Structure–activity relationships of Cmpd-6 analogs

Different chemical scaffolds in the R2 and R3 regions between Cmpd-6 and its analogs are illustrated. Changes in the Vmax value by Cmpd-6 or each analog at 32 μM are expressed as percentages of the maximal level of the ISO-induced activity in the vehicle (DMSO) control in each assay. Changes in the EC50 value are expressed as fold shifts compared with the control value obtained in the vehicle (DMSO)-treated curve in each assay. Every value represents mean ± S.D. obtained from four independent experiments done in duplicate. Statistical analyses were performed using one-way analysis of variance with Dunnett’s multiple comparison post-tests compared with the control Cmpd-6–treated value in each assay. Adjusted *P < 0.05; **P < 0.01; ***P < 0.001.

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  • Rc, receptor.