Search results for "SCAR"

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…

Acetylcholine and nicotine stimulate the release of granulocyte-macrophage colony stimulating factor from cultured human bronchial epithelial cells.

1998

Primary cultures of human bronchial epithelial cells (HBE-cells) were established to measure granulocyte-macrophage colony stimulating factor (GM-CSF) release. HBE-cells showed a basal GM-CSF release (82+/-20 ng/well/24 h; 30 donors), which was increased by interleukin-1 beta(IL-1beta, 1 ng/ml) by 270%. This effect was blocked by 1 microM dactinomycin or 10 microM cycloheximide, i.e. the stimulatory effect of IL-1beta depended on de-novo synthesis. Histamine (100 microM) and acetylcholine ( 100 nM) stimulated GM-CSF release more than two-fold above the baseline. Nicotine (1 microM) increased GM-CSF release to a similar extent, and this effect was prevented by 30 microM (+)-tubocurarine. The…

Desensitization of inhibitory prejunctional alpha 2-adrenoceptors and putative imidazoline receptors on rabbit heart sympathetic nerves.

1993

To find out whether sympathetic nerves of the rabbit heart possess pharmacologically relevant prejunctional imidazoline receptors different from α-autoreceptors, the inhibition by oxymetazoline, aganodine and BDF 6143 (4-chloro-2-[2-imidazoline-2-ylamino]-isoindoline hydrochloride) of endogenous noradrenaline overflow evoked by stimulation of extrinsic postganglionic sympathetic nerves (0.66 Hz, 80 pulses) was investigated. In addition we wanted to find out whether either type of these prejunctional receptors undergoes desensitization upon pre-exposure to respective agonists. The α2-adrenoceptor agonist oxymetazoline inhibited the evoked noradrenaline overflow (2.9 nmol/l, IC50; about 90010…

Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors.

2003

Galantamine (Reminyl), an approved treatment for Alzheimer's disease (AD), is a potent allosteric potentiating ligand (APL) of human alpha 3 beta 4, alpha 4 beta 2, and alpha 6 beta 4 nicotinic receptors (nAChRs), and of the chicken/mouse chimeric alpha 7/5-hydroxytryptamine3 receptor, as was shown by whole-cell patch-clamp studies of human embryonic kidney-293 cells stably expressing a single nAChR subtype. Galantamine potentiates agonist responses of the four nAChR subtypes studied in the same window of concentrations (i.e., 0.1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg. At concentrations10 microM, gal…

β2 long-acting and anticholinergic drugs control TGF-β1-mediated neutrophilic inflammation in COPD

2012

AbstractWe quantified TGF-β1 and acetylcholine (ACh) concentrations in induced sputum supernatants (ISSs) from 18 healthy controls (HC), 22 healthy smokers (HS) and 21 COPDs. ISSs from HC, HS and COPD as well as rhTGF-β1 were also tested in neutrophil adhesion and in mAChR2, mAChR3 and ChAT expression experiments in human bronchial epithelial cells (16-HBE). Finally, we evaluated the effects of Olodaterol (a novel inhaled β2-adrenoceptor agonist) and Tiotropium Spiriva®, alone or in combination, on neutrophil adhesion and mAChRs and ChAT expression in stimulated 16-HBE. The results showed that 1) TGF-β1 and ACh concentrations are increased in ISSs from COPD in comparison to HC and HS, and T…

Detecting crop water requirement indicators in irrigated agroecosystems from soil water content profiles: An application for a citrus orchard.

2022

Abstract Most perennial crops sensitive to water scarcity, such as citrus, can benefit from efficient water management, which allows for reduced water consumption while increasing crop production on a long-term basis. However, when implementing water-saving strategies, it is necessary to monitor soil and/or plant water status in order to determine crop water demand. A plethora of devices providing indirect measurements of volumetric soil water content, such as the “drill and drop” multi-sensors probes (Sentek, Inc., Stepney, Australia), have been developed over the last decade. The objective of the paper was to analyse time-series of soil water content profiles and meteorological data colle…

International Legal Approaches to Waste Water Discharges

2002

Este capítulo se dedica al estudio de los distintos enfoques jurídicos seguidos en el Derecho Internacional del Medio Ambiente sobre las descargas de aguas residuales. Comienza analizando los enfoques jurídicos fragmentarios iniciales sobre las descargas de aguas residuales, principalmente en la Antártida y el Océano Austral, en algunos mares regionales (especialmente, el Mediterráneo) y el caso particular de las descargas de basuras procedentes de buques. No obstante, dedico la parte principal de este capítulo al enfoque global que sobre esta cuestión clave de la contaminación marina se inició en 1995, así como a su aplicación jurídica global, regional y nacional. This chapter is devoted t…

Reverse osmosis and nanofiltration membranes for highly efficient PFASs removal: overview, challenges and future perspectives

2021

Today, it is extremely urgent to face the increasing shortage of clean and safe water resources, determined by the exponential growth of both world population and its consumerism, climate change and pollution. Water remediation from traditional chemicals and contaminants of emerging concerns (CECs) is supposed to be among the major methods to solve water scarcity issues. Reverse osmosis (RO) and nanofiltration (NF) membrane separation technologies have proven to be feasible, sustainable and highly effective methods for the removal of contaminants, comprising the extremely persistent and recalcitrant perfluoroalkyl substances (PFASs), which failed to be treated through the traditional water …

Recio Morales, Oscar: Alejandro O'Reilly, inspector general. Poder militar, familia y territorio en el reinado de Carlos III

2021

Elogio de el Exc.mo y rever.mo señor Don Francisco de Almeida Mascareñas Principal de la Santa Iglesia Patriarchal de Lisboa ...

Accion de gracias a la Sabiduria Divina, tutelar de la Academia Valenciana / que ... se leyó en nombre de D. Francisco de Almeida y Mascareñas ...: p. 27-41 Alg. caplletra orn., fris tip., vinyeta a la port Sign.: A-F4, [ ]1. - Reclams