LY-266,097 is a research ligand which acts as a potent and selective antagonist for the 5-HT2B receptor, with more than 100x selectivity over the related 5-HT2A and 5-HT2C receptor subtypes. However, other sources have stated that LY-266,097 is actually a biased agonist of the receptor, selective for Gq signaling but not β-arrestin2. The drug has been used to study the role of the 5-HT2B receptor in modulating dopamine release in the brain, as well as its involvement in other processes such as allodynia.
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