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Philippe_2013_Nucl.Med.Biol_40_919

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Title : Preclinical in vitro &\;in vivo evaluation of [(11)C]SNAP-7941 - the first PET tracer for the melanin concentrating hormone receptor 1 - Philippe_2013_Nucl.Med.Biol_40_919
Author(s) : Philippe C , Nics L , Zeilinger M , Kuntner C , Wanek T , Mairinger S , Shanab K , Spreitzer H , Viernstein H , Wadsak W , Mitterhauser M
Ref : Nucl Med Biol , 40 :919 , 2013
Abstract :

INTRODUCTION: Due to its involvement in a variety of pathologies (obesity, diabetes, gut inflammation and depression), the melanin concentrating hormone receptor 1 (MCHR1) is a new target for the treatment of these lifestyle diseases. We previously presented the radiosynthesis of [(11)C]SNAP-7941, the first potential PET tracer for the MCHR1.
METHODS: We herein present its in vitro and in vivo evaluation, including binding affinity, plasma stability, stability against liver mircrosomes and carboxylesterase, lipohilicity, biodistribution, in vivo metabolism and small-animal PET.
RESULTS: [(11)C]SNAP-7941 evinced high stability against liver microsomes, carboxylesterase and in human plasma. The first small-animal PET experiments revealed a 5 fold increased brain uptake after Pgp/BCRP inhibition. Therefore, it can be assumed that [(11)C]SNAP-7941 is a Pgp/BCRP substrate. No metabolites were found in brain. CONCLUSION: On the basis of these experiments with healthy rats, the suitability of [(11)C]SNAP-7941 for the visualisation of central and peripheral MCHR1 remains speculative.
PubMedSearch : Philippe_2013_Nucl.Med.Biol_40_919
PubMedID: 23829932

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Philippe C, Nics L, Zeilinger M, Kuntner C, Wanek T, Mairinger S, Shanab K, Spreitzer H, Viernstein H, Wadsak W, Mitterhauser M (2013)
Preclinical in vitro &\;in vivo evaluation of [(11)C]SNAP-7941 - the first PET tracer for the melanin concentrating hormone receptor 1
Nucl Med Biol 40 :919

Philippe C, Nics L, Zeilinger M, Kuntner C, Wanek T, Mairinger S, Shanab K, Spreitzer H, Viernstein H, Wadsak W, Mitterhauser M (2013)
Nucl Med Biol 40 :919