In:
CHIMIA, Swiss Chemical Society, Vol. 68, No. 4 ( 2014-04-30), p. 208-
Abstract:
The cannabinoid receptor type 2 (CB2) has a very low expression level in brain tissue under basal conditions, but it is up-regulated in diverse pathological conditions. Two promising lead structures from the literature, N-((3S,5S,7S)-adamantan-1-yl)-8-methoxy-4-oxo-1-pentyl-1,4-dihydroquinoline-3-carboxamide
and 8-butoxy-N-(2-fluoro-2-phenylethyl)-7-methoxy-2-oxo-1,2-dihydroquinoline-3-carboxamide – designated KD2 and KP23, respectively – were evaluated as potential PET ligands for imaging CB2. Both KD2 and KP23 were synthesized and labeled with carbon-11. In vitro autoradiographic studies on rodent spleen tissues showed that [11C]KD2 exhibits superior properties. A pilot study using [11C] KD2 on human post mortem ALS spinal cord slices indicated high CB2 expression level and specific binding, a very exciting finding if considering the future diagnostic
application of CB2 ligands and their utility in therapy monitoring. In vivo blocking studies in rats with [11C] KD2 showed also high specific uptake in spleen tissue. Although the protein-bound fraction is relatively high, KD2 or KD2 derivatives could be very useful tools
for the non-invasive investigation of CB2 levels under various neuroinflammatory conditions.
Type of Medium:
Online Resource
ISSN:
2673-2424
,
0009-4293
DOI:
10.2533/chimia.2014.208
Language:
Unknown
Publisher:
Swiss Chemical Society
Publication Date:
2014
detail.hit.zdb_id:
2179192-2
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