Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors

QR Code

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors

Positive allosteric modulators (PAMs) that target the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) are potential treatments for cognitive deficits in conditions such as Alzheimer's disease and schizophrenia. We recently reported novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one...

Full description

Bibliographic Details
Main Authors:	van der Westhuizen, Emma T., Spathis, Arthur, Khajehali, Elham, Jörg, Manuela, Mistry, Shailesh N., Capuano, Ben, Tobin, Andrew B., Sexton, Patrick M., Scammells, Peter J., Valant, Celine, Christopoulos, Arthur
Format:	Article
Language:	English
Published:	ASPET 2018
Subjects:	Acetylcholine receptors; Allosterism; Alzheimer's Disease; Biased agonism; Cholinergic pharmacology; Cognition; Drug discovery; G protein-coupled receptors (GPCRs); Muscarinic cholinergic receptors; Schizophrenia
Online Access:	https://eprints.nottingham.ac.uk/51358/

Similar Items

Functional studies of insecticides and acaricides acting on ligand-gated ion channels
by: Iqbal, Sofia
Published: (2019)

From a4ß2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design
by: Yu, L., et al.
Published: (2012)

An evaluation of DREADD receptor pharmacology in recombinant cells and astrocytes
by: Carpenter, Jessica
Published: (2020)

Inhibition of mammalian nicotinic acetylcholine receptors by philanthotoxin analogues is strongly influenced by subunit composition
by: Kachel, Hamid Saeid
Published: (2015)

4-Phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2015)

Insecticide resistance mediated 1 by an exon skipping event
by: Berger, Madeleine, et al.
Published: (2016)

Novel complementation biosensors to investigate G protein-coupled receptor kinetics and signalling bias
by: Dijon, Nicola C
Published: (2022)

Investigating cooperativity across adenosine A3 receptor homo- and hetero-oligomers
by: Groenewoud, N.J.A.
Published: (2019)

Effects of postbiotic and inulin supplements on growth performance, gut morphology, gene expression and fecal characteristics of broiler chicken
by: Karrem, Karwan Yaseen
Published: (2016)

Role of D1 receptor antagonism in contextual fear learning and memory
by: Heath, Florence
Published: (2015)

Biological significance of human epidermal growth factor receptor 2 (HER2) in breast cancer: effect of oestrogen receptor
by: Ahmad, Dena Akram Jerjees
Published: (2016)

Investigating the molecular basis of biased signalling at cannabinoid receptors
by: Dennis, Morgan Jane
Published: (2023)

Using super resolution microscopy to investigate the role of actin in adenosine receptor organisation
by: Garlick, Evelyn
Published: (2023)

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors
by: Sykes, David A., et al.
Published: (2017)

Effects of NAD at purine receptors in isolated blood vessels
by: Alefishat, Eman, et al.
Published: (2015)

Medicinal Chemistry & Chemical Biology Approaches to Investigate Prospective Treatments for CNS Diseases: Dopamine D1 Receptor Positive Allosteric Modulators, Dopamine D2 Receptor Positive & Negative Allosteric Modulators, Dopamine D2 Receptor-Ligand Kinetics
by: Fyfe, Tim
Published: (2019)

GPCRs through the keyhole: the role of protein flexibility in ligand binding to β-adrenoceptors
by: Emtage, Abigail L., et al.
Published: (2016)

Non-classical mechanisms of steroid sensing in the ovary: lessons from the bovine oxytocin model
by: Ivell, Richard, et al.
Published: (2014)

Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor
by: Mistry, Shailesh N., et al.
Published: (2016)

Exposure to non-kin females rapidly affects testicular morphology in non-reproductive male Damaraland mole-rats
by: Nice, P., et al.
Published: (2010)

Oleoylethanolamine and palmitoylethanolamine modulate intestinal permeability in vitro via TRPV1 and PPARα
by: Karwad, Mustafa A., et al.
Published: (2016)

The SEISICAT study: a pilot study assessing 1 efficacy and safety of spironolactone in cats with congestive heart failure secondary to cardiomyopathy
by: James, Rachel, et al.
Published: (2018)

Development of novel therapeutic agents designed to enhance insulin secretion through activation of the trace amine-associated receptor 1 (TAAR1)
by: Lenham, Rhianna
Published: (2025)

Investigating the SUMOylation and transcriptional regulation of Nurr1 and the splice variant Nurr-1a
by: Edey, Jade
Published: (2023)

Comparison of fecal hormone extraction methods and analysis on reproductive hormones in female Malayan tapirs
by: Ruslan, Muhammad Najib
Published: (2018)

Response of concentrate supplementation on ovulation rate and progesterone receptor gene in goats
by: Mohammed, Nur Hafizah
Published: (2018)

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)

Investigating ligand-directed signalling at the cannabinoid receptor 2
by: Hourani, Wafa
Published: (2019)

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist
by: Stoddart, Leigh A., et al.
Published: (2015)

Anti-nociceptive and desensitizing effects of olvanil on capsaicin-induced thermal hyperalgesia in the rat
by: Alsalem, Mohammad, et al.
Published: (2016)

The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA3 adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognition
by: Cheong, S., et al.
Published: (2010)

Identification and characterization of toll-like receptor (TLR) 2 and 4 mutations in colorectal
by: Davoodi, Homa
Published: (2009)

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor
by: Mistry, Shailesh N., et al.
Published: (2013)

The mannose receptor negatively modulates the Toll-like receptor 4–aryl hydrocarbon receptor–indoleamine 2,3-dioxygenase axis in dendritic cells affecting T helper cell polarization
by: Salazar, Fabián, et al.
Published: (2016)

Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603
by: Goulding, Joelle, et al.
Published: (2018)

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor
by: Abdul-Ridha, Alaa, et al.
Published: (2014)

Release currents of IP₃ receptor channel clusters and concentration profiles
by: Thul, Ruediger, et al.
Published: (2004)

Negative cooperativity across 1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 1-adrenoceptor binding conformation
by: Gherbi, Karolina, et al.
Published: (2015)

Androgen dependent mechanisms of pro-angiogenic networks in placental and tumor development
by: Metzler, Veronika M., et al.
Published: (2017)

Role of lectin receptors in recognition of Pseudomonas aeruginosa biofilms
by: Almuhanna, Yasir Saleh I
Published: (2021)