TABLE 6

K_inetic parameters for association and dissociation of ³H]Me-talnetant in hNK₃R WT membranes and of [³H]osanetant in the hNK₃R WT, T139A, and M346A membranes

The K_ob, K_off, K_on, t_½, and K_d values are mean ± S.E., calculated from three independent experiments (each performed in quadruplet) as described under Materials and Methods.

Compound	hNK₃R	Association Kinetic					Dissociation Kinetic		Apparent K_d
Compound	hNK₃R			K_ob	K_on	t_½	K_off	t_½	Apparent K_d
		min⁻¹	nM⁻¹ min⁻¹	min	min⁻¹	min	nM
[³H]Me-talnetant	WT	0.49 ± 0.04	0.34 ± 0.06	1.41 ± 0.16	0.15 ± 0.03	4.56 ± 0.52	0.44 ± 0.15
[³H]Osanetant	WT	0.17 ± 0.02	0.33 ± 0.04	4.01 ± 0.73	0.07 ± 0.01	10.10 ± 1.07	0.22 ± 0.06
	T139A	0.15 ± 0.01	0.29 ± 0.07	4.60 ± 0.31	0.03 ± 0.01	21.43 ± 2.4	0.12 ± 0.01
	M346A	0.14 ± 0.01	0.29 ± 0.06	5.04 ± 0.27	0.04 ± 0.01	17.72 ± 1.93	0.11 ± 0.01