The cardiovascular effects of gallamine triethiodide and succinylcholine chloride were studied in Beagle dogs during controlled halothane anesthesia. Small but significant increases in heart rate and mean arterial presssure were observed 1 minute after intravenous injection of succinylcholine chloride. Intravenous injection of gallamine triethiodide did not produce significant cardiovascular changes.
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Biochem Pharmacol
October 2021
Institute of Physiology, Czech Academy of Sciences, Prague, Czech Republic. Electronic address:
Endogenous neurosteroids and their synthetic analogues-neuroactive steroids-have been found to bind to muscarinic acetylcholine receptors and allosterically modulate acetylcholine binding and function. Using radioligand binding experiments we investigated their binding mode. We show that neuroactive steroids bind to two binding sites on muscarinic receptors.
View Article and Find Full Text PDFEur J Pharmacol
September 2020
Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy.
Although agonists and antagonists of muscarinic receptors have been known for long time, there is renewed interest in compounds (such as allosteric or bitopic ligands, or biased agonists) able to differently and selectively modulate these receptors. As a continuation of our previous research, we designed a new series of dimers of the well-known cholinergic agonist carbachol. The new compounds were tested on the five cloned human muscarinic receptors (hM) expressed in CHO cells by means of equilibrium binding experiments, showing a dependence of the binding affinity on the length and position of the linker connecting the two monomers.
View Article and Find Full Text PDFPharmacol Rep
April 2019
Laboratory of Physiology, Department of Medicine, School of Health Sciences, University of Thessaly, BIOPOLIS, Larissa, Greece. Electronic address:
Background: Muscarinic receptor antagonists are a usual treatment for chronic airway diseases, with increased bronchoconstriction, like asthma and chronic obstructive pulmonary disease. These diseases are usually accompanied by airway remodeling, involving airway smooth muscle cell (ASMC) proliferation. The purpose of this study was to examine the effect of the muscarinic receptor modulator gallamine on rabbit tracheal ASMC proliferation.
View Article and Find Full Text PDFEur J Pharmacol
March 2018
Departamento de Farmacobiología, Cinvestav-Coapa, Czda. de los Tenorios 235, Col. Granjas-Coapa, Del. Tlalpan, C.P. 14330 México City, Mexico.
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.
View Article and Find Full Text PDFEur J Pharmacol
February 2018
Departamento de Farmacobiología, Cinvestav Unidad Coapa, Czda. de los Tenorios 235, Col. Granjas-Coapa, Del. Tlalpan, C.P. 14330 México D.F., Mexico. Electronic address:
It has been reported that metformin reduces blood pressure although the mechanisms have not been described. Indeed, several mechanisms could be implicated including the interaction with α-adrenoceptors or inhibition of sympathetic outflow. Therefore, this study was designed to determine the capability of metformin to block the vasopressor responses induced by α-adrenoceptor agonists or selective electrical stimulation of sympathetic outflow.
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