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

[1]

Ametamey S. M., 2003, Journal of Labelled Compounds and Radiopharmaceuticals, V46, pS188

[2]

Ametamey SM, 2006, J NUCL MED, V47, P698

[3] PRACTICAL ASPECTS OF TWO-DIMENSIONAL TRANSVERSE NOE SPECTROSCOPY [J].

BAX, A ;

DAVIS, DG .

JOURNAL OF MAGNETIC RESONANCE, 1985, 63 (01) :207-213

[4] MOLECULAR AND FUNCTIONAL-CHARACTERIZATION OF RECOMBINANT HUMAN METABOTROPIC GLUTAMATE-RECEPTOR SUBTYPE-5 [J].

DAGGETT, LP ;

SACAAN, AI ;

AKONG, M ;

RAO, SP ;

HESS, SD ;

LIAW, C ;

URRUTIA, A ;

JACHEC, C ;

ELLIS, SB ;

DREESSEN, J ;

KNOPFEL, T ;

LANDWEHRMEYER, GB ;

TESTA, CM ;

YOUNG, AB ;

VARNEY, M ;

JOHNSON, EC ;

VELICELEBI, G .

NEUROPHARMACOLOGY, 1995, 34 (08) :871-886

[5] MOLECULAR-CLONING, FUNCTIONAL EXPRESSION AND PHARMACOLOGICAL CHARACTERIZATION OF THE HUMAN METABOTROPIC GLUTAMATE-RECEPTOR TYPE-2 [J].

FLOR, PJ ;

LINDAUER, K ;

PUTTNER, I ;

RUEGG, D ;

LUKIC, S ;

KNOPFEL, T ;

KUHN, R .

EUROPEAN JOURNAL OF NEUROSCIENCE, 1995, 7 (04) :622-629

[6] [3H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5 [J].

Gasparini, F ;

Andres, H ;

Flor, PJ ;

Heinrich, M ;

Inderbitzin, W ;

Lingenhöhl, K ;

Müller, H ;

Munk, VC ;

Omilusik, K ;

Stierlin, C ;

Stoehr, N ;

Vranesic, I ;

Kuhn, R .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (03) :407-409

[7] 2-methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist [J].

Gasparini, F ;

Lingenhöhl, K ;

Stoehr, N ;

Flor, PJ ;

Heinrich, M ;

Vranesic, I ;

Biollaz, M ;

Allgeier, H ;

Heckendorn, R ;

Urwyler, S ;

Varney, MA ;

Johnson, EC ;

Hess, SD ;

Rao, SP ;

Sacaan, AI ;

Santori, EM ;

Veliçelebi, G ;

Kuhn, R .

NEUROPHARMACOLOGY, 1999, 38 (10) :1493-1503

[8] RECOMBINANT HUMAN ALPHA(2)-ADRENOCEPTOR SUBTYPES - COMPARISON OF [H-3] RAUWOLSCINE, [H-3] ATIPAMEZOLE AND [H-3] RX821002 AS RADIOLIGANDS [J].

HALME, M ;

SJOHOLM, B ;

SAVOLA, JM ;

SCHEININ, M .

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH, 1995, 1266 (02) :207-214

[9]

Hamill T. G., 2003, Journal of Labelled Compounds and Radiopharmaceuticals, V46, pS184

[10] Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers [J].

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 .

SYNAPSE, 2005, 56 (04) :205-216

← 1 2 3 4 →