Results 131 to 140 of about 39,843 (183)

Characterization of Selective M5 Acetylcholine Muscarinic Receptor Modulators on Dopamine Signaling in the Striatum

The Journal of Pharmacology and Experimental Therapeutics, 2023
The type-5 muscarinic acetylcholine receptor (mAChR, M5) is almost exclusively expressed in dopamine (DA) neurons of the ventral tegmental area and substantia nigra pars compacta; therefore, they are ideally located to modulate DA signaling and underlying behaviors. However, the role of M5 in shaping DA release is still poorly characterized.
Vivien Zell, Greetje Teuns, Alexandra Stormy Needham, Sruti Mukherjee, Nathaniel Roscoe, Michelle Le, Lawrence Fourgeaud, Grace Woodruff, Anindya Bhattacharya, Mathieu Marella, Pascal Bonaventure, Wayne C. Drevets, Bartosz Balana   +12 more
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Activation mechanism of the M5 muscarinic acetylcholine receptor

Biophysical Journal, 2023
Lee Roy, A. De Velez, Jokent T. Gaza, Ricky B. Nellas   +3 more
openaire   +2 more sources

Evaluation of 1,2,5-thiadiazoles as modulators of M1/M5 muscarinic receptor subtypes

Bioorganic & Medicinal Chemistry, 2014
Abstract Studies have demonstrated the presence of allosteric binding sites on each of the muscarinic acetylcholine receptor (mAChR) subtypes. Since most drugs targeting muscarinic receptors bind to the highly conserved orthosteric binding site, they fail to achieve appreciable subtype selectivity. Targeting non-conserved allosteric sites may provide
Aditya Maheshwari, P.S.S. Rao, William S. Messer   +2 more
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An Improved Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor

Synfacts, 2022
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Acute food deprivation reverses morphine-induced locomotion deficits in M5 muscarinic receptor knockout mice

Behavioural Brain Research, 2013
Lesions of the pedunculopontine tegmental nucleus (PPT), one of two sources of cholinergic input to the ventral tegmental area (VTA), block conditioned place preference (CPP) for morphine in drug-naïve rats. M5 muscarinic cholinergic receptors, expressed by midbrain dopamine neurons, are critical for the ability of morphine to increase nucleus ...
Stephan, Steidl, Esther, Lee, David, Wasserman, John S, Yeomans   +3 more
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Muscarinic Acetylcholine Receptor M5

Definitions, 2020
Muscarinic acetylcholine receptor M5 (532 aa, ~60 kDa) is encoded by the human CHRM5 gene. This protein plays a role in both acetylcholine binding and G protein-coupled receptor signaling.
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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, Sichen 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

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. Gentry, Alice E. Berizzi, Ziva Vuckovic, E. T. van der Westhuizen, Geoff V. Thompson, M. Yeasmin, C. Lindsley, P. Sexton, C. Langmead, A. Tobin, A. Christopoulos, C. Valant, D. Thal   +13 more
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Allosteric regulation of cloned m1–m5 muscarinic receptor subtypes

Biochemical Pharmacology, 1991
Allosteric regulation of [3H]N-methylscopolamine [( 3H]NMS) and [3H]quinuclidinyl benzilate [( 3H]QNB) dissociation from the m1-m5 muscarinic receptor subtypes was examined in transfected CHO-K1 cells. Half-times of dissociation of [3H]NMS from cell membranes (at 23 degrees) ranged from less than 5 min for the m2 subtype to more than 60 min for the m5 ...
J, Ellis, J, Huyler, M R, Brann
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Neuronal muscarinic acetylcholine receptor subtype modulation of inspiratory bursting at hypoglossal motoneurons in developing neonatal mice in vitro

Physiology, 2023
Muscarinic acetylcholine receptor modulation contributes to changes in hypoglossal motoneuron excitability through pre- and post-synaptic effects, an important mechanism for regulation of airway tone during sleep.
S. Dudley, Tatum Banayat, Asha Kurup, Kellie T. Jeong, Sophia M. Koziol, Lori M. Buhlman, A. Revill   +6 more
semanticscholar   +1 more source