683746-68-1

JNJ-5207787 is an antagonist of the neuropeptide Y (NPY) receptor Y₂ that blocks peptide YY binding (IC₅₀ = 100 nM). It displays 100-fold selectivity for Y₂ over other NPY receptors and has minimal effect on a panel of 50 receptors, ion channels, and transporters, except for sodium channel 2. JNJ-5207787 is intraperitoneally bioavailable and brain penetrant in rats, occupying maximally 50% of Y₂ receptor binding sites in the hypothalamic area.

JNJ 5207787 is a small molecule antagonist of the neuropeptide Y Y2 receptor.

human Y₂ receptor: 7.0 (pIC₅₀); rat Y₂ receptor: 7.1 (pIC₅₀)

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