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Table 2 Short summary of tracer evaluation in rats, pigs and humans

From: Blocking of efflux transporters in rats improves translational validation of brain radioligands

Tracer Target-specific binding confirmed Prediction outcomec Translated to humans
Rat Pig
Traditionala P-gpIb
[18F]MH.MZ Yes Yes Yes Yes
[18F]Altanserin No Yes Yes Yes
[11C]Pimavanserin No No No  
[11C]Cimbi-36 Yes Yes Yes Yes
[11C]Cimbi-717 No No Yes  
[11C]Cimbi-701 No No Yes  
[11C]BA-10 No Yes Yes  
[18F]Fallypride Yes Yes Yes Yes
  1. Concrete estimates of target-specific binding at baseline and its changes in response to target receptor blockade in rats and pigs, as well as estimates of target-specific binding in humans are summarized in Additional file 1: Table S3
  2. aTraditional evaluation workflow without P-gp inhibition
  3. bP-gpI = P-gp inhibition
  4. cPrediction outcome indicates if the evaluation outcome in pigs could (thumb up) or could not (thumb down) be correctly predicted from evaluation outcome in rats