Results 21 to 30 of about 5,170 (209)

A Molecular Mechanism for Endocytic Recycling of the M5 Muscarinic Acetylcholine Receptor

, 2010
A thesis presented to the faculty of The Rockefeller University in partial fulfillment of the requirements for the degree of Doctor of ...
Jacob Bendor
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

The M5 muscarinic acetylcholine receptor third intracellular loop regulates receptor function and oligomerization

Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, 2010
Besides some pharmacological, biochemical and biophysical evidences support the contention that muscarinic acetylcholine receptors can form homo- and heterodimers, the existence of specific M3 and M5 muscarinic receptors oligomers in living cells is a new concept.
Dasiel O. Borroto‐Escuela, Gloria García-Negredo, Pere Garriga, Kjell Fuxé, Francisco Ciruela   +4 more
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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.
Ziva Vuckovic, Patrick R. Gentry, Alice E. Berizzi, Kunio Hirata, Swapna Varghese, Geoff Thompson, Emma T. van der Westhuizen, Wessel A.C. Burger, Raphaёl Rahmani, Celine Valant, Christopher J. Langmead, Craig W. Lindsley, Jonathan Baell, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos, David M. Thal   +16 more
openaire   +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

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

Assessment of Quercetin Antiemetic Properties: In Vivo and In Silico Investigations on Receptor Binding Affinity and Synergistic Effects

Plants, 2023
Quercetin (QUA), a flavonoid compound, is ubiquitously found in plants and has demonstrated a diverse range of biological activities. The primary objective of the current study is to assess the potential antiemetic properties of QUA using an in vivo and ...
Raihan Chowdhury, Md. Shimul Bhuia, Asraful Islam Rakib, Rubel Hasan, Henrique Douglas Melo Coutinho, Isaac Moura Araújo, Irwin Rose Alencar de Menezes, Muhammad Torequl Islam   +7 more
doaj   +1 more source

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
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., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Identification and Role of Muscarinic Receptor Subtypes Expressed in Rat Adrenal Medullary Cells

Journal of Pharmacological Sciences, 2011
.: The muscarinic receptor is known to be involved in the acetylcholine (ACh)-induced secretion of catecholamines in the adrenal medullary (AM) cells of various mammals.
Keita Harada, Hidetada Matsuoka, Takeyoshi Sata, Akira Warashina, Masumi Inoue   +4 more
doaj   +1 more source

Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]

, 2016
Pulmonary hypertension (PH) is a complex disease comprising a pathologic remodeling and thickening of the pulmonary vessels causing an after load on the right heart ventricle that can result in ventricular failure. Triggered by oxidative stress, episodes
Ahmed, Mohamed, Al-Abed, Yousef, Coleman, Thomas, Lakshminrusimha, Satyanarayana, Patel, Hardik, VanPatten, Sonya   +5 more
core   +2 more sources