In:
Chemistry & Biodiversity, Wiley, Vol. 13, No. 7 ( 2016-07), p. 875-883
Abstract:
Here, we describe the very first attempt to visualize in vivo formyl peptide receptors ( FPR s) in mouse brain by positron emission tomography ( PET ). FPR s are expressed in microglial cells where they mediate chemotactic activity of β ‐amyloid peptide in Alzheimer disease and, thus, are involved in neuroinflammatory processes. To this purpose, we have selected (2 S )‐3‐(1 H ‐Indol‐3‐yl)‐2‐{[(4‐methoxyphenyl)carbamoyl]amino}‐ N ‐{[1‐(5‐methoxypyridin‐2‐yl)cyclohexyl]methyl}propanamide (( S )‐ 1 ), that we have previously identified as a potent non‐peptidic FPR agonist. ( S )‐[ 11 C]‐ 1 has been prepared in high radiochemical yield. ( S )‐[ 11 C]‐ 1 showed very low penetration of blood–brain barrier and, thus, was unable to accumulate into the brain. In addition, ( S )‐[ 11 C]‐ 1 was not able to label FPR s receptors in brain slices of PS 19 and APP 23 mice, two animal models of Alzheimer disease. Although ( S )‐[ 11 C]‐ 1 was not suitable to visualize FPR s in the brain, this study provides useful information for the design and characterization of future potential PET radioligands for visualization of brain FPR s by PET .
Type of Medium:
Online Resource
ISSN:
1612-1872
,
1612-1880
DOI:
10.1002/cbdv.201500281
Language:
English
Publisher:
Wiley
Publication Date:
2016
detail.hit.zdb_id:
2139001-0
SSG:
12
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