Search results for "Adrenergic receptor"
showing 10 items of 62 documents
MiR-133 Modulates the β1Adrenergic Receptor Transduction Cascade.
2014
Rationale : The sympathetic nervous system plays a fundamental role in the regulation of myocardial function. During chronic pressure overload, overactivation of the sympathetic nervous system induces the release of catecholamines, which activate β-adrenergic receptors in cardiomyocytes and lead to increased heart rate and cardiac contractility. However, chronic stimulation of β-adrenergic receptors leads to impaired cardiac function, and β-blockers are widely used as therapeutic agents for the treatment of cardiac disease. MicroRNA-133 (miR-133) is highly expressed in the myocardium and is involved in controlling cardiac function through regulation of messenger RNA translation/stability. …
Nitric oxide is formed in a subpopulation of rat pineal cells and acts as an intercellular messenger.
1998
In the rat pineal, formation of the second messenger cyclic GMP (cGMP) is under adrenergic control. Two important sequential steps mediate adrenergic signal transduction by cGMP, receptor-stimulated nitric oxide (NO) formation by the enzyme NO synthase I (NOS I), and NO-induced cGMP formation by the cytosolic enzyme guanylyl cyclase. With regard to the first step in cGMP transduction (i.e. NO formation) we found, by means of NOS I immunostaining and NADPH-diaphorase staining, that the presence of NOS I was restricted to a subpopulation of pineal cells, generally surrounded by NOS I-negative cells. Considering the fact that NO is able to permeate the cell membrane, the question arises whethe…
Alpha-adrenergic modulation of glutathione metabolism in isolated rat hepatocytes.
1988
Glutathione metabolism was studied in isolated hepatocytes from 48-h starved rats. Phenylephrine (10 microM, final concentration) was incubated in the presence of a mixture of L-glutamine, glycine, L-serine, and L-methionine (at 10 times their normal plasma concentration). Alpha-adrenergic stimulation provoked a decrease in glutathione (GSH) synthesis. This effect was accompanied by an enhanced efflux of glutathione from the cells. Phenylephrine stimulated the rate of glutathione disulfide (GSSG) formation; however, this effect was clearly insufficient to explain the disappearance of GSH. Our results suggest that the decrease in cellular GSH levels observed under conditions of shock, stress…
beta-Adrenoceptor and GRK3 expression in human lymphocytes is related to blood pressure and urinary albumin excretion.
2010
31 p., figuras, abreviaturas y bibliografía
Effects of cerivastatin on adrenergic pathways, hypertrophic growth and TGFbeta expression in adult ventricular cardiomyocytes.
2010
Abstract The effects of statin treatment in the setting of heart failure have already been shown. Nevertheless, there is little knowledge about its influence on adrenergic pathways in cardiomyocytes. Therefore, this study investigated the impact of cerivastatin on adrenoceptor-mediated signalling pathways in isolated adult ventricular cardiomyocytes. It focused on two endpoints: hypertrophic growth and TGFbeta expression. Cultured cardiomyocytes were used to study rac activation (analysed by its translocation into the membrane fraction), ROS formation (H 2 DCF fluorescence) and hypertrophic growth ( 14 C-phenylalanine incorporation). Alpha- and beta-adrenoceptor stimulation showed significa…
Effects of antidepressants in adrenergic neurotransmission of human vas deferens
2000
Objectives. To evaluate the effects of sertraline, fluoxetine, and amitriptyline on the contractile responses of the human vas deferens muscle elicited by norepinephrine, electrical field stimulation, and KCl, because the therapeutic action of antidepressants may be accompanied by sexual dysfunction related to the contractility of the vas deferens smooth muscle. Methods. Ring segments of the epididymal part of the vas deferens were taken from 32 elective vasectomies and mounted in organ baths for isometric recording of tension. We then studied the effects of sertraline, fluoxetine, and amitriptyline on the neurogenic and agonist-induced contractile responses. Results. Amitriptyline caused c…
Molecular connectivity to find β-blockers with low toxicity
1997
Abstract Molecular connectivity has been used to find new β-blocker drugs using linear discriminant analysis and connectivity functions with different topological descriptors. Among the selected compounds stands out the probucol and the β-carotene. Both of them interact with β adrenoceptors.
Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?
2007
International audience; The management of premature birth still remains unsatisfactory. Since the relative lack of efficiency and/or safety of current tocolytic agents have been highlighted, it is necessary to develop new uterorelaxant drugs deprived of important maternal and foetal side effects. Our work reported in this review focuses on a potential new target for tocolytic drugs, the beta3-adrenoceptor (ADRB3). This third type of ADRB is shown to be present and functional in human myometrium. We demonstrated that ADRB3 agonists are able to inhibit in-vitro spontaneous contractions of myometrial strips, via a cyclic AMP-mediated pathway. Furthermore, we established that ADRB3 is the predo…
Die Wirkung von ?-Receptoren blockierenden Substanzen auf die durch Adrenalin gesteigerte 42K-Abgabe des Meerschweinchenvorhofs
1966
An isolierten linken Meerschweinchenvorhofen wurde der Einflus des Adrenalins und der β-Receptoren blockierenden Substanz 1-(3-Methylphenoxy)-2-hydroxy-3-isopropylaminopropan (MHIP; Ko 592) auf den K-Umsatz und auf elektrophysiologische Mesgrosen, die mit Hilfe der Mikroelektrodentechnik bestimmt wurden, untersucht.
8-NH2-Boldine, an Antagonist of α1Aand α1BAdrenoceptors without Affinity for the α1DSubtype: Structural Requirements for Aporphines at α1-Adrenocepto…
2005
Structure-activity analysis of 21 aporphine derivatives was performed by examining their affinities for cloned human alpha (1A), alpha (1B) and alpha (1D) adrenoceptors (AR) using membranes prepared from rat-1 fibroblasts stably expressing each alpha (1)-AR subtype. All the compounds tested competed for [ (125)I]-HEAT binding with steep and monophasic curves. The most interesting compound was 8-NH (2)-boldine, which retains the selective affinity for alpha(1A)-AR (pKi = 6.37 +/- 0.21) vs. alpha(1B)-AR (pKi = 5.53 +/- 0.11) exhibited by 1,2,9,10-tetraoxygenated aporphines, but shows low affinity for alpha(1D)-AR (pKi < 2.5). Binding studies on native adrenoceptors present in rat cerebral cor…