Emerging opportunities and concerns for drug discovery at serotonin 5-HT2B receptors.
5-HT(2B) receptors have been reported to play an important role at cardiac, intestinal and central levels, as well as in bone marrow formation and growth. In the last decade, 5-HT(2B) receptors have also gained much attention as new targets in therapeutics, but also as off-targets because their activation along with the inhibition of serotonin transporters plays a significant role in the pathogenesis of 5-HT induced valvulopathy. Taking this into account, the present review focuses on the new therapeutic applications of 5-HT(2B) receptor ligands as well as on the potential concerns.
Brea
José
J
Departamento de Farmacología, Facultad de Farmacia. University of Santiago de Compostela. E-15782 Spain.
Castro-Palomino
Julio
J
Yeste
Sandra
S
Cubero
Elena
E
Párraga
Antonio
A
Domínguez
Eduardo
E
Loza
María Isabel
MI
D055808:Drug Discovery; D006801:Humans; D008024:Ligands; D044403:Receptor, Serotonin, 5-HT2B / Q000737:chemistry / Q000378:metabolism; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D017366:Serotonin Receptor Agonists / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D008024:Ligands; D044403:Receptor, Serotonin, 5-HT2B; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists