Results 21 to 30 of about 107,657 (326)

Sex-dependent anti-stress effect of an α5 subunit containing GABAA receptor positive allosteric modulator

Frontiers in Pharmacology, 2016
Rationale: Current first-line treatments for stress-related disorders such as Major Depressive Disorder (MDD) act on monoaminergic systems and take weeks to achieve a therapeutic effect with poor response and low remission rates.
Sean C. Piantadosi, Sean C. Piantadosi, Beverly J French, Michael M Poe, Tamara Timić, Bojan Marković, Mohan Pabba, Marianne Seney, Hyunjung Oh, Beverley Anne Orser, Miroslav M Savic, James M Cook, Etienne Sibille, Etienne Sibille, Etienne Sibille, Etienne Sibille   +15 more
doaj   +2 more sources

Antipsychotic profiles of TASP0443294, a novel and orally active positive allosteric modulator of metabotropic glutamate 2 receptor

Journal of Pharmacological Sciences, 2015
Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has been shown to be effective in a number of animal models of schizophrenia.
Hirohiko Hikichi, Tetsuaki Hiyoshi, Toshiyuki Marumo, Yasumitsu Tomishima, Ayaka Kaku, Izumi Iida, Hiroki Urabe, Tomoko Tamita, Akito Yasuhara, Jun-ichi Karasawa, Shigeyuki Chaki   +10 more
doaj   +2 more sources

MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate

ACS Medicinal Chemistry Letters, 2018
Douglas C Beshore, Christina N Di Marco, Marion Wittmann   +2 more
exaly   +2 more sources

Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators

Molecules, 2023
Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric ...
Dina Manetti, Silvia Dei, Hugo R. Arias, Laura Braconi, Alessio Gabellini, Elisabetta Teodori, Maria Novella Romanelli   +6 more
doaj   +1 more source

The allosterically modulated FFAR2 is transactivated by signals generated by other neutrophil GPCRs.

PLoS ONE, 2023
Positive allosteric modulators for free fatty acid receptor 2 (FFAR2/GPR43), that affect receptor function through binding to two distinct allosteric binding sites, were used to determine the correlation between the responses induced in neutrophils by ...
Simon Lind, Kenneth L Granberg, Huamei Forsman, Claes Dahlgren   +3 more
doaj   +2 more sources

Prospects for the use of allosteric drugs in real-world clinical practice

Реальная клиническая практика: данные и доказательства, 2023
While the clinical validity of the use of allosteric regulation is known, scientists are working on the discovery of new methods for the development of allosteric drugs that can modulate the functions of enzymes, depending on the desired therapeutic ...
I. R. Svechkareva, A. S. Kolbin
doaj   +1 more source

Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]

Proceedings of the National Academy of Sciences, 2013
μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford, Mary J, Clark, Tom S, Wehrman, Samuel W, Gerritz, Martyn, Banks, Jonathan, O'Connell, John R, Traynor, Andrew, Alt   +7 more
openaire   +2 more sources

Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2

eLife, 2022
Activation of G protein-coupled receptors (GPCRs) is an allosteric process. It involves conformational coupling between the orthosteric ligand binding site and the G protein binding site. Factors that bind at non-cognate ligand binding sites to alter the
Brandon Wey-Hung Liauw, Arash Foroutan, Michael R Schamber, Weifeng Lu, Hamid Samareh Afsari, Reza Vafabakhsh   +5 more
doaj   +1 more source

Unique Positive Cooperativity Between the β-Arrestin–Biased β-Blocker Carvedilol and a Small Molecule Positive Allosteric Modulator of the β2-Adrenergic Receptor

Molecular Pharmacology, 2021
Among β-blockers that are clinically prescribed for heart failure, carvedilol is a first-choice agent with unique pharmacological properties. Carvedilol is distinct from other β-blockers in its ability to elicit β-arrestin–biased agonism, which has been ...
Biswaranjan Pani, Seungkirl Ahn, Paula K. Rambarat, Shashank Vege, Alem W. Kahsai, Andrew Liu, Bruno N Valan, D. Staus, T. Costa, R. Lefkowitz   +9 more
semanticscholar   +1 more source

The Allosteric Activation of α7 nAChR by α-Conotoxin MrIC Is Modified by Mutations at the Vestibular Site

Toxins, 2021
α-conotoxins are 13–19 amino acid toxin peptides that bind various nicotinic acetylcholine receptor (nAChR) subtypes. α-conotoxin Mr1.7c (MrIC) is a 17 amino acid peptide that targets α7 nAChR.
Alican Gulsevin, Roger L. Papke, Clare Stokes, Hue N. T. Tran, Aihua H. Jin, Irina Vetter, Jens Meiler   +6 more
doaj   +1 more source