roflumilast (pde4 inhibitor)  (Tocris)

Journal: British journal of pharmacology

Article Title: Inhibition of the upregulated phosphodiesterase 4D isoforms improves SERCA2a function in diabetic cardiomyopathy.

doi: 10.1111/bph.17411

Figure Lengend Snippet: FIGURE 2 Inhibition of PDE4 rescues PKA phosphorylation of phospholamban and SR calcium load in high-fat diet (HFD)-fed cardiomyocytes. (a, b, f, g) Cardiac myocytes isolated from normal chow (NC) or HFD mice were treated with Roli (10 μM) for 10 min. Cells were lysed for western blots to detect the levels of phosphorylation of PLB at Ser16 and RYR2 at Ser2808. The quantification of western blot is shown in dot plots. (c–e) Cardiac myocytes loaded with calcium dye Fluo-4AM and paced at 1 Hz. Myocytes were treated with EHNA (10 μM), cilostamide (Cilo) (1 μM), rolipram (Roli) (10 μM) and sildenafil (Sild) (1 μM) as indicated. Calcium signals and SS were recorded. The maximal changes in sarcomere shortening (SS), calcium decay tau and transient amplitude were plotted. *P < 0.05 by two-way ANOVA followed by Tukey's test.

Article Snippet: The HFD group was randomly divided into a vehicle (saline or 0.05% sodium carboxymethylcellulose) group, a 10 mg kg 1 PDE4 inhibitor roflumilast treatment group (dissolved in saline; Elmasry et al., 2022; Hatzelmann et al., 2010), or a 0.03 mg kg 1 PDE4D inhibitor BPN14770 (Selleck, Houston, TX, USA) treatment group (dissolved in 0.05% sodium carboxymethylcellulose; Y. Wang et al., 2020).

Techniques: Inhibition, Phospho-proteomics, Isolation, Western Blot

Journal: Signal Transduction and Targeted Therapy

Article Title: Signaling pathways in obesity: mechanisms and therapeutic interventions

doi: 10.1038/s41392-022-01149-x

Figure Lengend Snippet: Weight-loss drugs in clinical development after 2015

Article Snippet: PDE4/5 inhibitor , Roflumilast , Obesity , Altana Pharma , Phase 3 , NCT04800172.

Techniques: Inhibition