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