Table 2

Histamine-induced cAMP production in HEK-293 cells transiently expressing the D115A or D115N mutant H2 receptor or different levels of the wild-type H2 receptor

H2ReceptorBmaxEC50Emax
fmol/mg nM pmol/well
WT341341  ± 70180  ± 3212  ± 2
WT632632  ± 100151  ± 6320  ± 1*
WT15361536  ± 157151  ± 5142  ± 6**
D115N231  ± 34121  ± 4688  ± 12***
D115A305  ± 60222  ± 9566  ± 13**

Cells were incubated with increasing concentrations of histamine for 10 min at 37°C in DMEM in the presence of 300 μM IBMX and 25 mM HEPES, pH 7.4. Data represent the mean ± S.E. of three to six independent experiments. The asterisks indicate a significant difference from HEK-293 cells transiently expressing the wild-type receptor at a density of 341 fmol/mg protein (see Materials and Methods).