Results 61 to 70 of about 58,465 (248)

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

The Role of Orthosteric Building Blocks of Bitopic Ligands for Muscarinic M1 Receptors [PDF]

ACS Omega, 2020
The muscarinic M-1 acetylcholine receptor is an important drug target for the treatment of various neurological disorders. Designing M-1 receptor-selective drugs has proven challenging, mainly due to the high conservation of the acetylcholine binding site among muscarinic receptor subtypes.
Daniela Volpato, Michael Kauk, Regina Messerer, Marcel Bermudez, Gerhard Wolber, Andreas Bock, Carsten Hoffmann, Ulrike Holzgrabe   +7 more
openaire   +6 more sources

An Antibody Biosensor Establishes the Activation of the M1 Muscarinic Acetylcholine Receptor during Learning and Memory*♦

Journal of Biological Chemistry, 2016
Establishing the in vivo activation status of G protein-coupled receptors would not only indicate physiological roles of G protein-coupled receptors but would also aid drug discovery by establishing drug/receptor engagement.
Adrian J Butcher, S. Bradley, R. Prihandoko, Simon M. Brooke, A. Mogg, J. Bourgognon, Timothy Macedo-Hatch, J. Edwards, A. Bottrill, R. Challiss, L. Broad, C. Felder, A. Tobin   +12 more
semanticscholar   +1 more source

Effect of Mutated Cu, Zn Superoxide Dismutase (SOD1G93A) on Modulation of Transductional Pathway Mediated by M1 Muscarinic Receptor in SK-N-BE and NSC-34 Cells

Frontiers in Physiology, 2018
The constitutive secretion of antioxidant Cu-Zn Superoxide dismutase (SOD1) has been widely demonstrated in many cellular lines. In addition, we showed that as well as the basal SOD1 secretion, this enzyme is also exported through depolarization of ...
Simona Damiano, Anna Sasso, Roberta Accetta, Marcellino Monda, Bruno De Luca, Luigi Michele Pavone, Anna Belfiore, Mariarosaria Santillo, Paolo Mondola   +8 more
doaj   +1 more source

Relationship between membrane phosphatidylinositol-4,5-bisphosphate and receptor-mediated inhibition of native neuronal M channels [PDF]

, 2005
The relationship between receptor-induced membrane phosphatidylinositol-4'5'-bisphosphate (PIP2) hydrolysis and M-current inhibition was assessed in single-dissociated rat sympathetic neurons by simultaneous or parallel recording of membrane current and ...
Abogadie, FC, Brown, DA, Filippov, AK, Hughes, S, Marsh, SJ, Tatulian, L, Winks, JS   +6 more
core   +1 more source

Molecular Determinants of Allosteric Modulation at the M1 Muscarinic Acetylcholine Receptor [PDF]

Journal of Biological Chemistry, 2014
Benzylquinolone carboxylic acid (BQCA) is an unprecedented example of a selective positive allosteric modulator of acetylcholine at the M1 muscarinic acetylcholine receptor (mAChR). To probe the structural basis underlying its selectivity, we utilized site-directed mutagenesis, analytical modeling, and molecular dynamics to delineate regions of the M1 ...
Abdul-Ridha, Alaa, López, Laura, Keov, Peter, Thal, David M., Mistry, Shailesh N., Sexton, Patrick M., Lane, J. Robert, Canals, Meritxell, Christopoulos, Arthur   +8 more
openaire   +4 more sources

Elevated Hippocampal Cholinergic Neurostimulating Peptide precursor protein (HCNP-pp) mRNA in the amygdala in major depression [PDF]

, 2015
The amygdala is innervated by the cholinergic system and is involved in major depressive disorder (MDD). Evidence suggests a hyper-activate cholinergic system in MDD.
Argibay, Pablo, Bassi, Sabrina Cecilia, Seney, Marianne L., Sibille, Etienne   +3 more
core   +1 more source

Population Pharmacokinetic and Exposure‐Response Analysis of the Cognitive Effects of TAK‐071 in Participants With Parkinson Disease and Cognitive Impairment

Clinical Pharmacology in Drug Development, EarlyView.
Abstract TAK‐071 is a novel muscarinic M1 positive allosteric modulator under investigation for the treatment of cognitive impairment and falls associated with Parkinson disease (PD). This study evaluated population pharmacokinetics of TAK‐071 following single (1‐160 mg) and multiple (3‐15 mg once daily) oral‐dose TAK‐071 in 112 healthy participants ...
Hongxia Jia, Axel Facius, Rachel Jennings, Yaming Hang, Jaya Padmanabhan, Niraj M. Shanbhag, Brian T. Harel, Arthur Simen, Wei Yin   +8 more
wiley   +1 more source

Cholinergic Regulation of hnRNPA2/B1 Translation by M1 Muscarinic Receptors [PDF]

The Journal of Neuroscience, 2016
Cholinergic vulnerability, characterized by loss of acetylcholine (ACh), is one of the hallmarks of Alzheimer's disease (AD). Previous work has suggested that decreased ACh activity in AD may contribute to pathological changes through global alterations in alternative splicing.
Benjamin Kolisnyk, Mohammed A. Al-Onaizi, Jason Xu, Gustavo M. Parfitt, Valeriy G. Ostapchenko, Geula Hanin, Hermona Soreq, Marco A. M. Prado, Vania F. Prado   +8 more
openaire   +5 more sources

Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]

, 2003
Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio, Marinissen, Maria Julia, Offermanns, Stefan, Servitja, Joan-Marc, Simon, Melvin I.   +4 more
core   +1 more source