Therapeutic potential of group III metabotropic glutamate receptors

H Lavreysen, FM Dautzenberg - Current medicinal chemistry, 2008 - ingentaconnect.com
Metabotropic glutamate (mGlu) receptors have received much attention, driven by a strong
belief in the potential of these modulatory glutamate receptors as drug targets. So far, major …

[PDF][PDF] Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents

…, SR Stauffer, JS Daniels, CM Niswender, H Lavreysen… - Neuron, 2015 - cell.com
Schizophrenia is associated with disruptions in N-methyl-D-aspartate glutamate receptor
subtype (NMDAR)-mediated excitatory synaptic signaling. The metabotropic glutamate …

Metabotropic glutamate receptors: their therapeutic potential in anxiety

W Spooren, A Lesage, H Lavreysen… - … Neurobiology of Anxiety …, 2010 - Springer
Psychiatric and neurological disorders are linked to changes in synaptic excitatory processes
with a key role for glutamate, that is, the most abundant excitatory amino-acid. Molecular …

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous …

…, E Days, Y Zhou, AL Rodriguez, H Lavreysen… - Molecular …, 2012 - ASPET
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor subtype 5 (mGlu 5
) have emerged as an exciting new approach for the treatment of schizophrenia and other …

JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist

H Lavreysen, R Wouters, F Bischoff, SN Pereira… - …, 2004 - Elsevier
We examined the pharmacological profile of (3,4-dihydro-2H-pyrano[2,3]b quinolin-7-yl) (cis-4-methoxycyclohexyl)
methanone (JNJ16259685). At recombinant rat and human …

Discovery of 3-Cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): A Positive Allosteric Modulator of the …

…, GJ Macdonald, D Oehlrich, H Lavreysen… - Journal of medicinal …, 2012 - ACS Publications
Advanced leads from a series of 1,2,4-triazolo[4,3-a]pyridines with mGlu2 receptor PAM
activity are reported. By modification of the analogous imidazo[1,2-a]pyridine series, the newly …

Characterization of 2-[[4-fluoro-3-(trifluoromethyl) phenyl] amino]-4-(4-pyridinyl)-5-thiazolemethanol (JNJ-1930942), a novel positive allosteric modulator of the α7 …

T Dinklo, H Shaban, JW Thuring, H Lavreysen… - … of Pharmacology and …, 2011 - ASPET
The α 7 nicotinic acetylcholine receptor (nAChR) is a potential therapeutic target for the
treatment of cognitive deficits associated with schizophrenia, Alzheimer's disease, Parkinson's …

[3H] R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists

H Lavreysen, C Janssen, F Bischoff, X Langlois… - Molecular …, 2003 - ASPET
R214127 was shown to be a potent and noncompetitive metabotropic glutamate 1 (mGlu1)
receptor-selective antagonist. The kinetics and pharmacology of [ 3 H]1-(3,4-dihydro-2H-…

Scaffold hopping from pyridones to imidazo [1, 2-a] pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor

…, ML Linares, D Oehlrich, H Lavreysen… - Bioorganic & medicinal …, 2010 - Elsevier
Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel
positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent …

Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission …

…, L Iturrino, X Langlois, H Lavreysen… - Journal of medicinal …, 2012 - ACS Publications
The synthesis and in vitro and in vivo evaluation of a new series of 7-(phenylpiperidinyl)-1,2,4-triazolo[4,3-a]pyridines,
which were conveniently radiolabeled with carbon-11, as …