The calcium-sensing receptor as a regulator of cellular fate in normal and pathological conditions [PDF]
, 2013 The calcium-sensing receptor (CaSR) belongs to the evolutionarily conserved family of plasma membrane G protein-coupled receptors (GPCRs). Early studies identified an essential role for the CaSR in systemic calcium homeostasis through its ability to ...
Benoit, Yves +3 more
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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 +13 more
doaj +1 more source
Cells, 2021 Phytochemicals, such as monoterpenes, polyphenols, curcuminoids, and flavonoids, are known to have anti-inflammatory, antioxidant, neuroprotective, and procognitive effects.
Waheed Shabbir +3 more
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Intracellular mechanisms underlying the nicotinic enhancement of LTP in the rat dentate gyrus [PDF]
, 2008 We have previously shown that activation of nicotinic acetylcholine receptors (nAChRs) enhanced long-term potentiation (LTP) in the rat dentate gyrus in vitro via activation of α7 nAChR. In the present studies, mechanisms underlying the acute and chronic
Abel +81 more
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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 +9 more
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Mode of action of the positive modulator PNU-120596 on alpha7 nicotinic acetylcholine receptors. [PDF]
, 2014 We investigated the mode of action of PNU-120596, a type II positive allosteric modulator of the rat alpha7 nicotinic acetylcholine receptor expressed by GH4C1 cells, using patch-clamp and fast solution exchange. We made two important observations: first,
Mike, Árpád +3 more
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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 +7 more
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Neuropeptide receptor positive allosteric modulation in epilepsy: Galanin modulation revealed [PDF]
Proceedings of the National Academy of Sciences, 2010 The therapeutic potential of neuropeptides has long been recognized; some successes have been registered, for example, in the tachykinin, endothelin, somatostatin, angiotensin, calcitonin gene-related peptide (CGRP), orexin, or glucagon-like peptide 1 (GLP1) fields (1), primarily in peripheral applications.
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Robust photoregulation of GABA(A) receptors by allosteric modulation with a propofol analogue. [PDF]
, 2012 Photochemical switches represent a powerful method for improving pharmacological therapies and controlling cellular physiology. Here we report the photoregulation of GABA(A) receptors (GABA(A)Rs) by a derivative of propofol (2,6-diisopropylphenol), a ...
Bruzik, Karol S +8 more
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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 +5 more
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