[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy:: Potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor

被引:125
作者
Cosford, NDP
Roppe, J
Tehrani, L
Schweiger, EJ
Seiders, TJ
Chaudary, A
Rao, S
Varney, MA
机构
[1] Merck Res Labs, Dept Chem, MRLSDB2, San Diego, CA 92121 USA
[2] Merck Res Labs, Dept Neuropharmacol, MRLSDB1, San Diego, CA 92121 USA
[3] Merck Res Labs, Dept Drug Metab, Rahway, NJ 07065 USA
关键词
D O I
10.1016/S0960-894X(02)00997-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The design, synthesis, and characterization of two potent, non-competitive radioligands, [H-3]-methoxymethyl-MTEP and [H-3]-methoxy-PEPy, that are selective for the mGlu5 receptor are described. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:351 / 354
页数:4
相关论文
共 16 条
[1]  
ANDERSON J, IN PRESS J PHARM EXP
[2]   Anxiolytic-like activity of the mGluR5 antagonist MPEP - A comparison with diazepam and buspirone [J].
Brodkin, J ;
Busse, C ;
Sukoff, SJ ;
Varney, MA .
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 2002, 73 (02) :359-366
[3]   Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice [J].
Chiamulera, C ;
Epping-Jordan, MP ;
Zocchi, A ;
Marcon, C ;
Cottiny, C ;
Tacconi, S ;
Corsi, M ;
Orzi, F ;
Conquet, F .
NATURE NEUROSCIENCE, 2001, 4 (09) :873-874
[4]  
COSFORD NDP, IN PRESS J MED CHEM
[5]   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
[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]  
Klodzinska A, 2000, POL J PHARMACOL, V52, P463
[8]  
PATEL S, IN PRSS LIFE SCI
[9]   The Metabotropic Glutamate Receptors: Structure, Activation Mechanism and Pharmacology [J].
Pin, Jean-Philippe ;
Acher, Francine .
CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS, 2002, 1 (03) :297-317
[10]   The metabotropic glutamate receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) blocks fear conditioning in rats [J].
Schulz, B ;
Fendt, M ;
Gasparini, F ;
Lingenhöhl, K ;
Kuhn, R ;
Koch, M .
NEUROPHARMACOLOGY, 2001, 41 (01) :1-7