dbo:abstract |
BW-723C86 is a tryptamine derivative drug which acts as a 5-HT2B receptor agonist. It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT2B receptor in a range of other tissues. BW-723C86 is actually a mixed 5-HT2B/5-HT2C agonist, and while it has good selectivity over 5-HT2A 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-HT2B agonist was available until the potent and selective 5-HT2B activity of 6-APB was discovered in 2012. Highly selective 5-HT2C antagonists are available however, and so a combination of BW-723C86 with a selective 5-HT2C antagonist allows 5-HT2B 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. (en) |
dbo:casNumber |
160521-72-2 |
dbo:fdaUniiCode |
8JMH6M2ELN |
dbo:pubchem |
4284720 |
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rdfs:comment |
BW-723C86 is a tryptamine derivative drug which acts as a 5-HT2B receptor agonist. It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT2B receptor in a range of other tissues. (en) |
rdfs:label |
BW-723C86 (en) BW-723C86 (zh) |
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