Results 61 to 70 of about 121,181 (303)

Identification of compounds acting as negative allosteric modulators of the LPA1 receptor [PDF]

European Journal of Pharmacology, 2018
The Lysophosphatidic Acid 1 Receptor (LPA1 receptor) has been linked to the initiation and progression of a variety of poorly treated fibrotic conditions. Several compounds that have been described as LPA1 receptor antagonists have progressed into clinical trials: 1-(4-{4-[3-methyl-4-({[(1R)-1-phenylethoxy]carbonyl}amino)-1,2-oxazol-5-yl]phenyl}phenyl ...
Ellery, Jonathan, Dickson, Louise, Cheung, Toni, Ciuclan, Loredana, Bunyard, Peter, Mack, Stephen, Buffham, William J., Farnaby, William, Mitchell, Philip, Brown, Daniel, Isaacs, Richard, Barnes, Matt   +11 more
openaire   +3 more sources

Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters

Data in Brief, 2017
The data in this article outline the methods used for the administration of GET 73 in the first time-in-human manuscript entitled “Phase I randomized clinical trial for the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative ...
Carolina L. Haass-Koffler, Kimberly Goodyear, Victoria M. Long, Harrison H. Tran, Antonella Loche, Roberto Cacciaglia, Robert M. Swift, Lorenzo Leggio   +7 more
doaj   +1 more source

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Communications Biology, 2020
Kennedy et al. report the pharmacological and in vivo profiling of two small molecule PAR2 inhibitors and an agonist. They conclude that while the small molecule agonist and one of the inhibitors bind to the orthosteric PAR2 binding site, the other ...
Amanda J. Kennedy, Linda Sundström, Stefan Geschwindner, Eunice K. Y. Poon, Yuhong Jiang, Rongfeng Chen, Rob Cooke, Shawn Johnstone, Andrew Madin, Junxian Lim, Qingqi Liu, Rink-Jan Lohman, Anneli Nordqvist, Maria Fridén-Saxin, Wenzhen Yang, Dean G. Brown, David P. Fairlie, Niek Dekker   +17 more
doaj   +1 more source

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1 [PDF]

Bioorganic & Medicinal Chemistry Letters, 2013
Development of SAR in an octahydropyrrolo[3,4-c]pyrrole series of negative allosteric modulators of mGlu1 using a functional cell-based assay is described in this Letter. The octahydropyrrolo[3,4-c]pyrrole scaffold was chosen as an isosteric replacement for the piperazine ring found in the initial hit compound. Characterization of selected compounds in
Jason T, Manka, Alice L, Rodriguez, Ryan D, Morrison, Daryl F, Venable, Hyekyung P, Cho, Anna L, Blobaum, J Scott, Daniels, Colleen M, Niswender, P Jeffrey, Conn, Craig W, Lindsley, Kyle A, Emmitte   +10 more
openaire   +2 more sources

Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine [v1; ref status: indexed, http://f1000r.es/o0]

F1000Research, 2013
We investigated the role of metabotropic glutamate receptor type 5 (mGluR5) in methamphetamine-induced behavioral sensitization. The mGluR5 positive allosteric modulator (3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl) benzamide (CDPPB) and negative allosteric ...
Peter R Kufahl, Natali E Nemirovsky, Lucas R Watterson, Nicholas Zautra, M Foster Olive   +4 more
doaj   +1 more source

Binding of a negative allosteric modulator and competitive antagonist can occur simultaneously at the ionotropic glutamate receptor GluA2

The FEBS Journal, 2020
Ionotropic glutamate receptors are ligand‐gated ion channels governing neurotransmission in the central nervous system. Three major types of antagonists are known for the AMPA‐type receptor GluA2: competitive, noncompetitive (i.e., negative allosteric ...
Christian Krintel, J. Dorosz, A. H. Larsen, Thor Seneca Thorsen, R. Venskutonytė, O. Mirza, M. Gajhede, T. Boesen, J. Kastrup   +8 more
semanticscholar   +1 more source

A Novel Family of Negative and Positive Allosteric Modulators of NMDA Receptors [PDF]

The Journal of Pharmacology and Experimental Therapeutics, 2010
The N-methyl-D-aspartate (NMDA) receptor family regulates various central nervous system functions, such as synaptic plasticity. However, hypo- or hyperactivation of NMDA receptors is critically involved in many neurological and psychiatric conditions, such as pain, stroke, epilepsy, neurodegeneration, schizophrenia, and depression.
Costa, BM, Irvine, MW, Fang, G, Eaves, RJ, Mayo-Martin, MB, Skifter, DA, Jane, DE, Monaghan, DT   +7 more
openaire   +3 more sources

Distinctive binding properties of the negative allosteric modulator, [3H]SB269,652, at recombinant dopamine D3 receptors [PDF]

, 2018
Recently, employing radioligand displacement and functional coupling studies, we demonstrated that SB269,652 (N-[(1r,4r)-4-[2-(7-cyano-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-1H-indole-2-carboxamide) interacts in an atypical manner with ...
Mannoury la Cour, Clotilde, Irene Fasciani, Fasciani, Irene, Clotilde Mannoury la Cour, Aloisi, Gabriella, Ilaria Pietrantoni, Mario Rossi, Roberto Maggio, Millan, Mark J., Mark J. Millan, Gabriella Aloisi, Francesco Marampon, Marco Scarselli, Maggio, Roberto, Rossi, Mario, Millan, Mark J, Marampon, Francesco, Scarselli, Marco, Pietrantoni, Ilaria   +18 more
core   +1 more source

In Vivo Non-radioactive Assessment of mGlu5 Receptor-Activated Polyphosphoinositide Hydrolysis in Response to Systemic Administration of a Positive Allosteric Modulator

Frontiers in Pharmacology, 2018
mGlu5 receptor-mediated polyphosphoinositide (PI) hydrolysis is classically measured by determining the amount of radioactivity incorporated in inositolmonophosphate (InsP) after labeling of membrane phospholipids with radioactive inositol. Although this
Anna R. Zuena, Luisa Iacovelli, Rosamaria Orlando, Luisa Di Menna, Paola Casolini, Giovanni Sebastiano Alemà, Gabriele Di Cicco, Giuseppe Battaglia, Ferdinando Nicoletti, Ferdinando Nicoletti   +9 more
doaj   +1 more source

Negative and positive allosteric modulators of the P2X ₇ receptor [PDF]

British Journal of Pharmacology, 2008
Background and purpose: Antagonist effects at the P2X 7 receptor are complex with many behaving in a non‐competitive manner. In this study, the effects of N ‐[2‐({2‐[(2‐hydroxyethyl)amino]ethyl}amino)‐5‐
A D, Michel, L J, Chambers, D S, Walter
openaire   +2 more sources