Search results for "Muscarinic acetylcholine receptor"
showing 10 items of 182 documents
A muscarinic mechanism inhibiting the release of noradrenaline from peripheral adrenergic nerve fibres by nicotinic agents.
1968
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.
2003
A series of 2,3-disubstituted indenes, which are analogues of the widely used histamine H(1) receptor antagonist dimethindene, have been synthesized and studied as muscarinic and histamine receptor antagonists. The affinities of these compounds for the five human muscarinic receptor subtypes (M(1)-M(5)) and for human histamine H(1) receptors were determined in radioligand binding studies using membranes from transfected Chinese hamster ovary (CHO) cells and [(3)H]N-methylscopolamine ([(3)H]NMS). The results demonstrate that the diisopropyl analogue 19 has a similar high affinity as (S)-dimethindene at M(2) receptors ((S)-dimethindene: pK(i) = 7.52; (-)-19: pK(i) = 7.37) with an improved sel…
Detection of Fibroblast Growth Factor Receptor 1 (FGFR1) Transactivation by Muscarinic Acetylcholine Receptors (mAChRs) in Primary Neuronal Hippocamp…
2018
In addition to their canonical intracellular signals involved in the regulation of neuronal plasticity, G-protein coupled receptors can also rapidly transactivate tyrosine kinase receptors and their downstream intracellular signaling in absence of specific ligands. Here we describe our protocol for dissociating and maintaining hippocampal primary neurons in high- and low-density culture, followed by a description of methods employed to evaluate neurite outgrowth and protein phosphorylation associated with fibroblast growth factor receptor 1 transactivation by muscarinic acetylcholine receptors. Our goal was to provide the reader with detailed protocols of the abovementioned techniques and t…
THE EFFECTS OF MUSCARINIC AGONISTS AND ANTAGONISTS ON ACETYLCHOLINE RELEASE FROM PERIPHERAL CHOLINERGIC NERVES IN THE ABSENCE AND PRESENCE OF A CHOLI…
1980
Use of Antibodies in the Research on Muscarinic Receptor Subtypes
2016
Cellular Acetylcholine Receptor Expression in the Brain of Patients with Alzheimer’s and Parkinson’s Dementia
1995
Binding studies and receptor autoradiography reveal the overall changes of acetylcholine receptors (AChR) in Alzheimer’s and Parkinson’s dementia cortices.2,5 A detailed account of these changes requires a study of neurochemical phenotype of individual neurons as basic elements of networks constituting the substrate of cortical functions.4 Examples will be given for cell-type specific AChR localization in normal and diseased human cerebral cortex.
Acetylcholine receptors (muscarinic) (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
2019
Muscarinic acetylcholine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [45]) are GPCRs of the Class A, rhodopsin-like family where the endogenous agonist is acetylcholine. In addition to the agents listed in the table, AC-42, its structural analogues AC-260584 and 77-LH-28-1, N-desmethylclozapine, TBPB and LuAE51090 have been described as functionally selective agonists of the M1 receptor subtype via binding in a mode distinct from that utilized by non-selective agonists [243, 242, 253, 155, 154, 181, 137, 11, 230]. There are two pharmacologically characterised allosteric sites on muscarinic receptors, one defined by it binding gallami…
ChemInform Abstract: Synthesis and Muscarinic Activity of Isoxazole-Substituted 1,2,5,6- Tetrahydropyridines.
2010
ChemInform Abstract: Design and Pharmacology of Quinuclidine Derivatives as M2-Selective Muscarinic Receptor Ligands.
2010
Acetylcholine At Motor Nerves: Storage, Release, and Presynaptic Modulati On By Autoreceptors and Adrenoceptors
1992
Publisher Summary This chapter focuses on the modulation of acetylcholine release from the motor endplate by presynaptic receptors. An individual neuron can regulate its function, the release of transmitters or modulators, through the activation of local feedback loops. After escaping the neuronal membrane and entering the synaptic cleft (or extracellular space), the transmitter activates both the receptors localized at the endorgan (postsynaptic receptors) and the receptors localized at the nerve terminal within its diffusion radius (so-called presynaptic or neuronal receptors). Stimulation of presynaptic receptors triggers the generation of intracellular signals that modify ion channels o…