Journal: Pharmacology Research & Perspectives

Article Title: In vitro evaluation suggests fenfluramine and norfenfluramine are unlikely to act as perpetrators of drug interactions

doi: 10.1002/prp2.959

Figure Lengend Snippet: IC 50 and % of inhibition of selected CYP450s by Fenfluramine (FFA) and norfenfluramine (nFFA) and the calculated ratio of intrinsic clearance values R 1

Article Snippet: FFA hydrochloride and nFFA hydrochloride—[1‐(3‐trifluoromethyl) phenyl]propan‐2‐amine hydrochloride—were obtained from Zogenix, Inc. (Emeryville, CA).

Techniques: Inhibition

Journal: Pharmacology Research & Perspectives

Article Title: In vitro evaluation suggests fenfluramine and norfenfluramine are unlikely to act as perpetrators of drug interactions

doi: 10.1002/prp2.959

Figure Lengend Snippet: Evaluation of Fenfluramine (FFA) and norfenfluramine (nFFA) potential to induce CYP1A2, CYP2B6, or CYP3A4 mRNA in vivo

Article Snippet: FFA hydrochloride and nFFA hydrochloride—[1‐(3‐trifluoromethyl) phenyl]propan‐2‐amine hydrochloride—were obtained from Zogenix, Inc. (Emeryville, CA).

Techniques: In Vivo, Control

Journal: Pharmacology Research & Perspectives

Article Title: In vitro evaluation suggests fenfluramine and norfenfluramine are unlikely to act as perpetrators of drug interactions

doi: 10.1002/prp2.959

Figure Lengend Snippet: Effects of various concentrations of fenfluramine (FFA), norfenfluramine (nFFA), or control on CYP1A2, CYP2B6, and CYP3A4 mRNA levels. Primary human hepatocyte cultures from three donors were incubated for 72 h with medium containing 0−40 µM FFA, 0−50 µM nFFA, or positive and negative controls. Levels of CYP1A2 mRNA (A), CYP2B6 mRNA (B), and CYP3A4 mRNA (C) were measured by quantitative polymerase chain reaction and were normalized first to the levels of glyceraldehyde 3‐phosphate dehydrogenase mRNA, and then to the levels of corresponding CYP450 mRNAs in vehicle control cultures, as described in Materials and Methods . Hashed lines indicate 2‐fold induction threshold

Article Snippet: FFA hydrochloride and nFFA hydrochloride—[1‐(3‐trifluoromethyl) phenyl]propan‐2‐amine hydrochloride—were obtained from Zogenix, Inc. (Emeryville, CA).

Techniques: Control, Incubation, Real-time Polymerase Chain Reaction

Journal: Pharmacology Research & Perspectives

Article Title: In vitro evaluation suggests fenfluramine and norfenfluramine are unlikely to act as perpetrators of drug interactions

doi: 10.1002/prp2.959

Figure Lengend Snippet: Fenfluramine (FFA) and norfenfluramine (nFFA) potential to inhibit drug transporters—definitions and values of R

Article Snippet: FFA hydrochloride and nFFA hydrochloride—[1‐(3‐trifluoromethyl) phenyl]propan‐2‐amine hydrochloride—were obtained from Zogenix, Inc. (Emeryville, CA).

Techniques:

Journal: Pharmacology Research & Perspectives

Article Title: In vitro evaluation suggests fenfluramine and norfenfluramine are unlikely to act as perpetrators of drug interactions

doi: 10.1002/prp2.959

Figure Lengend Snippet: Inhibition of OCT2 and MATE1 drug transporters by fenfluramine (FFA) and norfenfluramine (nFFA). Accumulation of 14 C‐metformin uptake into HEK‐OCT2 cells in the presence of (A) FFA or (B) nFFA. Accumulation of 14 C‐metformin into HEK‐MATE1 cells in the presence of (C) FFA or (D) nFFA

Article Snippet: FFA hydrochloride and nFFA hydrochloride—[1‐(3‐trifluoromethyl) phenyl]propan‐2‐amine hydrochloride—were obtained from Zogenix, Inc. (Emeryville, CA).

Techniques: Inhibition