Purinergic Receptor Ligands: State-of-the Art of the Medicinal Chemistry and Application to Neurodegenerative Diseases

Abstract

Event Abstract Back to Event Purinergic Receptor Ligands: State-of-the Art of the Medicinal Chemistry and Application to Neurodegenerative Diseases Gloria Cristalli1* 1 Universita di Camerino, via S. Agostino 1, Dipartimento di Scienze Chimiche, Italy The involvement of purinergic P1 and P2 receptors is described under different CNS acute and chronic pathological conditions. A large body of evidence suggests that activation of purinergic receptors can be detrimental or protective after brain insults, depending on the nature of brain injury and associated pathological conditions. The clinical utility of adenosine was recognized late in 1980s and since then only preparations of adenosine itself were present on the market until April 2008 when FDA has approved Lexiscan, an adenosine derivative substituted at the 2-position, for use as pharmacologic stress agent in patients undergoing nuclear perfusion imaging. As far as P2 receptors, clopidogrel, a selective inhibitor of the platelet ADP receptor P2Y12, is used for therapies in acute coronary syndromes. Currently, some other purinergic receptor agonists and antagonists have begun preclinical and clinical trials.The present lecture will be focused on the description of novel P1 and P2 receptor ligands. More in detail, the activity of new adenosine A2A receptor antagonists in different in vivo experimental models of Parkinson’s disease, and the neuroprotective effects of new highly potent and selective agonists for the A3 receptor in rat hippocampal slices, will be presented. Furthermore, the activity of novel P2X3 receptor ligands will be discussed. P2X3 subtype is an ATP-gated ionotropic receptor thought to mediate nociception especially in conditions like neuropathic and chronic pain. Hence, compounds behaving as partial agonists of P2X3 receptors could be potentially useful drugs to regulate the sensitivity of such receptors to painful stimuli. Keywords: CNS diseases, P1 ligands, P2 ligands, purinergic receptors Conference: 3rd Mediterranean Conference of Neuroscience , Alexandria, Egypt, 13 Dec - 16 Dec, 2009. Presentation Type: Oral Presentation Topic: Symposium 27 – The purinergic system as a target for the development of novel drugs for acute and chronic CNS disorders Citation: Cristalli G (2009). Purinergic Receptor Ligands: State-of-the Art of the Medicinal Chemistry and Application to Neurodegenerative Diseases. Front. Neurosci. Conference Abstract: 3rd Mediterranean Conference of Neuroscience . doi: 10.3389/conf.neuro.01.2009.16.094 Copyright: The abstracts in this collection have not been subject to any Frontiers peer review or checks, and are not endorsed by Frontiers. They are made available through the Frontiers publishing platform as a service to conference organizers and presenters. The copyright in the individual abstracts is owned by the author of each abstract or his/her employer unless otherwise stated. Each abstract, as well as the collection of abstracts, are published under a Creative Commons CC-BY 4.0 (attribution) licence (https://creativecommons.org/licenses/by/4.0/) and may thus be reproduced, translated, adapted and be the subject of derivative works provided the authors and Frontiers are attributed. For Frontiers’ terms and conditions please see https://www.frontiersin.org/legal/terms-and-conditions. Received: 20 Nov 2009; Published Online: 20 Nov 2009. * Correspondence: Gloria Cristalli, Universita di Camerino, via S. Agostino 1, Dipartimento di Scienze Chimiche, Camerino (MC), Italy, gloria.cristalli@unicam.it Login Required This action requires you to be registered with Frontiers and logged in. To register or login click here. Abstract Info Abstract The Authors in Frontiers Gloria Cristalli Google Gloria Cristalli Google Scholar Gloria Cristalli PubMed Gloria Cristalli Related Article in Frontiers Google Scholar PubMed Abstract Close Back to top Javascript is disabled. Please enable Javascript in your browser settings in order to see all the content on this page.