A library of compounds targeted to the vasopressin/oxytocin family of receptors was screened for activity at a cloned human oxytocin receptor using a reporter gene assay. Potency and selectivity were optimised to afford compound 39, EC50 = 33 nM. This series of compounds represents the first disclosed, non-peptide, low molecular weight agonists of the hormone oxytocin (OT).
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http://dx.doi.org/10.1016/j.bmcl.2004.04.107 | DOI Listing |
Biochem Pharmacol
November 2023
Laboratory of Basic and Behavioral Neuroendocrinology (LANBAC), Department of Physiology, Center for Biological and Health Sciences, Federal University of Sergipe, São Cristóvão, SE, Brazil; Graduate Program in Physiological Sciences, Federal University of Sergipe, São Cristóvão, SE, Brazil. Electronic address:
Although it has been previously demonstrated that oxytocin (OXT) receptor stimulation can control skeletal muscle mass in vivo, the intracellular mechanisms that mediate this effect are still poorly understood. Thus, rat oxidative skeletal muscles were isolated and incubated with OXT or WAY-267,464, a non-peptide selective OXT receptor (OXTR) agonist, in the presence or absence of atosiban (ATB), an OXTR antagonist, and overall proteolysis was evaluated. The results indicated that both OXT and WAY-267,464 suppressed muscle proteolysis, and this effect was blocked by the addition of ATB.
View Article and Find Full Text PDFInt J Mol Sci
June 2023
Institute for Stem Cell Research and Regenerative Medicine, Medical Faculty, Heinrich-Heine University Düsseldorf, 40225 Düsseldorf, Germany.
Podocytes are highly specialized cells that play a pivotal role in the blood filtration process in the glomeruli of the kidney, and their dysfunction leads to renal diseases. For this reason, the study and application of this cell type is of great importance in the field of regenerative medicine. Hypertension is mainly regulated by the renin-angiotensin-aldosterone system (RAAS), with its main mediator being angiotensin II (ANG II).
View Article and Find Full Text PDFBiol Aujourdhui
February 2023
Laboratoire d'Innovation Thérapeutique, UMR7200, Faculté de Pharmacie de Strasbourg, 74 route du Rhin, 67400 Illkirch, France.
It is known since the fifties that oxytocin is a neurohormone synthesized in the brain and released in blood circulation to trigger uterus contraction during delivery. It is also involved in milk ejection during breast-feeding. Over the past 25 years, many other central and peripheral functions have been discovered, in particular for attachment between child and parents as well as between individuals and interaction between a human being and its social group.
View Article and Find Full Text PDFExpert Rev Neurother
February 2022
Cardiology Department, Private Polyclinic Center Eurofarm Sarajevo, Sarajevo, Bosnia and Herzegovina.
Introduction: Neuroactive peptides are peptides produced by neurons and released through controlled mechanisms that bind to specific receptors on nerve, glial, or other cell types, causing biochemical response(s) within these cells.
Areas Covered: This article summarizes and interprets recent advancements in our knowledge of neuroactive peptides with pro- or anti-convulsant action, and about new drugs that use the molecular machinery of neuroactive peptides to suppress seizures.
Expert Opinion: According to the results of preclinical and limited clinical investigations to date, the highest potential to become anti-epileptic drugs with marketing authorization belongs to non-peptide agonists of melanocortin receptors, thyrotropin-releasing hormone receptors, ghrelin receptors, galanin receptors, somatostatin and cortistatin receptors, oxytocin receptors, cholecystokinin receptors, and opioid kappa receptors, followed by non-peptide antagonists of the renin-angiotensin system, corticotropin-releasing hormone receptors, NK1 receptors for substance P, arginine-vasopressin receptors, and opioid delta receptors.
J Pharm Biomed Anal
January 2022
Division of Chemical Metrology and Analytical Science, National Institute of Metrology, Beijing 100029, PR China. Electronic address:
Oxytocin is not only a significant peptide drug for enhancing uterine contractions, but also an emerging biomarker and therapeutic target of mental disorders in clinical practice. There is a pressing need for the standardization of oxytocin assays because of its low pharmaceutical quality and large variations among measurement approaches. International System of Units (SI)-traceable analytical methods and well-characterized pure reference materials are urgently needed to set up standard reference measurement systems in laboratory medicine, ensuring the accuracy and comparability of test results.
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