Figure 3.

Antagonism of prazosin-induced upregulation by KMD-3213 in mutant alpha-1a AR. (A) CHO cells expressing the mutant alpha-1a AR were treated for 48 h with various concentrations of prazosin in the absence or presence of 1 nM KMD-3213, and the specific binding of [³H]-prazosin was measured. B_max values were expressed as per cent of the B_max in the membrane from the cells treated with no drug and represented mean±s.e.mean from five independent experiments. (B) CHO cells expressing the mutant alpha-1a AR were co-incubated for 48 h with 1 nM prazosin in the presence of various concentrations of KMD-3213 and the specific binding of [³H]-prazosin was measured. The up-regulation of the receptor density is expressed as per cent of the up-regulation in the membrane from the cells treated with prazosin only and represented mean±s.e.mean from four experiments.