Results 21 to 30 of about 5,023 (210)

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). Previous studies from our group and others have demonstrated that acute administration of the long-acting M5 negative allosteric modulator (NAM) ML375 attenuates ...
Laura B. Teal, Michael Bubser, Edith Duncan, Robert W. Gould, Craig W. Lindsley, Carrie K. Jones   +5 more
openalex   +3 more sources

Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M1 – M5 muscarinic acetylcholine receptors [PDF]

Bioorganic & Medicinal Chemistry Letters, 2018
Novel quinuclidinyl N-phenylcarbamate analogs were synthesized, and binding affinities at M1-M5 muscarinic acetylcholine receptor (mAChR) subtypes were determined using Chinese hamster ovary (CHO) cell membranes stably expressing one specific subtype of human mAChR. Although not subtype selective, the lead analog (±)-quinuclidin-3-yl-(4-fluorophenethyl)
Nara Lee, G. Satheesh, Shobanbabu Bommagani, Kiranbabu Siripurapu, Guangrong Zheng, Linda P. Dwoskin   +5 more
openalex   +4 more sources

P2‐207: Discovery of a highly M5‐preferring muscarinic acetylcholine receptor allosteric potentiator [PDF]

Alzheimer's & Dementia, 2009
Thomas M. Bridges, Joy E. Marlo, Colleen M. Niswender, Patrick R. Gentry, C. David Weaver, P. Jeffrey Conn, Craig W. Lindsley   +6 more
openalex   +3 more sources

Light-Activated Pharmacological Tools for Exploring the Cholinergic System. [PDF]

Med Res Rev
ABSTRACT Cholinergic transmission plays a critical role in both the central and peripheral nervous systems, affecting processes such as learning, memory, and inflammation. Conventional cholinergic drugs generally suffer from poor selectivity and temporal precision, leading to undesired effects and limited therapeutic efficacy. Photopharmacology aims to
Colleoni A, Galli G, Dallanoce C, De Amici M, Gorostiza P, Matera C.   +5 more
europepmc   +2 more sources

Muscarinic—but Not Nicotinic—Acetylcholine Receptors Mediate a Nitric Oxide-Dependent Dilation in Brain Cortical Arterioles: A Possible Role for the M5 Receptor Subtype [PDF]

Journal of Cerebral Blood Flow & Metabolism, 2000
Increases in cortical cerebral blood flow are induced by stimulation of basal forebrain cholinergic neurons. This response is mediated in part by nitric oxide (NO) and reportedly involves both nicotinic and muscarinic receptors, some of which are possibly located in the vessel wall.
Ahmed Elhusseiny, Édith Hamel
openalex   +3 more sources

Crystal structure of the M₅ muscarinic acetylcholine receptor [PDF]

Proceedings of the National Academy of Sciences, 2019
AbstractThe human M5 muscarinic acetylcholine receptor (mAChR) has recently emerged as an exciting therapeutic target for treating a range of disorders, including drug addiction. However, a lack of structural information for this receptor subtype has limited further drug development and validation.
Patrick M. Sexton, Patrick M. Sexton, Wessel A.C. Burger, Kunio Hirata, Christopher J. Langmead, Raphaël Rahmani, Geoff Thompson, Swapna Varghese, Craig W. Lindsley, Celine Valant, Patrick R. Gentry, Arthur Christopoulos, Jonathan B. Baell, Andrew B. Tobin, David M. Thal, Alice E. Berizzi, Emma T van der Westhuizen, Ziva Vuckovic   +17 more
openaire   +6 more sources

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators [PDF]

Molecular Pharmacology, 2016
Recently, the first subtype-selective allosteric modulators of the M5 muscarinic acetylcholine receptor (mAChR) have been described, but their molecular mechanisms of action remain unknown. Using radioligand-binding and functional assays of inositol phosphate (IP) accumulation and Ca(2+) mobilization in a recombinant cell line stably expressing the ...
Sandra Den Hoedt, Alice E. Berizzi, Patrick R. Gentry, Patrick M. Sexton, Christopher J. Langmead, Arthur Christopoulos, Patricia Rueda   +6 more
openaire   +2 more sources

Synergistic Antiemetic Effects of Nerolidol on Domperidone, Hyoscine, and Ondansetron: In Vivo and in Silico Investigations on Receptor Binding Affinity. [PDF]

ChemistryOpen
Nerolidol shows prominent antiemetic activity and mitigates CuSO4.H2O‐mediated retching in chicks efficiently through its peripheral action. Additionally, the in silico studies have also shown possible antiemetic effects with greater binding affinity against muscarinic (specially, M2 and M3) and dopaminergic receptors.
Ghosh Situ S, Bhuia MS, Chowdhury R, Al Hasan S, Akber Ansari S, Aamer Ansari I, Ali A, Torequl Islam M.   +7 more
europepmc   +2 more sources

Autonomic Nervous System in Bone Remodeling: From Mechanisms to Novel Therapies in Orthopedic Diseases. [PDF]

Orthop Surg
Due to the close connection between the autonomic nervous system and skeletal system, large amounts of evidence have shown that neuromodulation plays a crucial role in regulating bone metabolism. Clinically, neuromodulation has exhibited promising therapeutic effects in treating joint disorders by significantly reducing inflammation and clinical scores.
Xia R, Peng H, Zhu X, Suolang W, Pambayi STL, Yang X, Zeng Y, Shen B.   +7 more
europepmc   +2 more sources

Acetylcholine and spinal locomotor networks: The insider

Physiological Reports, 2021
This article aims to review studies that have investigated the role of neurons that use the transmitter acetylcholine (ACh) in controlling the operation of locomotor neural networks within the spinal cord. This cholinergic system has the particularity of
Théo Mille, Camille Quilgars, Jean‐René Cazalets, Sandrine S. Bertrand   +3 more
doaj   +1 more source