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David Centurión, Saúl Huerta de la Cruz, Shirley V Castillo-Santiago, María Elena Becerril-Chacón, José A Torres-Pérez, Araceli Sánchez-López
Hydrogen sulfide is a gasotransmitter that mediates cardiovascular responses and could protect the heart from ischemia-reperfusion damage. Furthermore, this gas mediates bradycardia although the mechanisms involved remain elusive. In this regard, the inhibition of the cardiac sympathetic outflow may be partially involved. Thus, this study was designed to determine the capability of NaHS to inhibit the tachycardic responses induced by preganglionic stimulation of the cardioaccelerator sympathetic outflow. Wistar rats were anaesthetized with isoflurane, cannulated and pithed...
March 15, 2018: European Journal of Pharmacology
Anika Hoppe, Maria Marti-Solano, Matthäus Drabek, Moritz Bünemann, Peter Kolb, Andreas Rinne
Muscarinic receptors (M-Rs) for acetylcholine (ACh) belong to the class A of G protein-coupled receptors. M-Rs are activated by orthosteric agonists that bind to a specific site buried in the M-R transmembrane helix bundle. In the active conformation, receptor function can be modulated either by allosteric modulators, which bind to the extracellular receptor surface or by the membrane potential via an unknown mechanism. Here, we compared the modulation of M1 -Rs and M3 -Rs induced by changes in voltage to their allosteric modulation by chemical compounds...
January 2018: Cellular Signalling
Raj Kumar Chinnadurai, Ponne Saravanaraman, Rathanam Boopathy
Osteoblast differentiation is an essential event in the developmental process, which is favoured by the production of extra cellular matrix proteins and various enzymes including discrete ones like acetylcholinesterase (AChE). Despite the fact that AChE facilitates osteoblast differentiation, the significance of its catalytic functions [esterase and aryl acylamidase (AAA) activities] in the process is yet to be ascertained. In this context, SaOS-2 cell line was used in the present study to implicate the catalytic activities of AChE in process of osteoblast differentiation and mineralization...
March 2018: Molecular and Cellular Biochemistry
Eloísa Rubio-Beltrán, Alejandro Labastida-Ramírez, Oswaldo Hernández-Abreu, Antoinette MaassenVanDenBrink, Carlos M Villalón
Calcitonin gene-related peptide (CGRP) plays a role in several (patho)physiological functions, and modulation of its release is considered a therapeutic target. In this respect, electrical spinal (T9--T12) stimulation of the perivascular sensory outflow in pithed rats produces vasodepressor responses mediated by CGRP release. This study investigated the role of imidazoline I1 and I2 receptors in the inhibition by moxonidine and agmatine of these vasodepressor responses. Male Wistar pithed rats (pretreated i...
July 8, 2017: European Journal of Pharmacology
Dimitri A Cozanitis
In 1957, Professor Daniel Bovet received the Nobel Prize in Physiology or Medicine for his studies on various compounds including the muscle relaxants gallamine and succinylcholine that became very useful in anaesthesia. Textbooks credit Professor Bovet for the discovery of these drugs. However, although he indeed did discover their pharmacological character, the actual syntheses were made by Ernest Fourneau and Reid Hunt, respectively; sadly, these two scientists have largely been ignored. In this paper, a brief biography of Bovet is presented along with some of his more notable accomplishments...
November 2016: Wiener Medizinische Wochenschrift
David Centurión, Saúl Huerta De la Cruz, Erika J Gutiérrez-Lara, Jesús H Beltrán-Ornelas, Araceli Sánchez-López
It has been reported that i.v. administration of NaHS, a donor of H2S, elicited dose-dependent hypotension although the mechanisms are not completely understood. In this regard, several mechanisms could be involved including the inhibition of the vasopressor sympathetic outflow. Thus, this study was designed to determine the potential capability of NaHS to mediate inhibition of the vasopressor responses induced by preganglionic sympathetic stimulation. For this purpose, Wistar rats were anaesthetised, pithed and cannulated for drug administration...
January 5, 2016: European Journal of Pharmacology
H E AlQot, N A Elnozahi, M M Mohy El-Din, A E Bistawroos, M S Abou Zeit-Har
The objective of this study is to probe the effects of dopamine and potential interactions with nicotine at the motor end plate. To accomplish this, we measured the amplitude of nerve-evoked muscle twitches of the isolated rat phrenic hemi-diaphragm preparation. Dopamine potentiated indirect muscle twitches in normal and gallamine-presensitized preparations amounting to a maximum of 31.14±0.71% and 69.23±1.96%, respectively. The dopamine-induced facilitation was well maintained in presence of 10 µM propranolol but greatly reduced in presence of 6 µM SCH 23390 or 3 µM dantrolene...
