Results 301 to 310 of about 107,657 (326)

Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA

Bioorganic & Medicinal Chemistry Letters, 2007
This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to a unique allosteric binding site distinct from other mGluR5 PAMs, CPPHA has been the focus of ...
Zhijian, Zhao, David D, Wisnoski, Julie A, O'Brien, Wei, Lemaire, David L, Williams, Marlene A, Jacobson, Marion, Wittman, Sookhee N, Ha, Herve, Schaffhauser, Cyrille, Sur, Doug J, Pettibone, Mark E, Duggan, P Jeffrey, Conn, George D, Hartman, Craig W, Lindsley   +14 more
openaire   +2 more sources

mGluR2 positive allosteric modulators: a patent review (2009 – present)

Expert Opinion on Therapeutic Patents, 2013
The mGlu2 receptor, which belongs to the group II subfamily of metabotropic glutamate receptors (mGlu) along with the mGlu3 receptor, has proven to be of particular importance in neuropharmacology. Preferentially expressed on presynaptic nerve terminals, the mGlu2 receptor negatively modulates glutamate and GABA release and is widely distributed in the
Andrés A, Trabanco, José María, Cid
openaire   +2 more sources

QSAR design of triazolopyridine mGlu2 receptor positive allosteric modulators

Journal of Molecular Graphics and Modelling, 2014
Two QSAR approaches were applied to assist the design and to prioritise the synthesis of new active mGlu2 receptor positive allosteric modulators (PAMs). With the aim to explore a particular point of substitution the models successfully prioritised molecules originating from chemistry ideas and a large virtual library. The two methods, 3D topomer CoMFA
Gary, Tresadern, José-Maria, Cid, Andrés A, Trabanco   +2 more
openaire   +2 more sources

Positive allosteric modulators of the calcium-sensing receptor

2021
The present invention relates to non-naturally occurring antibodies or active antibody fragments specifically binding the calcium-sensing receptor (CaSR), acting as positive allosteric modulators (PAMs) to provide for potent therapeutic agents. More particular, the immunoglobulin single variable domains (ISVDs) identified herein reveal a novel ...
Steyaert, Jan, Pardon, Els, Wohlkönig, Alexandre, Zögg, Thomas, Mos, Iris, BRÄUNER-OSBORNE, Hans, Mosolff Mathiesen, Jesper   +6 more
openaire   +2 more sources

mGluR5 positive allosteric modulators

Drugs of the Future, 2008
null Chen, Y., null Conn, P.J.
openaire   +1 more source

Antidepressant-Like Effects of CX717, a Positive Allosteric Modulator of AMPA Receptors

Molecular Neurobiology, 2020
M. Gordillo-Salas, Raquel Pascual-Antón, Jun Ren, J. Greer, A. Adell   +4 more
semanticscholar   +1 more source

Reprogramming CBX8-PRC1 function with a positive allosteric modulator

Cell Chemical Biology, 2022
Junghyun L Suh, Daniel Bsteh, Bryce Hart   +2 more
exaly  

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor.

Journal of Medicinal Chemistry, 2017
Gabriel Martinez Botella, F. Salituro, B. Harrison, R. Beresis, Zhu Bai, M. Blanco, Gabriel M. Belfort, Jing Dai, Carlos M. Loya, M. Ackley, Alison L. Althaus, S. Grossman, E. Hoffmann, James J. Doherty, A. Robichaud   +14 more
semanticscholar   +1 more source

Pharmacokinetic and pharmacodynamic characterisation of JNJ-40411813, a positive allosteric modulator of mGluR2, in two randomised, double-blind phase-I studies

Journal of Psychopharmacology, 2015
Ion Anghelescu, Luc Van Nueten, Peter De Boer   +2 more
exaly  

Pharmacological characterisation of MDI-222, a novel AMPA receptor positive allosteric modulator with an improved safety profile

Journal of Psychopharmacology, 2020
Simon E Ward, John R Atack
exaly