The dopamine transporter (DAT) clears neurotransmitters from the extracellular space and serves as an important regulator of signal amplitude and duration at sites of dopamine release. Several different intracellular signaling pathways have been observed
Suzanne M. Underhill, Susan G. Amara
doaj +1 more source
Expression of muscarinic acetylcholine receptors M3 and M5 in osteoporosis [PDF]
Cholinergic signaling via muscarinic acetylcholine receptors (mAChR) is known to influence various physiological functions. In bone, M3 mAChR and M5 mAChR were identified on the membrane of osteoblast-like cells. M3 mAChR seems to be particularly relevant for bone physiology, as signaling via this receptor was reported to increase bone formation and ...
Kauschke, Vivien +3 more
openaire +2 more sources
Novel Allosteric Effects of Amiodarone at the Muscarinic M5 Receptor [PDF]
Allosteric sites on muscarinic receptors may present superior therapeutic targets for several central nervous system disorders, due to the potential of allosteric ligands to provide more selective modulation and to preserve the spatiotemporal patterning that is characteristic of synaptic transmission.
Edward, Stahl, John, Ellis
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A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity
Anticholinergic burden tools have relevant pharmacological gaps that may explain their limited predictive ability for clinical outcomes. The aim of this study was to provide a universal pharmacological-based list of drugs with their documented affinity ...
Marta Lavrador +5 more
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Muscarinic M5 receptors modulate ethanol seeking in rats [PDF]
Despite the cost to both individual and society, alcohol use disorders (AUDs) remain a major health risk within society, and both relapse and heavy drinking are still poorly controlled with current medications. Here we demonstrate for the first time that a centrally active and selective negative allosteric modulator for the rat M5 muscarinic ...
Alice E. Berizzi +9 more
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Multitargeting nature of muscarinic orthosteric agonists and antagonists
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
doaj +1 more source
Ultrasonic vocalizations induced by sex and amphetamine in M2, M4, M5 muscarinic and D2 dopamine receptor knockout mice. [PDF]
Adult mice communicate by emitting ultrasonic vocalizations (USVs) during the appetitive phases of sexual behavior. However, little is known about the genes important in controlling call production.
Haoran Wang +4 more
doaj +1 more source
Voltage Dependence of Muscarinic M1-,M3- and M5 Receptors [PDF]
Muscarinic receptors (MR) are G protein-coupled receptors (GPCRs). Localized to the plasma membrane, they sense changes of the membrane potential and exhibit voltage-dependent signaling. Because voltage activates Gq-coupled receptors (e.g. M1R) but deactivates Gi-coupled receptors (e.g.
Rinne, Andreas +3 more
openaire +1 more source
Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype
Heterologous down-regulation of histamine H1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M1 –M5 ...
Katsuhiro Miyoshi +5 more
doaj +1 more source
Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J. +14 more
core +2 more sources

