TABLE 1

Antagonists selected in the study

Values were obtained from radioligand displacement assays by competition with 0.02 nM 125I-NDP-α-MSH on HEK293 cells expressing hMC4R (Kd,, 0.5 nM; Bmax, 3900 fmol/mg protein).

StructureNomenclatureCodeKiInhibition @ 10 μM
μM%
Embedded Image2-(2-(2-Methoxy-5-nitrobenzylthio)phenyl)-1,4,5,6-tetrahydropyrimidineMTHP0.09488
Embedded Image3-(4-(2-(4-Fluorophenyl)-2-(4-methylpiperazin-1-yl)ethyl)piperazin-1-yl)-2-methyl-1-phenylpropan-1-onePPPone0.69188
Embedded Image2-(5-Bromo-2-methoxyphenethyl)-N-(N-((1-ethylpiperidin-4-yl)methyl)carbamimidoyl)-3-fluorobenzamideMPCI0.21894
Embedded ImageN-((2R)-3(2,4-Dichlorophenyl)-1-(4-(2-((1-methoxypropan-2-ylamino)methyl)phenyl)piperazin-1-yl)-1-oxopropan-2-yl)propionamideDCPMP0.023788
Embedded Image1-(1-(4-Fluorophenyl)-2-(4-(4-(naphthalene-1-yl)butyl)piperazin-1-yl)ethyl)-4-methylpiperazinNBP0.002489