Results 51 to 60 of about 107,657 (326)

2.3 positive allosteric modulator in mice [PDF]

, 2023
Rationale There is currently no treatment for spinocerebellar ataxias (SCAs), which are a group of genetic disorders that often cause a lack of coordination, difficulty walking, slurred speech, tremors, and eventually death.
Zhang, Miao, Nam, Young-Woo, Chandrashekar, Devaraj Venkatapura, Mehvar, Reza, Rahman, Mohammad Asikur, Young‐Woo Nam, Syed, Basir, Hamidreza Montazeri Aliabadi, Reza Mehvar, Montazeri Aliabadi, Hamidreza, Basir Syed, Mohammad Asikur Rahman, David Salehi, Miao Zhang, Salehi, David, Devaraj Venkatapura Chandrashekar   +15 more
core   +1 more source

The positive allosteric modulator of NMDA receptors, GNE‐9278, blocks the ethanol‐induced decrease of excitability in developing retrosplenial cortex neurons from mice

Neuropsychopharmacology Reports, 2023
Binge‐like exposure to ethanol during the brain growth spurt triggers apoptotic neurodegeneration in multiple brain regions, including the retrosplenial cortex, a brain region that is part of the hippocampal‐diencephalic‐cingulate memory network. This is
Clark W. Bird, Carlos F. Valenzuela
doaj   +1 more source

A novel small positive allosteric modulator of neuropeptide receptor PAC1-R exerts neuroprotective effects in MPTP mouse Parkinson’s disease model

Acta Biochimica et Biophysica Sinica, 2022
As a neuropeptide pituitary adenylate cyclase-activating polypeptide (PACAP)-preferring receptor, PAC1-R mediates effective neuroprotective activity.
Fan Guangchun, Chen Shang, Tao Zhengxin, Zhang Huahua, Yu Rongjie   +4 more
doaj   +1 more source

The GABAB Positive Allosteric Modulator ADX71441 Attenuates Alcohol Self-Administration and Relapse to Alcohol Seeking in Rats

Neuropsychopharmacology, 2017
GABAergic signaling is involved in modulating the reinforcing properties of alcohol, and GABA(B) receptors have been proposed as a potential target for clinical treatment of alcoholism.
E. Augier, R. Dulman, Ruslan Damadzic, Andrew Pilling, J. P. Hamilton, M. Heilig   +5 more
semanticscholar   +2 more sources

An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor [PDF]

, 2020
Most drugs acting on G-protein-coupled receptors target the orthosteric binding pocket where the native hormone or neurotransmitter binds. There is much interest in finding allosteric ligands for these targets because they modulate physiologic signaling ...
Hirata, Kunio, Kobilka, Brian K, Liu, Xiangyu, Magdalena Korczynska, Xu, Xinyu, Stanek, Markus, Matt, Rachel Ann, Shoichet, Brian K, Stößel, Anne, Jake Mahoney, Xiangyu Liu, Brian K. Shoichet, Clark, Mary J, Harald Hübner, Kaindl, Jonas, Hübner, Harald, Peter Gmeiner, Sunahara, Roger K, Markus Stanek, Daniela Dengler, Korczynska, Magdalena, Dengler, Daniela, Kunio Hirata, Roger K. Sunahara, Mahoney, Jake, Xinyu Xu, Gmeiner, Peter, Anne Stößel, Brian K. Kobilka, Jonas Kaindl, Rachel Ann Matt, Mary J. Clark   +31 more
core   +1 more source

Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer

eLife, 2017
GPCRs play critical roles in cell communication. Although GPCRs can form heteromers, their role in signaling remains elusive. Here we used rat metabotropic glutamate (mGlu) receptors as prototypical dimers to study the functional interaction between each
Junke Liu, Zongyong Zhang, David Moreno-Delgado, James AR Dalton, Xavier Rovira, Ana Trapero, Cyril Goudet, Amadeu Llebaria, Jesús Giraldo, Qilin Yuan, Philippe Rondard, Siluo Huang, Jianfeng Liu, Jean-Philippe Pin   +13 more
doaj   +1 more source

Apigenin and Structurally Related Flavonoids Allosterically Potentiate the Function of Human α7-Nicotinic Acetylcholine Receptors Expressed in SH-EP1 Cells

Cells, 2021
Phytochemicals, such as monoterpenes, polyphenols, curcuminoids, and flavonoids, are known to have anti-inflammatory, antioxidant, neuroprotective, and procognitive effects.
Waheed Shabbir, Keun-Hang Susan Yang, Bassem Sadek, Murat Oz   +3 more
doaj   +1 more source

Flavonoids as positive allosteric modulators of α7 nicotinic receptors

Neuropharmacology, 2019
The use of positive allosteric modulators (PAM) of α7 nicotinic receptors is a promising therapy for neurodegenerative, inflammatory and cognitive disorders. Flavonoids are polyphenolic compounds showing neuroprotective, anti-inflammatory and pro-cognitive actions. Besides their well-known antioxidant activity, flavonoids trigger intracellular pathways
Beatriz Elizabeth Nielsen, Isabel Bermudez, Cecilia Bouzat   +2 more
openaire   +4 more sources

Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y4 Receptor Positive Allosteric Modulator VU0506013

, 2023
Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y4 Receptor Positive Allosteric Modulator ...
Y Du (6951416), HM Cox (14474847), CD Weaver (16651125), J Meiler (13321746), J Stichel (13321740), AG Beck-Sickinger (14474886), NM Mishra (7807733), IR Tough (14474838), C Schüß (13321830), O Vu (16651122), KA Emmitte (16651128)   +10 more
core   +1 more source

Indomethacin Enhances Type 1 Cannabinoid Receptor Signaling

Frontiers in Molecular Neuroscience, 2019
In addition to its known actions as a non-selective cyclooxygenase (COX) 1 and 2 inhibitor, we hypothesized that indomethacin can act as an allosteric modulator of the type 1 cannabinoid receptor (CB1R) because of its shared structural features with the ...
Robert B. Laprairie, Robert B. Laprairie, Kawthar A. Mohamed, Ayat Zagzoog, Melanie E. M. Kelly, Melanie E. M. Kelly, Lesley A. Stevenson, Roger Pertwee, Eileen M. Denovan-Wright, Ganesh A. Thakur   +9 more
doaj   +1 more source