Search results for "Agoni"

CLONIDINE, A PARTIAL AGONIST OF THE HISTAMINERGIC H2 RECEPTORS?

1978

Origin of neuronal-like receptors in Metazoa: cloning of a metabotropic glutamate/GABA-like receptor from the marine sponge Geodia cydonium.

1999

To date, no conclusive evidence has been presented for the existence of neuronal-like elements in Porifera (sponges). In the present study, isolated cells from the marine sponge Geodia cydonium are shown to react to the excitatory amino acid glutamate with an increase in the concentration of intracellular calcium [Ca2+]i. This effect can also be observed when the compounds L-quisqualic acid (L-QA) or L-(+)-2-amino-4-phosphonobutyric acid (L-AP-4) are used. The effect of L-QA and L-AP-4, both agonists for metabotropic glutamate receptors (mGluRs), can be abolished by the antagonist of group I mGluRs, (RS)-alpha-methyl-4-carboxyphenylglycine. These data suggest that sponge cells contain an mG…

Back to the bases: Building a terrestrial water δ18O baseline for archaeological studies in North Patagonia (Argentina)

2020

Archaeology has been using stable oxygen as an isotopic tracer linked with water consumption for decades, and it has been demonstrated to be a powerful tool to assess paleomobility in bioarchaeology. Central-eastern North Patagonia (Argentina) is an especially appropriate region to apply it since it presents a high density of huntergatherer burials, it was a nodal zone criss-crossed by an extensive network of important routes, and it is characterized by a high environmental fragmentation due to the scarcity of fresh water sources. The aim of this paper is to build an empirical stable oxygen isotope baseline of terrestrial surface waters to assess the potentiality of tracing past human movem…

La longue agonie de la république des ouvriers papetiers : insubordination et normalisation au travail (France, début du XIXe siècle)

2011

Au debut du XIXe siecle, les compagnons papetiers – ce « corps republicain » denonce au XVIIIe siecle par les autorites – continuent d’entretenir une insubordination permanente pour defendre leur bon droit. Les modes, coutumes et rituels propres a ce groupe ont forge son identite sociale et politique a l’epoque moderne ; ils lui ont donne des armes pour controler le marche du travail et l’organisation de la production. Mais cette quete d’autonomie de la main-d’œuvre et son insubordination apparaissent de plus en plus intolerables aux fabricants et a l’Etat. Des lors, la souverainete du metier va peut a peut etre defaite et normalisee par l’intervention conjointe des regulations juridiques e…

Growth and Antagonism of <i>Trichoderma</i> spp. and Conifer Pathogen <i>Heterobasidion annosum</i&a…

2012

Variations in the radial growth rate of 24 isolates belonging to ten species of Trichoderma, three isolates of conifer pathogen Heterobasidion annosum s.s. and four isolates of H. parviporum were evaluated by incubation on a solid malt extract medium at a temperature of 4℃, 15℃ and 21℃. Trichoderma antagonism against Heterobasidion was investigated in dual culture in vitro. The slowest rate of growth was referable to all seven strains of Heterobasidion spp. All Heterobasidion spp. strains were overgrown by 63% of Trichoderma spp. strains after two weeks at 21℃ and by 33% of strains at 15℃. 21% of Trichoderma strains did not grow and only four strains belonging to T. koningii, T. viride and …

Association between use of novel glucose-lowering drugs and COVID-19 hospitalization and death in patients with type 2 diabetes: a nationwide registr…

2022

Abstract Aims Type 2 diabetes (T2DM) in patients with coronavirus disease-19 (COVID-19) is associated with a worse prognosis. We separately investigated the associations between the use of sodium-glucose cotransporter 2 inhibitors (SGLT2i), glucagon-like peptide-1 receptor agonists (GLP-1 RA), and dipeptidyl peptidase-4 inhibitors (DPP-4i), and the risk of COVID-19 hospitalization and death. Methods and results Patients with T2DM registered in the Swedish National Patient Registry and alive on 1 February 2020 were included. ‘Incident severe COVID-19’ was defined as the first hospitalization and/or death from COVID-19. A modified Poisson regression approach was applied to a 1:1 propensity sc…

Effects of Anandamide and Noxious Heat on Intracellular Calcium Concentration in Nociceptive DRG Neurons of Rats

2007

As an endogenous agonist at the cannabinoid receptor CB1 and the capsaicin-receptor TRPV1, anandamide may exert both anti- and pronociceptive actions. Therefore we studied the effects of anandamide and other activators of both receptors on changes in free cytosolic calcium ([Ca2+]i) in acutely dissociated small dorsal root ganglion neurons (diameter: ≤30 μm). Anandamide (10 μM) increased [Ca2+]iin 76% of the neurons. The EC50was 7.41 μM, the Hill slope was 2.15 ± 0.43 (mean ± SE). This increase was blocked by the competitive TRPV1-antagonist capsazepine (10 μM) and in Ca2+-free extracellular solution. Neither exclusion of voltage-gated sodium channels nor additional blockade of voltage-gate…

Identification of biological markers of liver X receptor (LXR) activation at the cell surface of human monocytes.

2012

Background Liver X receptor (LXR) α and LXR β (NR1H3 and NR1H2) are oxysterol-activated nuclear receptors involved in the control of major metabolic pathways such as cholesterol homeostasis, lipogenesis, inflammation and innate immunity. Synthetic LXR agonists are currently under development and could find applications in various fields such as cardiovascular diseases, cancer, diabetes and neurodegenerative diseases. The clinical development of LXR agonists requires the identification of biological markers for pharmacodynamic studies. In this context, monocytes represent an attractive target to monitor LXR activation. They are easily accessible cells present in peripheral blood; they expres…

Evaluation of enantioselective binding of basic drugs to plasma by ACE.

2007

The present paper deals with the evaluation of the stereoselective binding of antihistamines (brompheniramine, chlorpheniramine, hydroxyzine, orphenadrine and phenindamine), phenothiazines (promethazine and trimeprazine) and a local anesthetic (bupivacaine) to human plasma proteins. Since all of them are drugs highly bound to proteins, a methodology to determine the bound fraction of each drug enantiomer was proposed. This methodology includes the incubation of samples containing plasma and racemic drug, ultrafiltration of the mixture and the chiral separation of enantiomers in the bound drug fraction using affinity EKC (AEKC)-partial filling technique and HSA as chiral selector. The result…

Reduction of clozapine-induced hypersalivation by pirenzepine is safe.

2004

Introduction Hypersalivation is known as a frequent, disturbing, and socially stigmatizing side effect of therapy with the atypical antipsychotic clozapine. It has been shown that the addition of the anticholinergic pirenzepine is able to reduce clozapine-induced hypersalivation, probably by blocking M4-receptors. Nevertheless, a pharmacokinetic interaction between both compounds cannot be excluded. Methods In this pilot study, 29 schizophrenic patients (ICD-10; 51.7 % female; age: 36.7 +/- 8.7 years [mean +/- SD]) were included. Serum concentrations of clozapine and its pharmacologically active metabolite N-desmethylclozapine were determined under steady-state conditions by automated HPLC …