Naltrexone, Naloxone, Morphine, and Fentanyl Pharmacologically Chaperone a Mutant μ-Opioid Receptor via an Endoplasmic Reticulum Exit Site-Dependent Pathway. [PDF]
Pharmacol Res PerspectABSTRACT Opioid receptor antagonists increase the plasma membrane density of μ‐opioid receptors (MOR) in vivo, thereby inducing “supersensitivity” to opioid agonists. This phenomenon increases the risk of overdose in patients that were being treated with naltrexone (Ntx), a popular MOR antagonist.
Grant SN, Mulcahy MJ, Lester HA.
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Molecular pharmacology of an insect GABA receptor [PDF]
, 2010 Cys-loop receptors are ligand-gated ion channels that are involved in fast synaptic neurotransmission in the central and peripheral nervous system. The Cys-loop receptor RDL (‘resistant to dieldrin’) is a GABA-gated chloride channel from Drosophila ...
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Aspectos toxicológicos e químicos da Anatoxina-a e seus análogos
Química Nova, 2006 Anatoxin-a and its analogues are azabicyclic alkaloids that represent one of the most powerful nicotinic agonists known for the nicotinic acetylcholine receptor (nAChR). Because of this potent mechanism of action, anatoxin-a and its derivatives represent
Vania Rodríguez +4 more
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Heterogenous Cholinergic Nicotinic Receptors in the CNS
, 1988 Multiple nicotinic binding sites are found in mammalian brain. Several nicotinic agonists and antagonists have been used to characterize the nicotinic binding sites.
Nilsson, L +9 more
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Pharmaceuticals, 2020 Diabetes, obesity, atherosclerosis, and myocardial infarction are frequently co-morbid with major depressive disorder. In the current review, it is argued that vascular inflammation is a factor that is common to all disorders and that an endothelial ...
Hans O. Kalkman
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Differential Activation and Desensitization States Promoted by Noncanonical α7 Nicotinic Acetylcholine Receptor Agonists. [PDF]
, 2022 A series of dipicolyl amine pyrimidines (DPPs) were previously identified as potential α7 agonists by means of a calcium influx assay in the presence of the positive allosteric modulator (PAM) 1-(5-chloro-2,4-dimethoxy-phenyl)-3-(5-methyl-isoxazol-3-yl ...
Stokes, Clare +5 more
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Muscarinic and Nicotinic Contribution to Contrast Sensitivity of Macaque Area V1 Neurons
Frontiers in Neural Circuits, 2017 Acetylcholine is a neuromodulator that shapes information processing in different cortical and subcortical areas. Cell type and location specific cholinergic receptor distributions suggest that acetylcholine in macaque striate cortex should boost feed ...
Jose L. Herrero +2 more
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Nicotinic alpha 7 receptor agonists EVP-6124 and BMS-933043, attenuate scopolamine-induced deficits in visuo-spatial paired associates learning. [PDF]
PLoS ONE, 2017 Agonists at the nicotinic acetylcholine alpha 7 receptor (nAChR α7) subtype have the potential to treat cognitive deficits in patients with Alzheimer's disease (AD) or schizophrenia.
Michael R Weed +11 more
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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
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The role of neuronal nicotinic acetylcholine receptors in central cardiovascular regulation. [PDF]
, 2007 The central effect of nicotine on cardiovascular regulation has been extensively studied. However, due to its unselective nature for nicotinic acetylcholine receptors (nAChR) the involvement of specific nAChRs at sites in the brain, in central nervous ...
Moore, C.
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