TABLE 2

Relative binding, Emax, and EC50 values of various GnRH receptors

Values represent the mean ± S.E.M. of three independent experiments performed in duplicate. Binding was expressed as a percentage of specific binding of gmGnRHR-2 (gm2).

Receptors Relative Binding GnRH-I GnRH-II
Emax EC50Emax EC50
% gm2 fold induction log M fold induction log M
gm2 100 ± 1.2 9.33 ± 0.35 −6.00 ± 0.10 13.82 ± 0.35 −8.54 ± 0.13
rat 98.8 ± 1.8 12.49 ± 0.26 −8.31 ± 0.06* 8.78 ± 0.29 −7.54 ± 0.07*
r6TM 89.5 ± 1.1 9.59 ± 0.33 −7.16 ± 0.12* 5.45 ± 0.20 −7.95 ± 0.12
r6.5TM 168.1 ± 4.5 17.14 ± 0.38 −9.18 ± 0.08* 17.53 ± 0.35 −8.48 ± 0.07
rEL3S 21.8 ± 0.1 5.79 ± 0.18 −6.64 ± 0.10 7.72 ± 0.21 −8.21 ± 0.09
rEL3L 110.1 ± 5.4 6.24 ± 0.14 −8.38 ± 0.09* 6.37 ± 0.08 −8.76 ± 0.05
rEL3L/F7.37I 110.3 ± 9.4 6.83 ± 0.31 −8.25 ± 0.16* 10.77 ± 0.53 −8.24 ± 0.18
rEL3L/F7.38L 138.7 ± 1.1 7.63 ± 0.35 −7.98 ± 0.18* 10.56 ± 0.29 −8.34 ± 0.10
rEL3L/A7.42G 49.7 ± 3.4 6.31 ± 0.22 −8.25 ± 0.09* 5.43 ± 0.12 −8.79 ± 0.10
rEL3L/F7.43L 52.7 ± 0.1 3.89 ± 0.27 −7.81 ± 0.20* 4.61 ± 0.19 −8.63 ± 0.18
rEL3L/P7.46A 3.8 ± 0.5 N.D.
rEL3L/C7.47P 1.5 ± 1.0 N.D.
rEL3L/E7.32Q 70.7 ± 0.2 3.53 ± 0.14 −7.28 ± 0.15* 4.61 ± 0.14 −8.47 ± 0.14
rEL3L/PPS 332.2 ± 7.3 12.50 ± 0.27 −7.61 ± 0.07* 16.78 ± 0.35 −9.36 ± 0.09*
L7.43F 1.7 ± 1.2 N.D.
A7.46P 3.8 ± 0.9 N.D.
P7.47C 72.1 ± 2.1 6.46 ± 0.26 −5.93 ± 0.08 12.29 ± 0.57 −8.29 ± 0.17
L7.43F/A7.46P 3.2 ± 2.8 N.D.
L7.43F/P7.47C 16.8 ± 1.2 3.57 ± 0.07 −7.03 ± 0.07* 4.94 ± 0.15 −8.79 ± 0.17
A7.46P/P7.47C 303.3 ± 1.4 10.53 ± 0.61 −7.17 ± 0.17* 11.00 ± 0.29 −9.65 ± 0.12*
L7.43F/A7.46P/P7.47C 178.6 ± 8.6 5.93 ± 0.20 −8.21 ± 0.13* 7.06 ± 0.20 −9.82 ± 0.13*
SEP/l7.43F/A7.46P/P7.47C 11.1 ± 0.5 2.92 ± 0.08 −7.87 ± 0.12* 2.53 ± 0.10 −9.69 ± 0.26*
rEL3S/L7.43F/A7.46P/P7.47C 54.6 ± 2.1 4.68 ± 0.13 −8.76 ± 0.15* 6.14 ± 0.11 −9.59 ± 0.10*
SEP/I7.37F/L7.38F/L7.43F/A7.46P/P7.47C 51.2 ± 1.3 3.99 ± 0.14 −8.59 ± 0.17* 4.76 ± 0.17 −9.32 ± 0.17*
SEP/L7.38F/L7.43F/A7.46P/P7.47C 62.1 ± 1.7 5.27 ± 0.13 −8.79 ± 0.11* 5.79 ± 0.14 −9.43 ± 0.11*
  • N.D., not determined.

  • * P < 0.05 versus wild-type gm2.