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EJNMMI Research

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
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