BIIE-0246

BIIE-0246

BIIE-0246 is a drug used in scientific research which acts as a potent and selective antagonist for the Neuropeptide Y receptor Y2.[1] It was one of the first non-peptide Y2-selective antagonists developed, and remains among the most widely used tools for studying this receptor. It has been used to demonstrate a role for the Y2 subtype as a presynaptic autoreceptor limiting further neuropeptide Y release,[2][3] as well as modulating dopamine[4] and acetylcholine release.[5] It has also been shown to produce several behavioural effects in animals, including reducing alcohol consumption in addicted rats[6][7] and anxiolytic effects,[8] although while selective Y2 agonists are expected to be useful as anorectics,[9][10] BIIE-0246 did not appear to increase appetite when administered alone.[11]

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