Table 1

Saturation analysis-derived binding constants of the three diverse radioligands for wild-type and mutant human tachykinin NK2receptors expressed in CHO cells

RadioligandReceptor Type
Wild-typeHis198AlaTyr266Ala   KdTyr266PhePhe270AlaTyr289Ala   KdTyr289Phe
KdBmaxKdBmaxKdBmaxKdBmaxKdBmax
[125I]NKA2.4  ± 0.4206  ± 28N.D.N.D.2.8  ± 0.2211  ± 19N.D.N.D.2.0  ± 0.3199  ± 55
(5)(6)(12)
[3H]SR 489680.3  ± 0.13274  ± 14894.8  ± 1.1273  ± 431-150 , 1-160 N.D.1.2  ± 0.1779  ± 1011.6  ± 0.31230  ± 38N.D.N.D.
(6)(5)(6)(4)
[3H]MEN 114204.0  ± 0.41664  ± 41611.5  ± 2.1807  ± 82N.D.N.D.N.D.N.D.2.9  ± 0.33636  ± 391
(6)(4) (4)

Kd (nM) and Bmax (fmol/mg protein) values are expressed as mean ± S.E.M. of the number of independent determinations indicated in parentheses.

  • N.D., no detectable binding.

  • 1-150P < .05 versus wild-type.

  • 1-160P < .05 versus [3H]MEN 11420.