BIIE-0246 is a highly potent, high affinity antagonist selective for the Y2 receptor subtype. BIIE-0246 is a drug used in scientific research, 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, as well as modulating dopamine and acetylcholine release. Blockade of central neuropeptide Y (NPY) Y2 receptors by BIIE-0246 has being shown to reduce ethanol self-administration in rats.

BIBO-3304 is a subtype selective nonpeptide antagonist with subnanomolar affinity for the Y1 receptor subtype that significantly inhibits food intake induced by application of NPY or by fasting. BIBO-3304 is a NPY Y1 receptor antagonist (IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively) that displays > 2600-fold selectivity over Y2, Y4 and Y5 receptors.

BGC 20761 is an orally active, tryptamine analogue that is being developed by BTG as a procognitive antipsychotic for the treatment of schizophrenia. Preclinical development is underway in the US. This serotonin6 and serotonin2A receptor antagonist has nootropic properties with a balance of serotonergic and dopaminergic antagonist activity; BGC 20761 has moderate to low affinity for dopamine2, serotonin2C, histamine1, muscarinic M1-5, and α1 adrenergic receptors, indicating a potentially low propensity to cause serious adverse events.