Results 21 to 30 of about 18,462 (237)

Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100 [PDF]

Neuropsychopharmacology, 2014
Nellie Byun, Michael Grannan, Michael Bubser, Robert Barry, Analisa D. Thompson, John Rosanelli, Raajaram Gowrishankar, Nathaniel D. Kelm, Stephen Damon, Thomas M. Bridges, Bruce J. Melancon, James C. Tarr, John T. Brogan, Malcolm J. Avison, Ariel Y. Deutch, Jürgen Wess, Michael R. Wood, Craig W. Lindsley, John C. Gore, P. Jeffrey Conn, Carrie K. Jones   +20 more
openalex   +2 more sources

Clozapine is responsible for the in vivo imaging and pharmacological effects of clozapine-N-oxide in murine DREADD models [PDF]

Frontiers in Pharmacology
Although clozapine-N-oxide (CNO), a major metabolite of clozapine (CLZ), is a widely used agonist of designer receptors exclusively activated by designer drugs (DREADDs), the compound responsible for visualizing or activating DREADDs in nuclear medicine ...
Jian Wang, Jian Wang, Jian Wang, Jiale Qin, Katsushi Kumata, Ming-Rong Zhang, Jun Qian, Jun Qian, Jun Qian, Wen Zhou, Bin Ji, Bin Ji, Bin Ji, Bin Ji, Bin Ji   +14 more
doaj   +2 more sources

Structural and Dynamic Mechanisms of Allostery at the M4 Muscarinic Acetylcholine Receptor

Social Science Research Network, 2022
Ziva Vuckovic, Jinan Wang, Vi Pham, Jesse I. Mobbs, Matthew J. Belousoff, Apurba Bhattarai, Wessel A. C. Burger, Geoff Thompson, Mahmuda Yeasmin, Vindhya Nawaratne, Katie Leach, Emma T. van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W. Lindsley, Andrew B. Tobin, Patrick M. Sexton, Radostin Danev, Céline Valant, Yinglong Miao, Arthur Christopoulos, David M. Thal   +23 more
openalex   +2 more sources

Downstream Signaling of Muscarinic M₄ Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]

Pharmacol Res Perspect
ABSTRACT 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, Playle C, Palchaudhuri M, Hucke O, Gross U, Ursu D.   +5 more
europepmc   +2 more sources

Mechanisms of Pilocarpine-Induced Nitric Oxide and Prostaglandin Production in Porcine Ciliary Muscle. [PDF]

FASEB Bioadv
Pilocarpine activates M1 and M3 muscarinic receptors in porcine ciliary muscle, engaging calcium‐dependent phospholipase C (PLC), nitric oxide synthase (NOS), and cyclooxygenase (COX) pathways that increase prostaglandin E2 (PGE2) synthesis. Beyond nitric oxide (NO) modulation, PGE2 emerges as a key mediator linking muscarinic signaling to ciliary ...
Benozzi G, Quinteros Villarruel E, Zuluaga AF, Orman B.   +3 more
europepmc   +2 more sources

The M4 muscarinic acetylcholine receptor positive allosteric modulator VU0467154 normalizes non‐rapid eye movement sleep deficits in non‐pathologically aged mice.

Alzheimer's & Dementia, 2023
The central cholinergic system plays an important role in normal arousal and sleep/wake architecture, and is known to decline in non‐pathological aging and Alzheimer’s disease (AD).
Jason K. Russell, Laura Wan, Shalonda Ingram, M. Bubser, C. Lindsley, Carrie K Jones   +5 more
semanticscholar   +1 more source

Anti-inflammation of spirocyclopiperazinium salt compound LXM-10 targeting α7 nAChR and M4 mAChR and inhibiting JAK2/STAT3 pathway in rats. [PDF]

PLoS ONE, 2013
The present study aims to investigate the therapeutic effects of LXM-10 by intragastric administration in both acute and chronic inflammatory models, and to explore the underlying molecular mechanisms.
Weiwei Zhang, Qi Sun, Xiaoli Gao, Yimin Jiang, Runtao Li, Jia Ye   +5 more
doaj   +1 more source

Allosteric Modulators of the M4 Muscarinic Acetylcholine Receptor

ACS Medicinal Chemistry Letters, 2017
Robert B. Kargbo
openalex   +3 more sources

The Neuropathology of Alcohol Use Disorder: Cellular Insights From Human Post-Mortem Studies. [PDF]

J Neurochem
Major cellular changes in alcohol use disorder human post‐mortem brain. Alcohol use disorder (AUD) is a complex neurological disorder that undergoes neural changes, mainly degeneration and or cellular alterations impacting addiction behaviours. Key brain regions implicated in AUD are the cortex, striatum, corpus callosum, hippocampus, hypothalamus ...
Rasool AE, Cornish JL, Prasad AA.
europepmc   +2 more sources

Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR

Nature Communications, 2023
The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of high therapeutic interest due to its expression in regions of the brain involved in the regulation of psychosis, cognition, and addiction.
Wessel A. C. Burger, Vi Pham, Ziva Vuckovic, Alexander S. Powers, Jesse I. Mobbs, Yianni Laloudakis, Alisa Glukhova, Denise Wootten, Andrew B. Tobin, Patrick M. Sexton, Steven M. Paul, Christian C. Felder, Radostin Danev, Ron O. Dror, Arthur Christopoulos, Celine Valant, David M. Thal   +16 more
doaj   +1 more source