Search results for " antagonist"
showing 10 items of 1421 documents
Pharmacological characterization and autoradiographic localization of histamine H2 receptors in human brain identified with [125I]iodoaminopotentidin…
1992
125I-Aminopotentidine (125I-APT), a reversible probe of high specific radioactivity and high affinity and selectivity for the H2 receptor, was used to characterize and localize this histamine receptor subtype in human brain samples obtained at autopsy. On membranes of human caudate nucleus, specific 125I-APT binding at equilibrium revealed a single component, with a dissociation constant of 0.3 nM and maximal capacity of about 100 fmol/mg of protein. At 0.2 nM, 125I-APT specific binding, as defined with tiotidine, an H2-receptor antagonist chemically unrelated to iodoaminopotentidine, represented 40-50% of the total. Specific 125I-APT binding was inhibited by a series of typical H2-receptor…
Acetylcholine mediates the release of IL-8 in human bronchial epithelial cells by a NFkB/ERK-dependent mechanism
2007
Acetylcholine may play a role in cell activation and airway inflammation. We evaluated the levels of both mRNA and protein of muscarinic M(1), M(2), M(3) receptors in human bronchial epithelial cell line (16HBE). 16HBE cells were also stimulated with acetylcholine and extracellular signal-regulated kinase1/2 (ERK1/2) and NFkB pathway activation as well as the IL-8 release was assessed in the presence or absence of the inhibitor of Protein-kinase (PKC) (GF109203X), of the inhibitor of mitogenic activated protein-kinase kinase (MAPKK) (PDO9805), of the inhibitor of kinaseB-alpha phosphorilation (pIkBalpha) (BAY11-7082), and of muscarinic receptor antagonists tiotropium bromide, 4-Diphenylacet…
Gastrin: an acid-releasing, proliferative and immunomodulatory peptide?
2010
Gastrin release is affected by gastric inflammatory conditions. Antral G cells respond to inflammatory mediators by increasing gastrin secretion. Accumulating experimental evidence suggests that gastrin exerts immunomodulatory and proinflammatory effects. Gastrin could be a contributing factor to these pathologies, which may constitute a new justification for pharmacological blockade of gastrin action.
Appetite and Obesity
2011
Orexin (hypocretin) plays an important role in promoting wakefulness [1]. It stimulates wakefulness when injected in the cerebral ventricles, in the periventricular nucleus, dorsomedial hypothalamus, or lateral hypothalamus [2, 3]. Orexinergic neurons originate from the lateral hypothalamus and have projections to most parts of the central nervous system including the brain stem. The lack of orexin and/or orexin receptors is linked to narcolepsy [4–6].
Leptin and Leptin Receptor Are Expressed in the Human Endometrium and Endometrial Leptin Secretion Is Regulated by the Human Blastocyst1
2000
Embryonic implantation is a crucial event for the human reproductive function. Cytokines and paracrine molecules have been proposed as putative local regulators of this process. The leptin or the OB protein has been linked to the reproductive function and inflammatory response. In the present study, we describe for the first time the expression of leptin and leptin receptor (long form) in the secretory endometrium and that endometrial leptin secretion is regulated in vitro by the human blastocyst. Leptin and leptin receptor messenger RNA and protein were identified in secretory endometrium and in cultured endometrial epithelial cells (EECs) by RT-PCR, Western blot, and immunohistochemistry.…
Impairment of leptin/leptin receptor pathway in nasal epithelium from allergic turbinates
2016
BACKGROUND: Allergic rhinitis (AR) is characterized by a remodeling of nasal epithelium. Leptin adipokine has been already identified as a marker of homeostasis in human bronchial epithelial of asthmatics. TGF-β is a multi-functional cytokine and conflicting findings exist regarding its role in the remodeling responses of the upper airways in allergic rhinitis. OBJECTIVE: We sought to investigate ex-vivo the expression of leptin/leptin receptor pathway and TGF-β in human nasal epithelium. METHODS: 41 biopsies of inferior turbinates obtained from allergic patients with AR (A, n = 20) and from healthy control subjects (C, n = 21) were analyzed for leptin/leptin receptor and for TGF-β 1, 2, 3 …
Refractory Death Rattle: Deep Aspiration Facilitates the Effects of Antisecretory Agents
2011
Anticholinergic drugs, including atropine, hyoscine butylbromide, and scopolamine, have been shown to be equally effective in the treatment of death rattle. However, anticholinergic drugs may only be effective in reducing the production of further secretions, rather than eliminating the existing ones. A case is described in which a preventive procedure was undertaken to carefully eliminate secretions before starting anticholinergic drugs. Airway aspiration under light anesthesia removed secretions before starting anticholinergic drugs. Low doses of propofol were given intravenously to make a laryngoscopy feasible, allowing the complete aspiration of large amounts of tracheal secretions. No …
Exploring gastric emptying rate in minipigs: Effect of food type and pre-dosing of metoclopramide.
2018
The present study investigated the gastric emptying rate in Gottingen minipigs pre- and post-prandial and evaluated the effect of metoclopramide on the same parameter, using paracetamol as an absorption marker. The pharmacokinetic evaluation of the obtained plasma concentration data for paracetamol demonstrated that the fastest gastric emptying rate was observed in the animals that were allowed access to normal pig food. There was no significant difference in the stomach emptying rate observed between fasted and fed minipigs, when fed either with a FDA standard breakfast or a nutritional energy drink. Pre-dosing minipigs with metoclopramide (0.2 or 0.4 mg/kg) did not demonstrate any effect …
2012
Background and Purpose Diagnosis of paroxysmal atrial fibrillation (AF) can be challenging, but it is highly relevant in patients presenting with sinus rhythm and acute cerebral ischemia. We aimed to evaluate prospectively whether natriuretic peptide levels and kinetics identify patients with paroxysmal AF. Methods Patients with acute cerebral ischemia were included into the prospective observational Find-AF study. N-terminal pro brain-type natriuretic peptide (NT-proBNP), brain-type natriuretic peptide (BNP) and N-terminal pro atrial-type natriuretic peptide (NT-proANP) plasma levels were measured on admission, after 6 and 24 hours. Patients free from AF at presentation received 7 day Holt…