Results 261 to 270 of about 121,181 (303)

Characterization of an mGluR2/3 Negative Allosteric Modulator in Rodent Models of Depression

Journal of Neurogenetics, 2011
There is growing evidence suggesting that antagonists of group II metabotropic glutamate receptors (mGluR2/3) exhibit antidepressant-like properties in several preclinical models of depression. However, all those studies have been performed using competitive group II non-selective orthosteric antagonists.
Campo, Brice, Kalinichev, Mikhail, Lambeng, Nathalie, El Yacoubi, M, Royer-Urios, Isabelle, Schneider, Manfred, Legrand, Coline, Parron, Delphine, Girard, Francoise, Bessif, Abdelhak, Poli, Sonia, Vaugeois, Jean-Marie, Le Poul, Emmanuel, Celanire, Sylvain   +13 more
openaire   +4 more sources

Identification of a β-arrestin-biased negative allosteric modulator for the β 2 -adrenergic receptor

Proceedings of the National Academy of Sciences of the United States of America, 2023
Catecholamine-stimulated β2-adrenergic receptor (β2AR) signaling via the canonical Gs–adenylyl cyclase–cAMP–PKA pathway regulates numerous physiological functions, including the therapeutic effects of exogenous β-agonists in the treatment of airway ...
Michael Ippolito, Francesco De Pascali, Konstantin E Komolov   +2 more
exaly   +2 more sources

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Structure–Activity Relationships for Negative Allosteric mGluR5 Modulators

ChemMedChem, 2012
AbstractA series of compounds based on the mGluR5‐selective ligand 2‐methyl‐6‐(phenylethynyl)pyridine (MPEP) were designed and synthesized. The compounds were found to be either structural analogues of MPEP, substituted monomers, or dimeric analogues. All compounds retained mGluR5 selectivity with only weak or no activity at other mGluRs or iGluRs. The
Kaae, Birgitte H, Harpsøe, Kasper, Kvist, Trine, Mathiesen, Jesper M, Mølck, Christina, Gloriam, David E, Jimenez, Hermogenes N, Uberti, Michelle A, Nielsen, Søren M, Nielsen, Birgitte, Bräuner-Osborne, Hans, Sauerberg, Per, Clausen, Rasmus Prætorius, Madsen, Ulf   +13 more
openaire   +3 more sources

Negative allosteric modulation of the µ-opioid receptor

2023
Abstract The µ-opioid receptor (µOR) is a well-established target for analgesia, yet conventional opioid receptor agonists cause serious adverse effects, notably addiction and respiratory depression, which have led to the present opioid overdose epidemic. µOR negative allosteric modulators (NAMs) may serve as powerful
Evan S. O’Brien, Vipin Ashok Rangari, Amal El Daibani, Shainnel O. Eans, Betsy White, Haoqing Wang, Yuki Shiimura, Kaavya Krishna Kumar, Kevin Appourchaux, Weijiao Huang, Chensong Zhang, Jesper M. Mathiesen, Tao Che, Jay P. McLaughlin, Susruta Majumdar, Brian K. Kobilka   +15 more
openaire   +1 more source

Negative Allosteric Modulator of mGluR1 Improves Long-term Neurologic Deficits after Experimental Subarachnoid Hemorrhage.

ACS Chemical Neuroscience, 2020
Aneurysmal subarachnoid hemorrhage (SAH) causes permanent neurological sequelae, but the underlying mechanism needs to be further clarified. Here, we show that inhibition of metabotropic glutamate receptor 1 (mGluR1) with negative allosteric modulator ...
Hong-bin Wang, Wei-qi Wang, Qing-jian Wu, Ya-jun Hou, Han-xia Li, Hui-juan Yang, Ming‐feng Yang, Bao-liang Sun, Zong-yong Zhang   +8 more
semanticscholar   +1 more source

QSAR Study of Anticonvulsant Negative Allosteric Modulators of the AMPA Receptor

Journal of Medicinal Chemistry, 2004
A quantitative structure-activity relationship (QSAR) study was performed on a set of 49 negative allosteric modulators of AMPA receptor, acting as anticonvulsant agents, using multiple linear regression. The predictive ability of the resulting model was evaluated against a set of 12 compounds; the results showed good statistics in regression and ...
MACCHIARULO, Antonio, De Luca L., Costantino G., BARRECA, MARIA LETIZIA, Gitto R., PELLICCIARI, Roberto, Chimirri A.   +6 more
openaire   +4 more sources

Extracellular binding sites of positive and negative allosteric P2X4 receptor modulators

Life Sciences, 2022
P2X receptors are ATP-gated ion channels which play a role in many pathophysiological conditions. They are considered as novel drug targets, particularly in the fields of pain, (neuro) inflammation, and cancer. Due to difficulties in developing drug-like orthosteric ligands that bind to the highly polar ATP binding site, the design of positive and ...
Stephanie Weinhausen, Jessica Nagel, Vigneshwaran Namasivayam, Claudia Spanier, Aliaa Abdelrahman, Theodor Hanck, Ralf Hausmann, Christa E. Müller   +7 more
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BNC210, a negative allosteric modulator of the alpha 7 nicotinic acetylcholine receptor, demonstrates anxiolytic- and antidepressant-like effects in rodents.

Neuropharmacology
This work describes the characterization of BNC210 (6-[(2,3-dihydro-1H-inden-2-yl)amino]-1-ethyl-3-(4-morpholinylcarbonyl)-1,8-naphthyridin-4(1H)-one), a selective, small molecule, negative allosteric modulator (NAM) of α7 nicotinic acetylcholine ...
S. O'Connor, B. Sleebs, I. Street, B. Flynn, J. Baell, Carolyn J. Coles, N. Quazi, Dharam Paul, E. Poiraud, B. Huyard, S. Wagner, E. Andriambeloson, Errol B. de Souza   +12 more
semanticscholar   +1 more source

In search of negative allosteric modulators of biological targets

Drug Discovery Today, 2009
The value of using negative allosteric modulators of protein function in therapeutic treatment of human diseases is becoming more apparent. Many current screening paradigms, however, are not consciously designed to discover negative allosteric modulators, and those that are serendipitously discovered can be easily overlooked during the hit-picking ...
openaire   +2 more sources

PKCε acts as negative allosteric modulator of EGF receptor signalling

Cellular Signalling, 2011
Protein kinase C ε (PKCε) is a transforming oncogene and plays a pivotal role in numerous cellular processes including proliferation, invasion and differentiation. Recently, we described a function of PKCε as a scaffold protein linking PLCγ1 to the EGFR module.
Simona, Weisheit, Claudia, Schäfer, Carmen, Mertens, Alexander, Berndt, Claus, Liebmann   +4 more
openaire   +2 more sources