Results 51 to 60 of about 15,450 (220)

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

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor [PDF]

, 2014
Background: Selective and potent positive allosteric modulators (PAMs) of the M1 mAChR have been recently described. Results: Use of structural analogues and mutagenic mapping identified the mechanistic basis for increased PAM activity.
Abdul-Ridha, Byun, Canals, Christopoulos, Conn, Conn, Dror, Foster, Haga, Hulme, Jones, Katritch, Kenakin, Kennedy, Keov, Kruse, Kruse, Kruse, Kuduk, Kuduk, Kuduk, Lazareno, Leach, Leach, Lebois, Lebon, Ma, Matsui, May, Melancon, Mistry, Motulsky, Nathan, Nawaratne, Nickols, Phillips, Ragnarsson, Shirey, Shonberg, Stevens, Tarr, Valant, Venkatakrishnan   +42 more
core   +2 more sources

Effect of green flickering light on myopia development and expression of M1 muscarinic acetylcholine receptor in guinea pigs [PDF]

International Journal of Ophthalmology, 2018
AIM: To investigate the effects of green flickering light on refractive development and expression of muscarinic acetylcholine receptor (mAChR) M1 in the eyes of guinea pigs.
Yuan Tao, Xiao-Li Li, Li-Yuan Sun, Yu-Hua Wei, Xiao-Ting Yu, Hong Wang   +5 more
doaj   +1 more source

Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias

Frontiers in Pharmacology, 2021
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen, K. H. Christopher Choy, Celine Valant, Simon McKenzie-Nickson, Sophie J. Bradley, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos   +7 more
doaj   +1 more source

Mir-34a-5p Mediates Cross-Talk between M2 Muscarinic Receptors and Notch-1/EGFR Pathways in U87MG Glioblastoma Cells: Implication in Cell Proliferation [PDF]

, 2018
Glioblastoma (GBM) is the most aggressive human brain tumor. The high growth potential and decreased susceptibility to apoptosis of the glioma cells is mainly dependent on genetic amplifications or mutations of oncogenic or pro-apoptotic genes ...
Bevilacqua, Valeria, Caffarelli, Elisa, De Jaco, Antonella, Di Bari, Maria, Laneve, Pietro, Piovesana, Roberta, Talora, Claudio, Tata, Ada Maria, Trobiani, Laura   +8 more
core   +2 more sources

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of 18F‐Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3

ChemMedChem, EarlyView.
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Miguel A. Herrera‐Rueda, Maxwell A. Boateng, Melinda Wuest, Frederick G. West, Frank Wuest   +4 more
wiley   +1 more source

Pharmacological evaluation of the long-term effects of xanomeline on the M(1) muscarinic acetylcholine receptor. [PDF]

PLoS ONE, 2010
Xanomeline is a unique agonist of muscarinic receptors that possesses functional selectivity at the M(1) and M(4) receptor subtypes. It also exhibits wash-resistant binding to and activation of the receptor.
Marianne K O Grant, Meredith J Noetzel, Kayla C De Lorme, Jan Jakubík, Vladimír Doležal, Esam E El-Fakahany   +5 more
doaj   +1 more source

A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization [PDF]

, 2017
The dopamine D3 receptor (D3R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a ...
Caltabiano, Gianluigi, Jiménez-Rosés, Mireia, Marsango, Sara, Millan, Mark J., Milligan, Graeme, Pediani, John D., Ward, Richard J.   +6 more
core   +2 more sources

Status epilepticus: Updates on mechanisms and treatments

Epilepsia Open, EarlyView.
Abstract Status epilepticus (SE) consists of prolonged, self‐sustaining seizures and is a common neurological emergency that causes respiratory compromise and neuronal injury. Without prompt treatment, the seizures can become resistant to benzodiazepines, leading to the progressive evolution of established, refractory, and super‐refractory SE.
Suchitra Joshi, Jaideep Kapur
wiley   +1 more source

Presynaptic M1 muscarinic cholinoceptors mediate inhibition of excitatory synaptic transmission in the hippocampus in vitro [PDF]

, 1990
The effects of the cholinoceptor agonist, carbachol (CCh), were examined in the rat hippocampal slice preparation. Intracellular recordings from CA1 pyramidal neurones revealed that CCh (1–3 μM) inhibited excitatory postsynaptic responses evoked by ...
Sheridan, Robert D., Sutor, Bernd
core   +1 more source