Journal: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

Article Title: Impact of 5-HT7 receptor inverse agonism of lurasidone on monoaminergic tripartite synaptic transmission and pathophysiology of lower risk of weight gain.

doi: 10.1016/j.biopha.2022.112750

Figure Lengend Snippet: Fig. 4. Concentration-dependent effects of subchronic (panel A) and chronic (panel B) administration of lurasidone on 5-HT1AR protein expression in the plasma membrane fraction, using capillary immunoblotting. In the right-side panels pseudo-gel images of GAPDH and 5-HT1AR using capillary immunoblotting were represented. In the left-side panels, ordinate: mean ± SD (n = 6) of the relative protein level of 5-HT1AR (per GAPDH). Concentration-dependent effects of lur asidone (100 and 300 nM) on 5-HT1AR expression in the primary cultured astrocytes were analysed by one-way ANOVA with Tukey’s post hoc test (*P < 0.05, **P < 0.01 vs. control (lurasidone free)).

Article Snippet: Antibodies against GAPDH (NB300–327, 1:300, Novus Biologicals, Littleton, CO, USA), connexin43 (C6219, 1:100, Sigma-Aldrich, St. Louis, MO, USA), 5-HT1AR (NBP2–21590, 1:00, Novus Biologicals), 5-HT7R (NB100–56352, 1:00, Novus Biologicals), ERK (AF1576, 10 μg/mL, R&D systems, Minneapolis, MN, USA), phosphorylated-ERK (AF1018, 5 μg/mL, R&D Systems), AKT (AF1775, 1 μg/mL, R&D Systems), phosphorylated-AKT (AF877, 5 μg/mL, R&D Systems), AMPKα (2603, 1:50, Cell Signalling Technology, Danvers, MA, USA), and phosphorylated-AMPKα (2535, 1:50, Cell Signalling Technology) were diluted in an antibody diluent (Immuno Shot Platinum, CosmoBio) [23].

Techniques: Concentration Assay, Expressing, Clinical Proteomics, Membrane, Western Blot, Cell Culture, Control

Journal: MedChemComm

Article Title: Controlling cellular distribution of drugs with permeability modifying moieties † †Electronic supplementary information (ESI) available: Synthetic experimental details and extended assay results for select compounds. See DOI: 10.1039/c8md00412a

doi: 10.1039/c8md00412a

Figure Lengend Snippet: clog P , CEREP 5-HT 1A and β 2 AR receptor cell-based binding data for alprenolol 6 derivatives based on thio–ene reaction

Article Snippet: IC 50 (μM) Change d 6 — 2.652 10.9 0.0216 1 0.630 1 0.0005 1 0.0033 1 6.2a Boc 2.761 0.035 0.0241 1.12 >1 — 0.0037 7.4 0.0069 2.09 6.2b H 0.954 0.032 0.0358 1.66 >1 — 0.0103 20.6 0.10 30.3 6.2c SCD –6.526 NV 2.86 132 >1 — 0.547 1094 0.50 151 6.2d SAA –3.150 0.0046 0.261 12.1 >1 — 0.752 150 0.0834 25.3 6.2e CCT –1.986 0.0012 1.78 82.4 >1 — 0.512 1024 >1 303 Open in a separate window a NV (no value) indicates no permeability detected. b CEREP 5-HT 1A radioligand displacement assay and functional antagonist assays. c CEREP β 2 AR radioligand displacement and functional antagonist assays. d Change indicates ratio of assay results relative to 6 . caption a8 clog P , CEREP 5-HT 1A and β 2 AR receptor cell-based binding data for alprenolol 6 derivatives based on epoxide opening reaction

Techniques: Binding Assay

Journal: MedChemComm

Article Title: Controlling cellular distribution of drugs with permeability modifying moieties † †Electronic supplementary information (ESI) available: Synthetic experimental details and extended assay results for select compounds. See DOI: 10.1039/c8md00412a

doi: 10.1039/c8md00412a

Figure Lengend Snippet: clog P , CEREP 5-HT 1A and β 2 AR receptor cell-based binding data for alprenolol 6 derivatives based on epoxide opening reaction

Article Snippet: IC 50 (μM) Change d 6 — 2.652 10.9 0.0216 1 0.630 1 0.0005 1 0.0033 1 6.2a Boc 2.761 0.035 0.0241 1.12 >1 — 0.0037 7.4 0.0069 2.09 6.2b H 0.954 0.032 0.0358 1.66 >1 — 0.0103 20.6 0.10 30.3 6.2c SCD –6.526 NV 2.86 132 >1 — 0.547 1094 0.50 151 6.2d SAA –3.150 0.0046 0.261 12.1 >1 — 0.752 150 0.0834 25.3 6.2e CCT –1.986 0.0012 1.78 82.4 >1 — 0.512 1024 >1 303 Open in a separate window a NV (no value) indicates no permeability detected. b CEREP 5-HT 1A radioligand displacement assay and functional antagonist assays. c CEREP β 2 AR radioligand displacement and functional antagonist assays. d Change indicates ratio of assay results relative to 6 . caption a8 clog P , CEREP 5-HT 1A and β 2 AR receptor cell-based binding data for alprenolol 6 derivatives based on epoxide opening reaction

Techniques: Binding Assay