British Journal of Pharmacology, EarlyView., 2023 Abstract Autism spectrum disorders (ASDs) are diagnosed in 1/100 children worldwide, based on two core symptoms: deficits in social interaction and communication, and stereotyped behaviours. G protein‐coupled receptors (GPCRs) are the largest family of cell‐surface receptors that transduce extracellular signals to convergent intracellular signalling ...
Anil Annamneedi +6 more
wiley +1 more source
Gαq signalling from endosomes: A new conundrum
British Journal of Pharmacology, EarlyView., 2023 Abstract G‐protein‐coupled receptors (GPCRs) constitute the largest family of membrane receptors, and are involved in the transmission of a variety of extracellular stimuli such as hormones, neurotransmitters, light and odorants into intracellular responses.
Carole Daly, Bianca Plouffe
wiley +1 more source
Methylene Blue Is a Muscarinic Antagonist in Cardiac Myocytes [PDF]
Molecular Pharmacology, 1997 We studied the mechanism of action of methylene blue (Mblue), a putative guanylyl cyclase inhibitor, on the L-type calcium current (ICa) and the muscarinic activated K+ current (IK,ACh) in rat ventricular and atrial myocytes, respectively, and on the binding of [3H]quinuclidinyl benzylate in rat ventricular membranes.
Abi-Gerges, Najah +4 more
openaire +2 more sources
Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs [PDF]
, 2016 Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands is unknown.
Godin, Antoine G. +4 more
core +1 more source
Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]
, 2019 In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie +3 more
core +2 more sources
Molecular probes for muscarinic receptors: Functionalized congeners of selective muscarinic antagonists [PDF]
Life Sciences, 1995 The muscarinic agonist oxotremorine and the tricyclic muscarinic antagonists pirenzepine and telenzepine have been derivatized using a functionalized congener approach for the purpose of synthesizing high affinity ligand probes that are suitable for conjugation with prosthetic groups, for receptor cross-linking, fluorescent and radioactive detection ...
Kenneth A. Jacobson +2 more
openaire +3 more sources
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 +6 more
core +2 more sources
Combined Unilateral Blockade of Cholinergic, Peptidergic, And Serotonergic Receptors in The Ventral Respiratory Column Does Not Affect Breathing in Awake Or Sleeping Goats [PDF]
, 2015 Previous work in intact awake and sleeping goats has found that unilateral blockade of excitatory inputs in the ventral respiratory column (VRC) elicits changes in the concentrations of multiple neurochemicals, including serotonin (5-HT), substance P ...
Forster, Hubert +7 more
core +2 more sources
Muscarinic antagonist effects on executive control of attention [PDF]
The International Journal of Neuropsychopharmacology, 2009 Acetylcholine plays a major role in mediating attention processes. We investigated the muscarinic antagonist effect of scopolamine on functional neuro-anatomy of attention and cognition. We assessed 12 healthy volunteers while performing the Attention Network Task on 0.4 mg scopolamine and placebo in a single-blind randomized trial in a 1.5 T magnetic ...
Thienel, Renate +10 more
openaire +4 more sources
Carbachol increases intracellular free calcium concentrations in human granulosa-lutein cells [PDF]
, 1992 We investigated whether the stimulation of human granulosa-lutein cells with muscarinic and nicotinic receptor agonists can cause increases in intracellular free calcium (Ca2+), using Fura-2 microfluorimetry.
Föhr, K. J. +3 more
core +1 more source