A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models

GG Kinney, JA O'Brien, W Lemaire, M Burno… - … of Pharmacology and …, 2005 - ASPET
We found that 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide (CDPPB) is a potent
and selective positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (…

Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation

…, M Jacobson, D Bickel, M Burno… - Proceedings of the …, 2009 - National Acad Sciences
The forebrain cholinergic system promotes higher brain function in part by signaling through
the M 1 muscarinic acetylcholine receptor (mAChR). During Alzheimer's disease (AD), …

Metabotropic glutamate subtype 5 receptors modulate locomotor activity and sensorimotor gating in rodents

GG Kinney, M Burno, UC Campbell… - … of Pharmacology and …, 2003 - ASPET
Use-dependent N-methyl-d-aspartate receptor (NMDAR) antagonists produce behaviors in
human volunteers that resemble schizophrenia and exacerbate those behaviors in …

Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-Diphenyl-1H- pyrazol-5-yl)benzamides That …

…, W Lemaire, DL Williams, M Burno… - Journal of medicinal …, 2004 - ACS Publications
This report describes the discovery of the first centrally active allosteric modulators of the
metabotropic glutamate receptor subtype 5 (mGluR5). Appropriately substituted N-(1,3-diphenyl…

The glycine transporter type 1 inhibitor N-[3-(4′-fluorophenyl)-3-(4′-phenylphenoxy) propyl] sarcosine potentiates NMDA receptor-mediated responses in vivo and …

GG Kinney, C Sur, M Burno, PJ Mallorga… - Journal of …, 2003 - Soc Neuroscience
Glycine acts as a necessary coagonist for glutamate at the NMDA receptor (NMDAR) complex
by binding to the strychnine-insensitive glycine-B binding site on the NR1 subunit. The fact …

Design, Synthesis, and In Vivo Efficacy of Glycine Transporter‐1 (GlyT1) Inhibitors Derived from a Series of [4‐Phenyl‐1‐(propylsulfonyl) piperidin‐4‐yl] methyl …

…, TB Chen, RSL Chang, M Burno… - ChemMedChem …, 2006 - Wiley Online Library
Design, Synthesis, and In Vivo Efficacy of Glycine Transporter-1 (GlyT1) Inhibitors Derived
from a Series of [4-Phenyl-1-(propylsulfonyl) piperidin-4-yl] methyl Benzamides

Identification of a human 5-HT6 receptor variant produced by alternative splicing

…, BR Schurman, HL Schmitt, M Burno… - Molecular brain …, 1999 - Elsevier
The complexity of the 5-hydroxytryptamine (5-HT) (serotonin) receptor family has been increased
by the findings that isoforms or splice variants exist for subtypes such as the 5-HT 2B , 5…

A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors

W Lemaire, JA O'Brien, M Burno, AG Chaudhary… - European journal of …, 2002 - Elsevier
A novel, potent nonpeptide oxytocin receptor antagonist (1-(1-(2-(2,2,2-trifluoroethoxy)-4-(1-methylsulfonyl-4-piperidinyloxy)
phenylacetyl)-4-piperidinyl)-3,4-dihydro-2(1H)-quinolinone) …

[CITATION][C] P4‐305: Allosteric potentiation of the M1 muscarinic receptor provides unprecedented selectivity and a novel therapeutic strategy for the treatment of …

…, A Simon, M Burno… - Alzheimer's & …, 2008 - Wiley Online Library
Background Alzheimer's disease (AD) patients suffer from an inexorable loss of cognitive
function due in part to the degeneration of the basal forebrain cholinergic projection neurons. …

[CITATION][C] P1‐016: Dietary induction of hyperhomocystemia and the impact on Alzheimer's disease‐relevant markers

…, S Na, M Marlatt, D Bickel, M Burno… - Alzheimer's & …, 2008 - Wiley Online Library
Background In addition to the primary pathological features of extraneuronal amyloid β (Aβ)
protein deposition and intraneuronal aggregation of hyperphosphorylated tau in Alzheimer's …