Figure 2.
Constitutive activity of hmGlu5a receptor is decreased by N-terminal cysteine to serine mutations. HEK293 cells were transiently transfected with cDNAs coding for hmGlu5a WT or the indicated mutated receptors. IP production concentration–response curve of MPEP (a) or MTEP (b) applied on HEK293 expressing the WT or the indicated mutated receptors together with rEAAC1 and Gαq. The signal window between the constitutive activity and the ground state corresponds to 498±44 to 368±15 c.p.m.for the WT and 431±83 to 367±64 c.p.m. for the C57/99S mutant, respectively. For the tetramutant 4C-S, no MPEP- or MTEP-mediated inhibition could be measured. Mutant receptors C93S and C129S behaved as the WT (not shown). The presented data are the mean±s.e.m. of three experiments performed in quadruplicates from three independent transfections and is expressed as the percentage of the WT alone.