Downstream Signaling of Muscarinic M<sub>4</sub> Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]
Pharmacol Res PerspectABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M +5 more
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Nicotine receptor partial agonists for smoking cessation [PDF]
Sao Paulo Medical Journal, 2007 Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). Varenicline was developed as a nicotine receptor partial agonist from cytisine, a drug widely used in central
Cahill, Kate +3 more
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Nicotine receptor partial agonists for smoking cessation
Cochrane Database of Systematic Reviews, 2023 Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). This is an update of a Cochrane Review first published in 2007.To assess the effectiveness of nicotine ...
Livingstone-Banks, J +6 more
openaire +4 more sources
TC299423, a Novel Agonist for Nicotinic Acetylcholine Receptors [PDF]
Frontiers in Pharmacology, 2017 (E)-5-(Pyrimidin-5-yl)-1,2,3,4,7,8-hexahydroazocine (TC299423) is a novel agonist for nicotinic acetylcholine receptors (nAChRs). We examined its efficacy, affinity, and potency for α6β2∗ (α6β2-containing), α4β2∗, and α3β4∗ nAChRs, using [125I]-epibatidine binding, whole-cell patch-clamp recordings, synaptosomal 86Rb+ efflux, [3H]-dopamine release, and
Teagan R. Wall +12 more
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Cholinergic modulation of dopamine overflow in the rat neostriatum: A fast cyclic voltammetric study in vitro [PDF]
, 1994 Stimulus-evoked dopamine overflow in rat neostriatal slices was determined using fast cyclic voltammetry. The dopamine efflux induced by intrastriatal stimulation increased with stimulus intensity and was found to be enhanced by more than 100% upon ...
Kudernatsch, Martina, Sutor, Bernd
core +1 more source
Nicotine receptor partial agonists for smoking cessation [PDF]
Cochrane Database of Systematic Reviews, 2016 Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist).To review the efficacy of nicotine receptor partial agonists, including varenicline and cytisine, for smoking ...
Cahill, Kate +4 more
openaire +5 more sources
Alpha9 nicotinic acetylcholine receptors and the treatment of pain [PDF]
, 2009 Chronic pain is a vexing worldwide problem that causes substantial disability and consumes significant medical resources. Although there are numerous analgesic medications, these work through a small set of molecular mechanisms.
Absalom, Nathan +4 more
core +1 more source
Reward learning as a potential target for pharmacological augmentation of cognitive remediation for schizophrenia: a roadmap for preclinical development. [PDF]
, 2013 RationaleImpaired cognitive abilities are a key characteristic of schizophrenia. Although currently approved pharmacological treatments have demonstrated efficacy for positive symptoms, to date no pharmacological treatments successfully reverse cognitive
Acheson, Dean T +2 more
core +2 more sources
Regions of beta 2 and beta 4 responsible for differences between the steady state dose-response relationships of the alpha 3 beta 2 and alpha 3 beta 4 neuronal nicotinic receptors [PDF]
, 1995 We constructed chimeras of the rat beta 2 and beta 4 neuronal nicotinic subunits to locate the regions that contribute to differences between the acetylcholine (ACh) dose-response relationships of the alpha 3 beta 2 and alpha 3 beta 4 receptors ...
Cohen, B. N. +5 more
core +2 more sources
Identification of critical residues in loop E in the 5-HT(3AS)R binding site [PDF]
, 2002 BACKGROUND: The serotonin type 3 receptor (5-HT(3)R) is a member of a superfamily of ligand gated ion channels. All members of this family share a large degree of sequence homology and presumably significant structural similarity.
Joshi, Prasad R +4 more
core +3 more sources