Abstract:
:The vesicular acetylcholine transporter (VAChT) is a glycoprotein responsible for the accumulation of acetylcholine into pre-synaptic vesicules of cholinergic neurons. Cholinergic innervation has been shown to be decreased at the earlier stages of Alzheimer's disease (AD). Thus, the expression of VAChT has been correlated with the severity of the dementia and has been considered as a significant diagnostic target for AD. To this end numerous radioligands based on the vesamicol scaffold have been developed for imaging the VAChT using positron emission tomography (PET). Among the various radioligands only a small number have been evaluated in vivo in non-human primate and human. Despite promising in vitro, ex vivo and first in vivo studies, most of them are unsuitable for clinical use in humans due to poor selectivity over σ receptors, low extraction from the blood, slow brain kinetics or fast metabolism. To date (-)-[(11)C]OMV (1), (-)-[(11)C]MABV (2), (-)-[(18)F]-FEOBV (6), (-)-trans-2-hydroxy-3-(4-(4-[(18)F]fluorobenzoyl)piperidine)tetralin (8) and [(18)F]FBMV (12) are promising radioligands for the VAChT, though further validation is required to confirm their clinical usefulness.
journal_name
Curr Top Med Chemjournal_title
Current topics in medicinal chemistryauthors
Giboureau N,Som IM,Boucher-Arnold A,Guilloteau D,Kassiou Mdoi
10.2174/156802610793176846subject
Has Abstractpub_date
2010-01-01 00:00:00pages
1569-83issue
15eissn
1568-0266issn
1873-4294pii
BSP/ CTMC /E-Pub/-0100-10-16journal_volume
10pub_type
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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abstract::Natural quinoline alkaloid camptothecin (CPT) is used for the treatment of colon, lung, breast and ovarian cancers still facing challenges due to low solubility in aqueous and biological fluids. Its lactone form easily converts into a toxic carboxylic form at slightly basic pH, typical in blood and tissue fluid has ra...
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journal_title:Current topics in medicinal chemistry
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