Results 31 to 40 of about 4,995,094 (293)

Contrasting properties of α7-selective orthosteric and allosteric agonists examined on native nicotinic acetylcholine receptors. [PDF]

PLoS ONE, 2013
Subtype-selective ligands are important tools for the pharmacological characterisation of neurotransmitter receptors. This is particularly the case for nicotinic acetylcholine receptors (nAChRs), given the heterogeneity of their subunit composition.
JasKiran K Gill, Anna Chatzidaki, Daniel Ursu, Emanuele Sher, Neil S Millar   +4 more
doaj   +1 more source

Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia

Nature Communications, 2023
TRPV1 as a drug target suffers from side effects of hypothermia. Here, authors engineer a peptide, sRhTx, as a positive allosteric modulator of TRPV1 channel. It potentiates the activity of TRPV1 to reversibly ablate pain-sensing nerve terminals for long-
Heng Zhang, Jia-Jia Lin, Ya-Kai Xie, Xiu-Zu Song, Jia-Yi Sun, Bei-Lei Zhang, Yun-Kun Qi, Zhen-Zhong Xu, Fan Yang   +8 more
doaj   +1 more source

Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. [PDF]

, 2015
The mediodorsal thalamus (MD) likely plays an important role in cognition as it receives abundant afferent connections from the amygdala and prefrontal cortex (PFC).
Salt, T.E., Copeland, C.S., Neale, S.A., Neale, SA, Salt, TE, Copeland, CS   +5 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

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

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

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

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

De Novo Design of Peptidic Positive Allosteric Modulators Targeting TRPV1 with Analgesic Effects

Advanced Science, 2021
Transient receptor potential vanilloid 1 (TRPV1) ion channel is a nociceptor critically involved in pain sensation. Direct blockade of TRPV1 exhibits significant analgesic effects but also incurs severe side effects such as hyperthermia, causing failures
Lizhen Xu, Heng Zhang, Yunfei Wang, Xiancui Lu, Zhenye Zhao, Cheng Ma, Shilong Yang, Vladimir Yarov‐Yarovoy, Yuhua Tian, Jie Zheng, Fan Yang   +10 more
doaj   +1 more source

Positive Allosteric Modulator of GABA Lowers BOLD Responses in the Cingulate Cortex. [PDF]

PLoS ONE, 2016
Knowledge about the neural underpinnings of the negative blood oxygen level dependent (BOLD) responses in functional magnetic resonance imaging (fMRI) is still limited.
Susanna A Walter, Mikael Forsgren, Karin Lundengård, Rozalyn Simon, Maritha Torkildsen Nilsson, Birgitta Söderfeldt, Peter Lundberg, Maria Engström   +7 more
doaj   +1 more source