5; H-3]ABP688; ABP688; PET imaging;

D O I：

10.1016/j.bmc.2006.10.038

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

[C-11]ABP688 (2) has recently been demonstrated to be a useful PET tracer for in vivo imaging of the metabotropic glutamate receptors type 5 (mGluR5) in rodents. We describe here the identification and preclinical profiling of ABP688 and its tritiated version [H-3]ABP688, and show that its high affinity (K-d = 2 nM), selectivity, and pharmacokinetic properties fulfill all requirements for development as a PET tracer for clinical imaging of the mGlu5 receptor. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：903 / 914

页数：12

共 32 条

[31] Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist [J].