Journal: EJNMMI Research

Article Title: Heteroaryl derivatives of suvorexant as OX1R selective PET ligand candidates: Cu-mediated 18 F-fluorination of boroxines, in vitro and initial in vivo evaluation

doi: 10.1186/s13550-024-01141-2

Figure Lengend Snippet: Basolateral-to-apical transport of the P-gp substrate digoxin in P-gp expressing Caco-2 monolayers in the absence and presence of the P-gp inhibitor zosuquidar (ZSQ) ( A ) compared to basolateral-to-apical transport of 1c , 1f , 1b and 1d in the presence and absence of ZSQ ( B ). Amounts being present after 4 h in the apical compartment are shown in % of the amount administered to the basal side. Digoxin and all test compounds were each used in a concentration of 5 µM (ns: p ≥ 0.05, *p < 0.05, ***p < 0.001, n = 8)

Article Snippet: In brief, transport from the basolateral to apical compartment was determined after 4 h in the absence or presence of the P-gp inhibitor zosuquidar (Biomol GmbH, Hamburg, Germany).

Techniques: Expressing, Concentration Assay

Journal: International journal of pharmaceutics

Article Title: Circumvention of P-gp and MRP2 mediated efflux of lopinavir by a histidine based dipeptide prodrug

doi: 10.1016/j.ijpharm.2016.08.027

Figure Lengend Snippet: A–B permeability of LPV, Leu-LPV, His-Leu-LPV and LPV in presence of GF120918 and MK571 across MDCK-MDR1 and MDCK-MRP2 cells repsectively. The standard deviation for each data point was averaged over four samples (n=4). **P<0.05 compared with the control group.

Article Snippet: Unlabeled LPV and P-gp inhibitor, GF120918 were generous gift from Abbott Laboratories Inc. (North Chicago, IL, USA).

Techniques: Permeability, Standard Deviation, Control

Journal: International Journal of Molecular Sciences

Article Title: In Vitro Characterization of Renal Drug Transporter Activity in Kidney Cancer

doi: 10.3390/ijms231710177

Figure Lengend Snippet: P-glycoprotein drug transport activity. Uptake of calcein-AM in the presence or absence of the P-gp inhibitor valspodar. Functional data derived from fluorescent assays were fitted according to Michaelis–Menten kinetics to evaluate the drug transport activity in RPTEC-TERT1 cells ( A ), CAKI-1 cells ( B ), and 786-O cells ( C ). An increase in calcein retention after inhibition indicated the presence of P-gp-mediated efflux activity. Functional data were obtained from a minimum of two independent assays, performed in triplicate.

Article Snippet: Calcein fluorescence indicated that calcein-AM was not being secreted via P-gp, and its accumulation was evaluated using the specific P-gp inhibitor valspodar (Merck) (25 µM).

Techniques: Drug Transport Assay, Activity Assay, Functional Assay, Derivative Assay, Inhibition

Journal: International Journal of Molecular Sciences

Article Title: In Vitro Characterization of Renal Drug Transporter Activity in Kidney Cancer

doi: 10.3390/ijms231710177

Figure Lengend Snippet: Immunofluorescent localization of P-gp in non-tumor and RCC cell lines. In RPTEC-TERT1 cells ( A ), P-gp expression was seen dispersed throughout the cytoplasm, with no predominant localization in particular cellular structures. In CAKI-1 ( B ) and 786-O ( C ) cells, P-gp expression was seemingly confined to the nuclear region of the cells, which was evident from the co-localization of the nuclear tracer (blue) and the P-gp stain (red). Panels A1 , B1 , and C1 represent a composite image, including a nuclear tracer (Hoechst33342, blue), f-actin (Alexa488, green), and P-gp (Alexa555, red). Panels A2 , B2 , and C2 represent a composite image of P-gp and f-actin. Panels A3 , B3 , and C3 represent a composite image of P-gp and the nuclear staining. The images in panels A1 , B1 , and C1 were acquired with a magnification of 20× to provide an overview of cell density and monolayer growth. The images in panels A2,A3 , B2,B3 , and C2,C3 were acquired with a magnification of 60× to capture the cellular morphology in detail.

Article Snippet: Calcein fluorescence indicated that calcein-AM was not being secreted via P-gp, and its accumulation was evaluated using the specific P-gp inhibitor valspodar (Merck) (25 µM).

Techniques: Expressing, Staining

Journal: International Journal of Molecular Sciences

Article Title: In Vitro Characterization of Renal Drug Transporter Activity in Kidney Cancer

doi: 10.3390/ijms231710177

Figure Lengend Snippet: Effects of P-gp inhibition on cisplatin toxicity. The inhibitor valspodar reduced the cisplatin toxicity in RPTEC-TERT1 cells ( A ), but had no effect on CAKI-1 ( B ) and 786-O ( C ) cells. Similar effects were observed with the fluorescently labeled apoptosis marker annexin V, after a 200 µM cisplatin exposure. Annexin V fluorescence increased in RPTEC-TERT1 cells after cisplatin treatment ( D , G2 ) relative to the untreated cells ( G1 ), an effect that was absent when cisplatin was co-exposed with the P-gp inhibitor valspodar ( G3 ). Annexin V fluorescence was not affected by cisplatin in CAKI-1 ( E ) and 786-O ( F ) cells. The concentration of 200 µM was selected in order to induce limited toxicity and prevent excessive cell death. Images in panels G1–3 were acquired with a magnification of 20×.

Article Snippet: Calcein fluorescence indicated that calcein-AM was not being secreted via P-gp, and its accumulation was evaluated using the specific P-gp inhibitor valspodar (Merck) (25 µM).

Techniques: Inhibition, Labeling, Marker, Fluorescence, Concentration Assay

Journal: International Journal of Molecular Sciences

Article Title: In Vitro Characterization of Renal Drug Transporter Activity in Kidney Cancer

doi: 10.3390/ijms231710177

Figure Lengend Snippet: List of chemicals/reagents used in this study.

Article Snippet: Calcein fluorescence indicated that calcein-AM was not being secreted via P-gp, and its accumulation was evaluated using the specific P-gp inhibitor valspodar (Merck) (25 µM).

Techniques:

Journal: Pharmacy and Therapeutics

Article Title: Betrixaban (Bevyxxa)

doi:

Figure Lengend Snippet: Pharmacological Characteristics of Direct Oral Anticoagulants 16 – 18

Article Snippet: Dabigatran Pradaxa, Boehringer Ingelheim , Factor IIa , 6 , Twice daily , 12–14 , > 80 , 82–88 , Potent inducers and inhibitors of P-gp.

Techniques: