Search results for " bet"

Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.

2009

The beta-adrenergic agonist 1 (zilpaterol) is used as production enhancer in cattle. Binding experiments of separated enantiomers on recombinant human beta(2)-adrenergic and mu-opioid receptors and functional studies showed that the (-)-1 enantiomer accounts for essentially all the beta(2)-adrenergic agonist activity and that it exhibits less affinity toward the mu-opioid receptor than (+)-1, which is a mu-opioid receptor antagonist. X-ray crystallography revealed the absolute configuration of (-)-1 to be 6R,7R.

Introductory Lecture: Allosteric Modulation of Torpedo Nicotinic Acetylcholine Receptor Ion Channel Activity by Noncompetitive Agonists

1997

AbstractSimilar to other neuroreceptors of the vertebrate central nervous system, the nicotinic acetylcholine receptor (nAChR) is subject to modulatory control by allosterically acting ligands. Of particular interest in this regard are allosteric ligands that enhance the sensitivity of the receptor to its natural agonist acetylcholine (ACh), as such ligands could be useful as drugs in diseases associated with impaired nicotinic neurotransmission. Here we discuss the action of a novel class of nAChR ligands which act as allosterically potentiating ligands (APL) on the nicotinic responses induced by ACh and competitive agonists. In addition, APLs also act as noncompetitive agonists of very lo…

α7 Nicotinic acetylcholine receptors and modulation of gabaergic synaptic transmission in the hippocampus

2000

The present report provides new findings regarding modulation of gamma-aminobutyric acid (GABA) transmission by alpha7 nicotinic receptor activity in CA1 interneurons of rat hippocampal slices. Recordings were obtained from tight-seal cell-attached patches of the CA1 interneurons, and agonists were delivered to the neurons via a modified U-tube. Application for 6 s of the alpha7 nicotinic receptor-selective agonist choline (or =1 mM) to all CA1 interneurons tested triggered action potentials that were detected as fast current transients. The activity triggered by choline terminated well before the end of the agonist pulse, was blocked by the alpha7 nicotinic receptor antagonist methyllycaco…

Associations between personality, sports participation and athletic success. A comparison of Big Five in sporting and non-sporting adults

2018

Abstract The present study investigates whether the Big Five personality traits are different among diverse sports populations. A sample of 881 male athletes and non-athletes completed a self-report questionnaire measuring their personality traits. The Exploratory Structure Equation Modeling (ESEM) approach is adopted to test measurement invariance and mean differences among groups. The results indicate that athletes who had experienced the most success in their sport scored higher than non-athletes in each personality dimension of the Big Five, with the exception of openness, while less successful athletes scored higher than non-athletes only in extraversion and agreeableness. The more suc…

Consensus statement of the Italian society of pediatric allergy and immunology for the pragmatic management of children and adolescents with allergic…

2020

AbstractThe COVID-19 pandemic has surprised the entire population. The world has had to face an unprecedented pandemic. Only, Spanish flu had similar disastrous consequences. As a result, drastic measures (lockdown) have been adopted worldwide. Healthcare service has been overwhelmed by the extraordinary influx of patients, often requiring high intensity of care. Mortality has been associated with severe comorbidities, including chronic diseases. Patients with frailty were, therefore, the victim of the SARS-COV-2 infection. Allergy and asthma are the most prevalent chronic disorders in children and adolescents, so they need careful attention and, if necessary, an adaptation of their regular…

QUANTIFICATION OF GENETIC VARIANTS OF CASEINS IN MILK OF GIRGENTANA GOAT BREED

2013

In the milk of ruminants, more than 95% of proteins are synthesized by six structural genes, four caseins (alphas1, beta, alphas2 and κ-caseins) and two whey proteins (alpha-lactalbumin and beta-lactoglobulin). Goat casein genes have been found to show high polymorphism, which influences not only the quantity of casein in milk but also the structural and nutritional characteristics and technological properties of milk. The aim of this work was to separate and quantify the most common allelic variants of caseins in milk of Girgentana goat breed, a Sicilian autochthonous breed, and to evaluate the effect of casein polymorphisms on casein content. The alleles at different casein genes were det…

CHARACTERIZATION OF THE SYNAPTIC PROTEOME IN NON-DEMENTED SUBJECTS WITH ALZHEIMER’S NEUROPATHOLOGY

Some individuals, here refereed to as Non-Demented with Alzheimer’s Neuropathology (NDAN), retain their congitive function despite the presence of amyloid plaques and tau tangles typical of symptomatic Alzheimer’s Disease (AD). In NDAN, unlike AD, toxic amyloid beta oligomers do not localize to the postsynaptic densities (PSDs). Synaptic resistance to amyloid beta in NDAN may thus enable these individuals to remain cognitively intact despite the AD-like pathology. The mechanim(s) responsible for this resistance remains unresolved and understanding such protective biological processes could reveal novel targets for the development of effective treatments for AD. The current work describes th…

Targeting Alzheimer’s disease with multimodal polypeptide-based nanoconjugates

2021

LRP1-targeted St-Cl–polyglutamate conjugates as multivalent neuroprotective/neurotrophic therapeutics for Alzheimer’s disease.

Biomarkers Related to Synaptic Dysfunction to Discriminate Alzheimer’s Disease from Other Neurological Disorders

2022

Recently, the synaptic proteins neurogranin (Ng) and α-synuclein (α-Syn) have attracted scientific interest as potential biomarkers for synaptic dysfunction in neurodegenerative diseases. In this study, we measured the CSF Ng and α-Syn concentrations in patients affected by AD (n = 69), non-AD neurodegenerative disorders (n-AD = 50) and non-degenerative disorders (n-ND, n = 98). The concentrations of CSF Ng and α-Syn were significantly higher in AD than in n-AD and n-ND. Moreover, the Aβ42/Ng and Aβ42/α-Syn ratios showed statistically significant differences between groups and discriminated AD patients from n-AD patients, better than Ng or α-Syn…

Emerging contributions of formyl peptide receptors to neurodegenerative diseases.

2021

Abstract Inflammation is a central element of many neurodegenerative diseases. Formyl peptide receptors (FPRs) can trigger several receptor-dependent signal transduction pathways that play a key role in neuroinflammation and neurodegeneration. They are chemotactic receptors that help to regulate pro- and anti-inflammatory responses in most mammals. FPRs are primarily expressed in the immune and nervous systems where they interact with a complex pattern of pathogen-derived and host-endogenous molecules. Mounting evidence points towards a contribution of FPRs – via neuropathological ligands such as Amyloid beta, and neuroprotective ligands such as Humanin, Lipoxin A4, and Annexin A1 – to mult…