BW-723C86
# BW-723C86

BW-723C86 is a tryptamine derivative drug which acts as a $5-HT_{2B}$ receptor agonist. It has anxiolytic effects in animal studies, and is also used for investigating the function of the $5-HT_{2B}$ receptor in a range of other tissues.

BW-723C86 is actually a mixed $5-HT_{2B}/5-HT_{2C}$ agonist, and while it has good selectivity over $5-HT_{2A}$ and other serotonin receptor subtypes, it is around only 3 times as selective for 2B compared to 2C and so is much less selective than most research ligands, but no superior $5-HT_{2B}$ agonist was available until the potent and selective $5-HT_{2B}$ activity of 6-APB was discovered in 2012. Highly selective $5-HT_{2C}$ antagonists are available however, and so a combination of BW-723C86 with a selective $5-HT_{2C}$ antagonist allows $5-HT_{2B}$ mediated responses to be studied in isolation.

An in vitro study including assay on normal (healthy) human melanocytes found that BW-723C86 causes skin whitening. The mechanism of action of BW-723C86 is decreasing the expression of MITF which in turn, decreases the expression of the melanin main synthesizing enzymes: tyrosinase, TRP-1 and TRP-2. BW-723C86 is not cytotoxic to melanocytes and, unlike many skin whitening agents, does not directly inhibit the activity of tyrosinase.

