Asset Details
Do you wish to reserve the book?
In vitro and in vivo Human Metabolism of (S)-18FFluspidine – A Radioligand for Imaging σ1 Receptors With Positron Emission Tomography (PET)
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
In vitro and in vivo Human Metabolism of (S)-18FFluspidine – A Radioligand for Imaging σ1 Receptors With Positron Emission Tomography (PET)
Do you wish to request the book?
In vitro and in vivo Human Metabolism of (S)-18FFluspidine – A Radioligand for Imaging σ1 Receptors With Positron Emission Tomography (PET)
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
In vitro and in vivo Human Metabolism of (S)-18FFluspidine – A Radioligand for Imaging σ1 Receptors With Positron Emission Tomography (PET)
2019
Overview
( S )-[18F]fluspidine (( S )-[18F] 1 ) has recently been explored for positron emission tomography (PET) imaging of sigma-1 receptors in humans. In the current report, we have used plasma samples of healthy volunteers to investigate the radiometabolites of ( S )-[18F] 1 and elucidate their structures with LC-MS/MS. For the latter purpose additional in vitro studies were conducted by incubation of ( S )-[18F] 1 and ( S )- 1 with human liver microsomes (HLM). In vitro metabolites were characterized by interpretation of MS/MS fragmentation patterns from collision-induced dissociation or by use of reference compounds. Thereby, structures of corresponding radio-HPLC-detected radiometabolites, both in vitro and in vivo (human), could be identified. By incubation with HLM, mainly debenzylation and hydroxylation occurred, beside further mono- and di-oxygenations. The product hydroxylated at the fluoroethyl side chain was glucuronidated. Plasma samples (10, 20, 30 min p.i., n = 5-6), obtained from human subjects receiving 250–300 MBq ( S )-[18F] 1 showed 97.2, 95.4, and 91.0% of unchanged radioligand, respectively. In urine samples (90 min p.i.) the fraction of unchanged radioligand was only 2.6% and three major radiometabolites were detected. The one with the highest percentage, also found in plasma, matched the glucuronide formed in vitro . Only a small amount of debenzylated metabolite was detected. In conclusion, our metabolic study, in particular the high fractions of unchanged radioligand in plasma, confirms the suitability of ( S )-[18F] 1 as PET radioligand for sigma-1 receptor imaging.
Publisher
Frontiers Media SA,Frontiers Media S.A
Subject
We currently cannot retrieve any items related to this title. Kindly check back at a later time.