(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide

Description

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.

Uses

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

in vivo

IC 50

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

References

[1] PASCAL BONAVENTURE. Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor.[J]. Journal of Pharmacology and Experimental Therapeutics, 2004, 308 3: 1130-1137. DOI: 10.1124/jpet.103.060459
[2] G. MITTAPALLI E R. Ligands of the Neuropeptide Y Y2 Receptor[J]. ChemInform, 2014, 46 1. DOI: 10.1002/chin.201410270