Results 31 to 40 of about 107,657 (326)

A positive allosteric modulator for the muscarinic receptor (M1 mAChR) improves pathology and cognitive deficits in female APPswe/PSEN1ΔE9 mice

British Journal of Pharmacology, 2021
Alzheimer's disease (AD) is a neurodegenerative disease characterized by progressive cognitive decline, and women account for 60% of diagnosed cases. β‐Amyloid (Aβ) oligomers are considered the principal neurotoxic species in AD brains. The M1 muscarinic
Khaled S. Abd-Elrahman, Shaarika Sarasija, Tash-Lynn L. Colson, Stephen S. G. Ferguson   +3 more
semanticscholar   +1 more source

Safety, pharmacokinetics and quantitative EEG modulation of TAK‐071, a novel muscarinic M1 receptor positive allosteric modulator, in healthy subjects

British Journal of Clinical Pharmacology, 2021
TAK‐071 is a muscarinic M1 receptor positive allosteric modulator designed to have low cooperativity with acetylcholine. This was a first‐in‐human study to evaluate the safety, pharmacokinetics, and pharmacodynamics of TAK‐071.
W. Yin, Fahimeh Mamashli, D. Buhl, P. Khudyakov, D. Volfson, F. Martényi, H. Gevorkyan, L. Rosen, A. Simen   +8 more
semanticscholar   +1 more source

Allosteric Modulators of G Protein-Coupled Dopamine and Serotonin Receptors: A New Class of Atypical Antipsychotics

Pharmaceuticals, 2020
Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in 1952, strategies aimed at modifying the activity of dopamine receptors ...
Irene Fasciani, Francesco Petragnano, Gabriella Aloisi, Francesco Marampon, Marco Carli, Marco Scarselli, Roberto Maggio, Mario Rossi   +7 more
doaj   +1 more source

Positive Allosteric Modulation of TRPV1 as a Novel Analgesic Mechanism [PDF]

Molecular Pain, 2012
Background: The prevalence of long-term opiate use in treating chronic non-cancer pain is increasing, and prescription opioid abuse and dependence are a major public health concern. To explore alternatives to opioid-based analgesia, the present study investigates a novel allosteric pharmacological approach operating through the cation channel TRPV1 ...
Lebovitz Evan E, Keller Jason M, Kominsky Hal, Kaszas Krisztian, Maric Dragan, Iadarola Michael J   +5 more
openaire   +3 more sources

Mechanism of Positive Allosteric Modulators Acting on AMPA Receptors [PDF]

The Journal of Neuroscience, 2005
Ligand-gated ion channels involved in the modulation of synaptic strength are the AMPA, kainate, and NMDA glutamate receptors. Small molecules that potentiate AMPA receptor currents relieve cognitive deficits caused by neurodegenerative diseases such as Alzheimer's disease and show promise in the treatment of depression.
Rongsheng, Jin, Suzanne, Clark, Autumn M, Weeks, Joshua T, Dudman, Eric, Gouaux, Kathryn M, Partin   +5 more
openaire   +2 more sources

Potentiation and allosteric agonist activation of α7 nicotinic acetylcholine receptors: binding sites and hypotheses

Pharmacological Research, 2023
Considerable progress has been made in recent years towards the identification and characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs).
Victoria R. Sanders, Neil S. Millar
doaj   +1 more source

Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]

, 2007
Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
core   +1 more source

Conformational transitions and allosteric modulation in a heteromeric glycine receptor

Nature Communications, 2023
Glycine receptors (GlyR) are a critical postsynaptic component of spinal neurons. Here, the auhtors present cryo-EM structures of a heteromeric GlyR in the presence of an antagonist, agonist and agonist with a positive allosteric modulator.
Eric Gibbs, Emily Klemm, David Seiferth, Arvind Kumar, Serban L. Ilca, Philip C. Biggin, Sudha Chakrapani   +6 more
doaj   +1 more source

Allosterism vs. Orthosterism: Recent Findings and Future Perspectives on A2B AR Physio-Pathological Implications

Frontiers in Pharmacology, 2021
The development of GPCR (G-coupled protein receptor) allosteric modulators has attracted increasing interest in the last decades. The use of allosteric modulators in therapy offers several advantages with respect to orthosteric ones, as they can fine ...
Elisabetta Barresi, Claudia Martini, Federico Da Settimo, Giovanni Greco, Sabrina Taliani, Chiara Giacomelli, Maria Letizia Trincavelli   +6 more
doaj   +1 more source

Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor [PDF]

ACS Medicinal Chemistry Letters, 2010
Novel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physical and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads.
Robert M, Garbaccio, Edward J, Brnardic, Mark E, Fraley, George D, Hartman, Pete H, Hutson, Julie A, O'Brien, Brian C, Magliaro, Jason M, Uslaner, Sarah L, Huszar, Kerry L, Fillgrove, James H, Small, Cuyue, Tang, Yuhsin, Kuo, Marlene A, Jacobson   +13 more
openaire   +2 more sources