Evaluation of an inverse agonist with high affinity for the CB1 receptor, [11C]MePPEP, in rodents and humans

Rodents afforded us the opportunity to: use genetic knockouts to test receptor selectivity and susceptibility to transport by P-glycoprotein (P-gp); dose with high concentrations of agonists to test sensitivity of [11C]MePPEP displacement; check for accumulation of radiometabolites in the brain, whi...

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Bibliographic Details
Published inNeuroImage (Orlando, Fla.) Vol. 41; p. T197
Main Authors Terry, Garth E., Liow, J.-S., Chernet, E., Zoghbi, S.S., Phebus, L., Lerner, A., Felder, C.C., Tauscher, J., Schaus, J.M., Pike, V.W., Halldin, C., Innis, R.B.
Format Journal Article
LanguageEnglish
Published Amsterdam Elsevier Limited 01.01.2008
Subjects
Brain
Dosimetry
Human subjects
Rodents
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Summary:Rodents afforded us the opportunity to: use genetic knockouts to test receptor selectivity and susceptibility to transport by P-glycoprotein (P-gp); dose with high concentrations of agonists to test sensitivity of [11C]MePPEP displacement; check for accumulation of radiometabolites in the brain, which would disrupt compartment modeling. Using serial measurements of PET brain activity and plasma concentrations of [11C]MePPEP, we estimated CB1 receptor density in rat brain as distribution volume.
Bibliography:ObjectType-Article-1
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content type line 14
ISSN:1053-8119
1095-9572
DOI:10.1016/j.neuroimage.2008.04.164