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. Author manuscript; available in PMC: 2020 Apr 1.
Published in final edited form as: J Biomol Struct Dyn. 2018 May 17;37(7):1685–1699. doi: 10.1080/07391102.2018.1464957

Figure 4. (A). Comparison of binding affinity of SR-49059, SSR-149415, and the Manning compound with cV1aR and cV1bR.

Figure 4.

Docking analysis of ligands (agonist AVT and three VT antagonists) with the modeled cV1aR and cV1bR structures was performed to compare the binding affinity of each ligand to the receptors. Data (mean ± SEM) were obtained from twenty repetitions and are presented as the negative values of ΔGbinding (kcal/mol). (B). Dose-dependent inhibiting effect of two selected cV1bR antagonists, SSR-149415 and L-368899 on POMC hnRNA expression in AP cells following AVT/CRH treatments (1.0/0.1 nM, 6 hrs). The selected antagonists were applied 30 min before AVT/CRH treatments using 1, 10, 100, and 1000 pM concentrations to the AP cells. Total RNAs from AP cells were used for real-time RT-PCR of POMC hnRNA expression. (C). Combined inhibitory effects of selected antagonists on POMC hnRNA expression in AP cells. Selected antagonists for cV1aR and cV1bR (SR-49059/SSR-149415, SR-49059/L-368899, Manning/SSR-149415, and Manning/L-368899) were tested for 30 min followed by AVT/CRH (1.0 / 0.1 nM) administration. Six hours later, total RNAs were extracted and real time RT-PCR was performed for POMC hnRNA expression. Data were set as the fold changes of relative expression levels using the ΔΔCt method with GAPDH and β-actin as internal controls.