BW-723C86 is a tryptamine derivative drug which acts as a 5-HT<sub>2B</sub> receptor agonist. It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT<sub>2B</sub> receptor in a range of other tissues.
BW-723C86 is actually a mixed 5-HT<sub>2B</sub>/5-HT<sub>2C</sub> agonist, and while it has good selectivity over 5-HT<sub>2A</sub> 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<sub>2B</sub> agonist was available until the potent and selective 5-HT<sub>2B</sub> activity of 6-APB was discovered in 2012. Highly selective 5-HT<sub>2C</sub> antagonists are available however, and so a combination of BW-723C86 with a selective 5-HT<sub>2C</sub> antagonist allows 5-HT<sub>2B</sub> mediated responses to be studied in isolation.
The drug does not induce the head-twitch response, a behavioral proxy of psychedelic effects associated with serotonin 5-HT<sub>2A</sub> receptor agonism, across a wide range of doses. This may be related to the fact that it showed more than 200-fold selectivity for activation of the serotonin 5-HT<sub>2B</sub> receptor over the serotonin 5-HT<sub>2A</sub> receptor.
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.