Results 21 to 30 of about 40,413 (202)

Acetylcholine Receptor Stimulation Activates Protein Kinase C Mediated Internalization of the Dopamine Transporter

Frontiers in Cellular Neuroscience, 2021
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

Selective M5 muscarinic acetylcholine receptor negative allosteric modulator VU6008667 blocks acquisition of opioid self-administration.

Neuropharmacology, 2023
Recent evidence suggests that inhibition of the M5 muscarinic acetylcholine receptor (mAChR) may provide a novel non-opioid mechanism for the treatment of opioid use disorder (OUD).
Laura B. Teal, M. Bubser, Edith Duncan, Robert W. Gould, C. Lindsley, Carrie K. Jones   +5 more
semanticscholar   +1 more source

N-Arachidonoyl-phosphatidylethanolamide phospholipase D activation by muscarinic receptors. [PDF]

J Physiol
Abstract figure legend Activating muscarinic M3 receptors activates Gq‐pathway signalling, including the activation of phospholipase C (PLC) and release of calcium from internal stores as shown in the upper panel. It remains unclear whether the calcium acts on N‐arachidonoyl‐phosphatidylethanolamide phospholipase D (NAPE‐PLD) itself or upstream at N ...
Murataeva N, Schmitt C, Hyman E, Wager-Miller J, Matthews I, Cai R, Cai S, Li Y, Mackie K, Straiker A.   +9 more
europepmc   +2 more sources

Chronic Loss of Muscarinic M5 Receptor Function Manifests Disparate Impairments in Exploratory Behavior in Male and Female Mice despite Common Dopamine Regulation

Journal of Neuroscience, 2022
There are five cloned muscarinic acetylcholine receptors (M1–M5). Of these, the muscarinic type 5 receptor (M5) is the only one localized to dopamine neurons in the ventral tegmental area and substantia nigra. Unlike M1–M4, the M5 receptor has relatively
John A. Razidlo, Skylar Fausner, Anna E. Ingebretson, Liuchang Wang, Christopher L. Petersen, Salahudeen Mirza, Isabella N. Swank, Veronica A. Alvarez, Julia C. Lemos   +8 more
semanticscholar   +1 more source

Expression of muscarinic acetylcholine receptors M3 and M5 in osteoporosis [PDF]

Medical Science Monitor, 2014
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, Lips, Katrin Susanne, Heiss, Christian, Schnettler, Reinhard   +3 more
openaire   +2 more sources

Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.

Journal of Medicinal Chemistry, 2022
The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) represents a novel potential target for the treatment of multiple addictive disorders, including opioid use disorder.
Aaron T. Garrison, Douglas L. Orsi, Rory A. Capstick, David Whomble, Jinming Li, Trever R. Carter, Andrew S. Felts, P. Vinson, Alice L. Rodriguez, Allie Han, Krishma Hajari, Hyekyung P. Cho, Laura B. Teal, Madeline G Ragland, M. Ghamari-Langroudi, M. Bubser, Si-Chen Chang, N. Schnetz-Boutaud, O. Boutaud, A. L. Blobaum, Daniel J. Foster, C. Niswender, P. Conn, C. Lindsley, Carrie K. Jones, Changho Han   +25 more
semanticscholar   +1 more source

Novel Allosteric Effects of Amiodarone at the Muscarinic M5 Receptor [PDF]

The Journal of Pharmacology and Experimental Therapeutics, 2010
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
openaire   +2 more sources

Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor

ACS Chemical Neuroscience, 2021
The M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders.
Wessel A. C. Burger, P. R. Gentry, Alice E. Berizzi, Ziva Vuckovic, E. T. van der Westhuizen, G. Thompson, M. Yeasmin, C. Lindsley, P. Sexton, C. Langmead, A. Tobin, A. Christopoulos, C. Valant, D. Thal   +13 more
semanticscholar   +1 more source

A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity

Pharmaceutics, 2023
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, Ana C. Cabral, Manuel T. Veríssimo, Fernando Fernandez-Llimos, Isabel V. Figueiredo, M. Margarida Castel-Branco   +5 more
doaj   +1 more source

Multitargeting nature of muscarinic orthosteric agonists and antagonists

Frontiers in Physiology, 2022
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