Skip to main content
padlock icon - secure page this page is secure

Medicinal Chemistry of 5-HT5A Receptor Ligands: A Receptor Subtype with Unique Therapeutical Potential

Buy Article:

$68.00 + tax (Refund Policy)

Although the 5-HT5 receptor subfamily was discovered more than 15 years ago, it is unambiguously the least known 5-HT receptor subtype. The Gi/G0-mediated signal transduction and its intensive presence in raphe and other brainstem and pons nuclei suggest mechanisms similar to those of 5-HT1 receptors, the ligands of which are already applied in the treatment of e.g. anxiety and migraine. In addition, a unique coupling and inhibition of adenosine diphosphate-ribosyl cyclase have also been described. High concentrations of 5-HT5 receptor in other key regions including, e.g. locus coeruleus, nucleus of the solitary tract, arcuate and suprachiasmatic nuclei of the hypothalamus indicate a wide range of physiological effects, thus its ligands are potential drug candidates in various areas, e.g. anxiety, sleep, incontinence, food intake, learning and memory, pain or chemoreception pathways. These findings have motivated several institutes and pharmaceutical companies to participate in the research of this field. Despite extensive research, no selective agonist and only two selective antagonists have been identified until now. Beyond these compounds, the present review provides a complete overview on all other published 5-HT5A receptor ligands as well as on the structure, function, distribution, genetics and possible therapeutic applications of this receptor.
No References
No Citations
No Supplementary Data
No Article Media
No Metrics

Keywords: 5-HT autoreceptor; 5-HT5; 5-HT5A; Serotonin; anxiety; drug target; food intake; incontinence; learning and memory; neuronal hyperpolarization; pain; sleep

Document Type: Research Article

Affiliations: EGIS Pharmaceuticals Plc.,Chemical Research Division, P.O. Box 100, Budapest, H-1475 Hungary.

Publication date: April 1, 2010

More about this publication?
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more