Search results for "Muscarinic"

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…

Phorbol Esters and Muscarinic Receptor Agonists Activate Phospholipase D in Heart and Brain

1991

Phospholipase D (PLD) hydrolyzes phosphatidylcholine and thereby seems to play a key role in a novel pathway of signal transduction. PLD activity in rat hippocampal slices and atria of rat, guinea pig and chicken hearts was determined by measuring the catalytic products choline (Ch), phosphatidic acid (PA) and, in the presence of a primary alcohol, phosphatidylpropanol or phosphatidylethanol. It was found that the PLD activity was high, even under resting conditions, in both tissues, especially in the hippocampus, and that the enzyme activity could be enhanced by activation of protein kinase C and by muscarinic receptor stimulation.

Neuronal Growth and Behavioral Alterations in Mice Deficient for the Psychiatric Disease-Associated Negr1 Gene

2018

Neuronal growth regulator 1 (NEGR1), a member of the immunoglobulin superfamily cell adhesion molecule subgroup IgLON, has been implicated in neuronal growth and connectivity. In addition, genetic variants in or near the NEGR1 locus have been associated with obesity and more recently with learning difficulties, intellectual disability and psychiatric disorders. However, experimental evidence is lacking to support a possible link between NEGR1, neuronal growth and behavioral abnormalities. Initial expression analysis of NEGR1 mRNA in C57Bl/6 wildtype (WT) mice by in situ hybridization demonstrated marked expression in the entorhinal cortex (EC) and dentate granule cells. In co-cultures of co…

Safety of tiotropium and olodaterol fixed-dose combination for COPD in patients on β-blockers

2015

Introduction: The TONADO studies (NCT01431274; NCT01431287) established the efficacy and safety of a new once-daily fixed-dose combination (FDC) with tiotropium (T), a long-acting muscarinic antagonist, and olodaterol (O), a long-acting β 2 -agonist, for the treatment of COPD. This post hoc analysis evaluates T+O safety in the subgroup of patients (pts) receiving β-blockers (BBs) in these studies. Methods: These were randomised, double-blind, parallel-group, 52-week, Phase III trials comparing T+O FDC (2.5/5 µg; 5/5 µg) with the monocomponents. Adverse events (AEs) and serious AEs (SAEs) were recorded and SAEs independently adjudicated. Pooled safety data from pts receiving BBs at baseline …