Table 11.
Human in-vitro models of the blood–brain barrier. Receptor and transporter expression and function.
| Model type | ABC transporter expression/function | Vectorial net transport of ABC substrates | TFR expression/ function | LAT-1 expression/ function | Glut-1 expression/ function | MCT-1 expression/ function | Selected key references |
|---|---|---|---|---|---|---|---|
| hCMEC3/D3 (immortalized human brain endothelial cells) | P-gp (mRNA, PROT, WB) BCRP (mRNA, PROT, WB) Mrp-1 (mRNA,WB, PROT) Inhibitor data on uptake for all MRP5 (mRNA) | – | PROT | Not detected in proteomics study. However, uptake of gabapentin inhibitable by LAT-1 inhibition has been shown | PROT | PROT | 114,252,260 |
| hPSC (human pluripotent stem cells) | P-gp (ICC, mRNA) BCRP (ICC, mRNA) Mrp-1 (ICC, mRNA) Mrp-2, 4 and -5 (mRNA) Inhibitor data on uptake and transport for all | – | mRNA | mRNA | ICC, mRNA, relatively high PGlucose compared to PSucrose | mRNA | 118,256 |
| Cord blood-derived endothelial progenitor cells | P-gp (ICC, mRNA, WB) Inhibitor data on uptake BCRP (mRNA) Mrp-1, -4 and -5 (mRNA) | – | mRNA | mRNA | mRNA | mRNA | 116,117 |
–
: not investigated; ICC: immunocytochemistry; WB: Western blotting; PROT: MS-based proteomics; BCRP: breast cancer resistance protein; Mrp: multidrug-resistance protein.
Note: The permeability value of the smallest tested compound in the study is given.