Table 5.
Reports of P-gp transporter sensitivity for some PET radioligands across species, based on in vitro assays and on in vivo, mainly PET, studies.
| Radioligand | Imaging target | In vivo species | In vitro species | Substrate (Yes/No) | Reference |
|---|---|---|---|---|---|
| [11C]Carazolol | β-AR | M (g) | Yes | [191] | |
| [11C]Carazolol | β-AR | R (pc) | Yes | [191] | |
| [18F]S-1′-fluorocarazolol | β-AR | M (g) | Yes | [191] | |
| [18F]S-1′-fluorocarazolol | β-AR | R (pc) | Yes | [191] | |
| [18F]FCWAY | 5-HT1A | H (c) | Yes | [192] | |
| [18F]FCWAY | 5-HT1A | H (pt) | Yes | [192] | |
| [18F]MPPF | 5-HT1A | M (g) | Yes | [193] | |
| [18F]MPPF | 5-HT1A | M (g) | Yes | [194] | |
| [18F]MPPF | 5-HT1A | M (p) | Yes | [194] | |
| [18F]MPPF | 5-HT1A | R | Yes | [195] | |
| [18F]MPPF | 5-HT1A | R (pc) | Yes | [193] | |
| [18F]MPPF | 5-HT1A | R (pc) | Yes | [196] | |
| [18F]MPPF | 5-HT1A | NHP (pc) | No | [194] | |
| [18F]MPPF | 5-HT1A | H (c) | No | [197] | |
| [11C]RWAY | 5-HT1A | M | Yes | [198] | |
| [11C]RWAY | 5-HT1A | R | Yes | [198] | |
| [11C]RWAY | 5-HT2A | NHP | No | [154] | |
| [11C]WAY | 5-HT1A | R (pc) | Yes | [193] | |
| [11C]WAY | 5-HT1A | H (c) | No | [197] | |
| [18F]Altanserin | 5-HT2A | R (pc) | Yes | [190] | |
| [18F]Altanserin | 5-HT2A | R (pc) | Yes | [199] | |
| [18F]Altanserin | 5-HT2A | GP (pc) | Yes | [190] | |
| [18F]Altanserin | 5-HT2A | MP (pc) | Yes | [190] | |
| [18F]Altanserin | 5-HT2A | NHP (pc) | Yes | [190] | |
| [18F]MH-MZ | 5-HT2A | M (pc) | Yes | [200] | |
| [11C]PIB | Aβ | M (pc) | No | [201] | |
| [11C]PIB | Aβ | H (c) | No | [197] | |
| [11C]Flumazenil | Bz | R (pt) | Yes | [202] | |
| [11C]Flumazenil | Bz | M (pc) | Yes | [201] | |
| [11C]Flumazenil | Bz | H (c) | No | [197] | |
| [11C]MePPEP | CB1 | M (g) | No | [203] | |
| [11C]MePPEP | CB1 | NHP (pd) | No | [164] | |
| [18F]Fallypride | D2/D3 | M (pc) | Yes | [204] | |
| [18F]Fallypride | D2/D3 | M (g) | Yes | [204] | |
| [18F]Fallypride | D2/D3 | R (pc) | Yes | [204] | |
| [18F]Fallypride | D2/D3 | H (c) | No | [197] | |
| [11C]Raclopride | D2/D3 | M (pc) | No | [201] | |
| [11C]Raclopride | D2/D3 | H (c) | No | [197] | |
| [11C]Befloxatone | MAO-A | R (c) | No | [205] | |
| [11C]Befloxatone | MAO-A | H (c) | No | [197] | |
| [11C]GR205171 | NK1 | M (g) | Yes | [206] | |
| [11C]GR205171 | NK1 | R (pc) | Yes | [190] | |
| [11C]GR205171 | NK1 | GP (pc) | Yes | [190] | |
| [11C]GR205171 | NK1 | NHP (pc) | Yes | [190] | |
| [11C]PK11195 | TSPO | M (pc) | No | [201] | |
| [11C]PK11195 | TSPO | H (c) | No | [197] |
M = Mouse, R = Rat, GP = Guinea pig; MP = mini-pig; NHP = non-human primate; H = Human, c = cell-based assay; g = efflux transporter knockout; pc = pharmacological block of efflux transporter with cyclosporin A; pd = pharmacological block of efflux transporter with DCPQ; pt = pharmacological block of efflux transporter with tariquidar.