TABLE 2
Summary of parameters for kinetic binding of various ligands to NK3
All of the values were obtained in 50 mM Tris-HCl, pH 7.4, at 22°C. Radiolabeled osanetant, SB222200, and [MePhe7]NKB were used in filter binding assays to quantify association and dissociation binding kinetics. The apparent first-order rate constant for association kon[A], kon, and koff were obtained by fitting data to eqs. 12 to 14. The koff value for talnetant was determined using a hot-chase procedure with 125I-[MePhe7]NKB as discussed under Materials and Methods. The Kd values were taken as the ratio of koff/kon.