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Table 3 Inhibitory effects of various compounds on diphenhydramine uptake by hCMEC/D3 cells

From: Functional expression of a proton-coupled organic cation (H+/OC) antiporter in human brain capillary endothelial cell line hCMEC/D3, a human blood–brain barrier model

Inhibitor

Concentration (mM)

Relative uptake (% of control)

  

Amantadine

1

23.7 ± 3.8 ***

  

Quinidine

1

24.0 ± 6.2 ***

  

TEA

1

98.9 ± 12.3

  

Serotonin

1

84.7 ± 14.9

  

MPP+

1

90.2 ± 11.4

  

Choline

1

74.1 ± 7.3

  
  1. The inhibitory effects of selected compounds on diphenhydramine uptake by hCMEC/D3 cells. Uptake of diphenhydramine (30 μM) was measured at 37°C for 15 sec in the transport medium (pH 7.4) containing each compound (1 mM). Each column represents mean ± S.E. of three determinations. Asterisks show a significant difference, *** P < 0.01 vs control.