TABLE 2

Effect of mutations of Arg38(1.35) of the receptor to alanine and lysine on the GnRH peptide-stimulated IP responses

EC50 and Emax values are presented as mean ± S.E. of three or more independent experiments. The fold-change was calculated as the ratio of the EC50 values in the mutant and wild-type receptors. Emax is expressed relative to a wild-type control included in each transfection.



Wild-Type

R38A

R38K

EC50
Emax
EC50
EC50 -Fold Increase
Emax
EC50
EC50 -Fold Increase
Emax
nM % wt nM % wt nM % wt
GnRH I 0.87 ± 0.06 100 5672 ± 302 6520 42 ± 4 129 ± 9 146 100 ± 9
[Pro9,NHEt]GnRH I 0.18 ± 0.01 100 433 ± 21 2405 56 ± 3 14 ± 2 77 91 ± 6
GnRH II 26 ± 3 100 17070 ± 690 656 41 ± 5 1978 ± 334 76 104 ± 7
[Pro9,NHEt]GnRH II
1.9 ± 0.15
100
711 ± 62
374
58 ± 3
125 ± 12
65
96 ± 4