October 15, 2015: European Journal of Pharmacology
Guadalupe Manrique-Maldonado, Alain H Altamirano-Espinoza, Bruno A Marichal-Cancino, Eduardo Rivera-Mancilla, Victor Avilés-Rosas, Carlos M Villalón
This study has investigated whether pharmacological activation of Gi/o coupled histamine H3/H4 receptors inhibits the rat vasodepressor sensory outflow. For this purpose, 100 male Wistar rats were pithed, artificially ventilated and pretreated (i.v.) with: 25mg/kg gallamine, 2mg/kg/min hexamethonium and 20μg/kg/min methoxamine, followed by i.v. continuous infusions of physiological saline (0.02ml/min) or immepip (3.1, 10 or 31μg/kg/min; a histamine H3/H4 receptor agonist). Under these conditions, electrical stimulation (0...
May 5, 2015: European Journal of Pharmacology
Begoña Fonseca, Alejandro Martínez-Águila, Miguel Díaz-Hernández, Jesús Pintor
The purpose of this study is to investigate if the cholinergic stimulation by carbachol on tear secretion is a direct process or if it is also mediated by purinergic mechanisms. Experiments were performed in New Zealand male rabbits. The amount of tear secretion was measured with Schirmer's test and then analyzed by a HPLC protocol in order to study the nucleotide levels. Animal eyes were instilled with carbachol (a cholinergic agonist), pirenzepine, gallamine and 4-DAMP (muscarinic antagonists), PPADS, suramin and reactive blue 2 (purinergic antagonists), and a P2Y2 receptor small interfering RNA (siRNA)...
March 2015: Purinergic Signalling
Marco Tulio Menezes de Carvalho, Andrea Carla Celotto, Agnes Afrodite Sumarelli Albuquerque, Luciana Garros Ferreira, Verena Kise Capellini, Ana Paula Cassiano Silveira, Tales Rubens de Nadai, Paulo Roberto Barbosa Evora
BACKGROUND AND PURPOSE: There is a remarkable paucity of studies analyzing the role of the endothelium-derived relaxing factors on the vascular effects of organophosphates. This study was carried out to evaluate the vascular effects of malathion and the role of nitric oxide (NO) and prostacyclin (PGI2). METHODS: Vascular reactivity measuring isometric forces in vitro ('organ chambers') and flow cytometry (cells loaded with DAF-FM DA) were used. RESULTS: In rat thoracic aorta segments contracted with phenylephrine (Phe) (10(-7) mol/l), malathion (10(-10) to 10(-5) mol/l) induced concentration-dependent relaxation in arteries with intact endothelium (n = 7; p < 0...
2014: Pharmacology
Sunil Sahdeo, Alexey Tomilov, Kelly Komachi, Christine Iwahashi, Sandipan Datta, Owen Hughes, Paul Hagerman, Gino Cortopassi
Repurposing of FDA-approved drugs with effects on mitochondrial function might shorten the critical path to mitochondrial disease drug development. We improved a biosensor-based assay of mitochondrial O2 consumption, and identified mitofunctional defects in cell models of LHON and FXTAS. Using this platform, we screened a 1600-compound library of clinically used drugs. The assay identified drugs known to affect mitochondrial function, such as metformin and decoquinate. We also identified several drugs not previously known to affect mitochondrial respiration including acarbose, metaraminol, gallamine triethiodide, and acamprosate...
July 2014: Mitochondrion
Ma Trinidad Villamil-Hernández, Oscar Alcántara-Vázquez, Araceli Sánchez-López, Erika J Gutiérrez-Lara, David Centurión
The sympathetic nervous system that innervates the peripheral circulation is regulated by several mechanisms/receptors. It has been reported that prejunctional 5-HT1A, 5-HT1B, 5-HT1D, D2-like receptors and α2-adrenoceptors mediate the inhibition of the vasopressor sympathetic outflow in pithed rats. In addition, ergotamine, an antimigraine drug, displays affinity at the above receptors and may explain some of its adverse/therapeutic effects. Thus, the aims of this study were to investigate in pithed rats: (i) whether ergotamine produces inhibition of the vasopressor sympathetic outflow; and (ii) the major receptors involved in this effect...
October 5, 2014: European Journal of Pharmacology
Douglas A Schober, Carrie H Croy, Hongling Xiao, Arthur Christopoulos, Christian C Felder
In this study, we characterized a muscarinic acetylcholine receptor (mAChR) potentiator, LY2119620 (3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide) as a novel probe of the human M2 and M4 allosteric binding sites. Since the discovery of allosteric binding sites on G protein-coupled receptors, compounds targeting these novel sites have been starting to emerge. For example, LY2033298 (3-amino-5-chloro-6-methoxy-4-methyl-thieno(2,3-b)pyridine-2-carboxylic acid cyclopropylamid) and a derivative of this chemical scaffold, VU152100 (3-amino-N-(4-methoxybenzyl)-4,6-dim​ethylthieno[2,3-b]pyridine carboxamide), bind to the human M4 mAChR allosteric pocket...
