A Novel Role of Serotonin Receptor 2B Agonist as an Anti-Melanogenesis Agent.

Abstract

BW723C86, a serotonin receptor 2B agonist, has been investigated as a potential therapeutic for various conditions such as anxiety, hyperphagia and hypertension. However, the functional role of BW723C86 against melanogenesis remains unclear. In this study, we investigate the effect of serotonin receptor 2B (5-HTR2B) agonist on melanogenesis and elucidate the mechanism involved. BW723C86 reduced melanin synthesis and intracellular tyrosinase activity in melan-A cells and normal human melanocytes. The expression of melanogenesis-related proteins (tyrosinase, TRP-1 and TRP-2) and microphthalmia-associated transcription factor (MITF) in melan-A cells decreased after BW723C86 treatment. The promoter activity of MITF was also reduced by BW723C86 treatment. The reduced level of MITF was associated with inhibition of protein kinase A (PKA) and cAMP response element-binding protein (CREB) activation by BW723C86 treatment. These results suggest that the serotonin agonist BW723C86 could be a potential therapeutic agent for skin hyperpigmentation disorders.

• Authors: Eun Ju Oh, Jong Il Park, Ji Eun Lee, Cheol Hwan Myung, Su Yeon Kim, Sung Eun Chang, Jae Sung Hwang
• Journal: International journal of molecular sciences (Int J Mol Sci) Vol. 17 Issue 4 Pg. 546 (Apr 12 2016) ISSN: 1422-0067 [Electronic] Switzerland
• PMID: 27077852 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 1-(5-(2-thenyloxy)-1H-indol-3-yl)propan-2-amine
• Indoles
• Melanins
• Serotonin 5-HT2 Receptor Agonists
• Thiophenes
• Protein-Tyrosine Kinases

Topics

• Animals
• Cell Line
• Down-Regulation
• Humans
• Indoles (pharmacology)
• Melanins (metabolism)
• Melanocytes (cytology, drug effects, metabolism)
• Mice
• Protein-Tyrosine Kinases (genetics, metabolism)
• Serotonin 5-HT2 Receptor Agonists (pharmacology)
• Signal Transduction (drug effects)
• Thiophenes (pharmacology)