Please use this identifier to cite or link to this item: https://apo.ansto.gov.au/dspace/handle/10238/5907
Title: Synthesis and in vitro binding of N,N-Dialkyl-2-phenylindol-3-yl-glyoxylamides for the peripheral benzodiazepine binding sites.
Authors: Homes, T P
Mattner, F
Keller, P A
Katsifis, A
Keywords: CENTRAL NERVOUS SYSTEM
NERVOUS SYSTEM
IRON
IODINATION
BRAIN
INFLAMMATION
Issue Date: 1-Jun-2006
Publisher: PERGAMON-ELSEVIER SCIENCE LTD
Citation: Homes, T. P., Mattner, F., Keller, P. A., & Katsifis, A. (2006). Synthesis and in vitro binding of N,N-Dialkyl-2-phenylindol-3-yl-glyoxylamides for the peripheral benzodiazepine binding sites. Bioorganic and Medicinal Chemistry, 14(11), 3938-3946.
Abstract: A series of NN-dialkyl-2-phenylindol-3-glyoxylamides bearing the halogens iodine and bromine were synthesised and their binding affinity for the peripheral benzodiazepine binding sites (PBBS) in rat kidney mitochondrial membranes was evaluated Using [H-3]PK11195. Central benzodiazepine receptor (CBR) affinities were also evaluated in rat cortices using [H-3]flumazenil to determine their selectivity for PBBS over CBR. The tested compounds had PBBS binding affinities (IC50) ranging from 7.86 to 618 nM, with all compounds showing high selectivity over the CBR (CBR IC50 > 5000 nM). Among the 12 compounds tested, those with a diethylamide group were the most potent. The highest affinity iodinated PBBS ligand, N,N-diethyl-[5-chloro-2-(4-iodophenyl)indol-3-yl]glyoxylamide (4c), was radiolabelled with iodine-123. This high affinity and selective radioligand may be useful for imaging neurodegencration, inflammation and tumours using single photon emission computed tomography. © 2006, Elsevier Ltd.
Gov't Doc #: 4522
URI: http://dx.doi.org/10.1016/j.bmc.2006.01.039
http://apo.ansto.gov.au/dspace/handle/10238/5907
ISSN: 0968-0896
Appears in Collections:Journal Articles

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