"Functional antagonism" is often used to describe the general relaxant effect of beta 2 agonists and xanthines and their ability to protect the airways against bronchoconstrictor stimuli. This study in guinea pig isolated trachea addresses the question of whether the capacity of these drugs to protect against constrictor stimuli is related to smooth muscle relaxation. Three antimuscarinic drugs...

Human lung fibroblasts are a potential source of endothelin-1 (ET-1), a pro-fibrotic mediator. The present study explored possible muscarinic and β-adrenergic modulations of ET-1 expression in human lung fibroblasts. MRC-5 human lung fibroblasts were cultured. Expression of prepro-endothelin-1 (ppET-1) mRNA was determined by quantitative real time PCR. [(3)H]-Proline incorporation was determine...

The present experiments studied the effects of cholinergic agonists and antagonists on the spontaneous and acoustic-evoked discharge of auditory cortical neurons and examined whether these effects were mediated by muscarinic cholinergic receptors. A primary focus of this report is the analysis of specific effects of these agents on the spontaneous and tone-evoked discharge and on different temp...

The aim of the present study was to determine whether cholinergic increase in the size of a functional representation (collective evoked response from a large population of neurons) can be observed shortly (within an hour) after treatment onset and whether nicotinic receptors can participate in this type of modulation. Cholinergic agonist application has been found previously to increase the re...

We measured pharmacologically isolated GABAergic currents from layer II/III neurons of the rat auditory cortex using patch-clamp recording. Activation of muscarinic receptors by muscarine (1 μM) or oxotremorine (10 μM) decreased the amplitude of electrically evoked inhibitory postsynaptic currents to about one third of their control value. Neither miniature nor exogenously-evoked GABAergic curr...

BACKGROUND AND PURPOSE Conventional determination of agonist efficacy at G-protein coupled receptors is measured by stimulation of guanosine-5'-γ-thiotriphosphate (GTPγS) binding. We analysed the role of guanosine diphosphate (GDP) in the process of activation of the M₂ muscarinic acetylcholine receptor and provide evidence that negative cooperativity between agonist and GDP binding is an alter...

Sicca features are the central clinical manifestations of Sjögren's syndrome (SS), but recent studies have confirmed that primary SS has a systemic expression, including extraglandular manifestations. Patients with a predominantly extraepithelial expression should be managed differently from patients with predominantly periepithelial or sicca limited disease. In coming years treatment will be b...

Nicotine is a very widely used drug of abuse, which has many neurovegetative behavioural and psychological effects by interacting with neuronal nicotinic acetylcholine receptor. Cholinergic receptors can be divided into two types, muscarinic and nicotinic, based on the pharmacological action of various agonists and antagonists. This review summarises the major recent findings of nicotine effect...

Abbreviations: Global initiative for chronic Obstructive Lung Disease, GOLD; forced expiratory volume in 1 second, FEV1; inhaled corticosteroid, ICS; long-acting muscarinic antagonist, LAMA; long-acting beta2-agonists, LABA; chronic obstructive pulmonary disease, COPD Citation: Balkissoon R. Journal club: Inhaled corticosteroids—refining our understanding of their role in maintenance treatment ...

Cholinergic agonists have previously been shown to augment the ability of sensitized lymphocytes to injure cells bearing the sensitizing alleantigens. The cholinergic receptor of the attacking lymphocyte population has been studied with pharmacological manipulation of an in vitro system that quantitates the injury mediated by sensitized attacking cells upon target cells. The data reveal that mu...