July 2014: Molecular Pharmacology
No abstract text is available yet for this article.
November 1950: Journal
Marcelo J Alfonzo, Ramona González De Alfonzo, Marcelo A Alfonzo-González, Itala Lippo De Becemberg
Muscarinic acetylcholine receptors MAChRs from Bovine Tracheal Smooth Muscle (BTSM) plasma membranes are responsible for the cGMP rise and signal-amplitude peaks associated with smooth muscle contraction present in bronchial asthma. These MAChRs bind [(3)H]QNB and exhibit the classic G Protein Coupled-Receptor (GPCR) behavior towards muscarinic agonist and antagonists that is sensitive to sensitive to GTP analogs. Interestingly, the [(3)H]QNB binding activity was stimulated by cGMP and ATP, and was enhanced by IBMX and Zaprinast, inhibitors of cGMP-PDE...
December 2013: Molecular Membrane Biology
Clemens A Strohmaier, Herbert A Reitsamer, Jeffrey W Kiel
PURPOSE: Histological evidence suggests a role for the central nervous system in controlling episcleral venous pressure (EVP). Based on prior studies that identified candidate regions in the brain stem, the present study assessed the effect of electrical stimulation at the location of the superior salivatory nucleus (SSN) on EVP in rats. METHODS: Male Sprague-Dawley rats (n = 11) were anesthetized using pentobarbital sodium (50 mg/kg intraperitoneally initially, supplemented intravenously [IV] as needed) and paralyzed with gallamine triethiodide (1 mg/kg, IV)...
2013: Investigative Ophthalmology & Visual Science
Ma Trinidad Villamil-Hernández, Oscar Alcántara-Vázquez, Araceli Sánchez-López, David Centurión
α2-Adrenoceptors were first described as presynaptic receptors inhibiting the release of various transmitters from neurons in the central and peripheral nervous systems. In vitro studies have confirmed that α2A, α2B and α2C subtypes inhibited noradrenaline release from postganglionic sympathetic neurons but no study has been reported their involvement in the vasopressor sympathetic outflow in vivo. Thus, this study analysed the subtype(s) involved in the inhibition produced by the α2-adrenoceptor agonist, B-HT 933, on the vasopressor sympathetic outflow...
October 15, 2013: European Journal of Pharmacology
Guadalupe Manrique-Maldonado, Abimael González-Hernández, Alain H Altamirano-Espinoza, Bruno A Marichal-Cancino, Inna Ruiz-Salinas, Carlos M Villalón
Calcitonin gene-related peptide (CGRP) released from perivascular sensory nerves plays a role in the regulation of vascular tone. Indeed, electrical stimulation of the perivascular sensory out-flow in pithed rats produces vasodepressor responses, which are mainly mediated by CGRP release. This study investigated the potential role of dopamine D1 -like and D2 -like receptors in the inhibition of these vasodepressor responses. For this purpose, male Wistar pithed rats (pre-treated i.v. with 25 mg/kg gallamine and 2 mg/kg min...
February 2014: Basic & Clinical Pharmacology & Toxicology
Jian-You Lin, Joe Arthurs, Steve Reilly
The current study investigated whether internal pain-inducing agents can modulate palatability of a tastant in the same way as illness-inducing agents (e.g., lithium chloride). Similar to traditional conditioned taste aversion (CTA) experiments, during conditioning the rats were exposed to a saccharin solution followed by intraperitoneal injections of either gallamine (Experiment 1) or hypertonic sodium chloride (NaCl; Experiments 1 and 2). In addition to the total amount consumed, the time of each lick was recorded for lick pattern analysis...
July 2, 2013: Physiology & Behavior
Juciane Maria de Andrade Castro, Rodrigo R Resende, Luciana Mirotti, Esther Florsheim, Layra Lucy Albuquerque, Adriana Lino-dos-Santos-Franco, Eliane Gomes, Wothan Tavares de Lima, Marcelo de Franco, Orlando Garcia Ribeiro, Momtchilo Russo
Airway smooth muscle constriction induced by cholinergic agonists such as methacholine (MCh), which is typically increased in asthmatic patients, is regulated mainly by muscle muscarinic M3 receptors and negatively by vagal muscarinic M2 receptors. Here we evaluated basal (intrinsic) and allergen-induced (extrinsic) airway responses to MCh. We used two mouse lines selected to respond maximally (AIRmax) or minimally (AIRmin) to innate inflammatory stimuli. We found that in basal condition AIRmin mice responded more vigorously to MCh than AIRmax...
2013: BioMed Research International
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