Fig. 9.

Modulatory effect of LUF6096 in assays with HEK 293 cell membranes expressing the mEL1-hA₃AR mutant. a Effect of LUF6096 (10 μM) on [³⁵S]GTPγS binding while stimulating with a maximal concentration of Cl-IB-MECA (10 μM). b Effect of increasing concentrations of LUF6096 on [³⁵S]GTPγS binding in response to Cl-IB-MECA (10 μM). Data in this panel are presented as a percentage of maximal [³⁵S]GTPγS binding. c Effect of increasing concentrations of LUF6096 on binding of [¹²⁵I]I-AB-MECA in the hybrid association/equilibrium binding assay involving comparison of specific binding at 3 and 18 h. d Effect of LUF6096 on [¹²⁵I]I-AB-MECA dissociation kinetics. All of the assays were conducted as described in “Materials and methods” and in previous figure legends. Data are the mean ± SEM of four to eight experiments performed in triplicate ([¹²⁵I]I-AB-MECA binding assays) or quadruplicate ([³⁵S]GTPγS binding assays). Asterisk: P < 0.05 versus the wild-type human A₃AR by an unpaired Student’s t test