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001-es BibID:	BIBFORM007318
Első szerző:	Gulyás Balázs
Cím:	A comparative autoradiography study in post mortem whole hemisphere human brain slices taken from Alzheimer patients and age-matched controls using two radiolabelled DAA1106 analogues with high affinity to the peripheral benzodiazepine receptor (PBR) system / Balázs Gulyás, Boglárka Makkai, Péter Kása, Károly Gulya, Lidia Bakota, Szilvia Várszegi, Zsuzsa Beliczai, Jan Andersson, László Csiba, Andrea Thiele, Thomas Dyrks, Tetsuya Suhara, Kazutoshi Suzuki, Makato Higuchi, Christer Halldin
Dátum:	2009
ISSN:	0197-0186 (Print)
Megjegyzések:	The binding of two radiolabelled analogues(N-(5-[125I]Iodo-2-phenoxyphenyl)-N-(2,5-dimethoxybenzyl)acetamide ([125I]desfluoro-DAA1106)and N-(5-[125I]Fluoro-2-phenoxyphenyl)-N-(2-[125I]Iodo-5-methoxybenzyl)acetamide ([125I]desmethoxy-DAA1106)of the peripheral benzodiazepine receptor(PBR)(or TSPO,18 kDa translocator protein)ligand DAA1106 was examined by in vitro autoradiography on human post mortem whole hemisphere brain slices obtained from Alzheimer's disease (AD)patients and age-matched controls. Both [125I]desfluoro-IDAA1106 and [125I]desmethoxy-IDAA1106 were effectively binding to various brain structures. The binding could be blocked by the unlabelled ligand as well as by other PBR specific ligands. With both radiolabelled compounds, the binding showed regional inhomogeneity and the specific binding values proved to be the highest in the hippocampus, temporal and parietal cortex, the basal ganglia and thalamus in the AD brains. Compared with age-matched control brains, specific binding in several brain structures (temporal and parietal lobes, thalamus and white matter) in Alzheimer brains was significantly higher, indicating that the radioligands can effectively label-activated microglia and the up-regulated PBR/TSPO system in AD. Complementary immunohistochemical studies demonstrated reactive microglia activation in the AD brain tissue and indicated that increased ligand binding coincides with increased regional microglia activation due to neuroinflammation. These investigations yield further support to the PBR/TSPO binding capacity of DAA1106 in human brain tissue, demonstrate the effective usefulness of its radioiodinated analogues as imaging biomarkers in post mortem human studies, and indicate that its radiolabelled analogues, labelled with short half-time bioisotopes, can serve as prospective in vivo imaging biomarkers of activated microglia and the up-regulated PBR/TSPO system in the human brain.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban Peripheral benzodiazepine receptor (PBR) TSPO (18 kDa translocator protein) DAA1106 I-125 PK11195 Vinpocetine Human brain Whole hemisphere autoradiography Receptor binding
Megjelenés:	Neurochemistry International. - 54 : 1 (2009), p. 28-36. -
További szerzők:	Makkai Boglárka Kása Péter Gulya Károly Bakota Lidia Várszegi Szilvia Beliczai Zsuzsa Andersson, Jan Csiba László (1952-) (neurológus, pszichiáter) Thiele, Andrea Dyrks, Thomas Suhara, Tetsuya Suzuki, Kazutoshi Higuchi, Makato Halldin, Christer
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001-es BibID:	BIBFORM007320
Első szerző:	Gulyás Balázs
Cím:	In vitro evidence for competitive TSPO binding of the imaging biomarker cadidates vinpocetine and two iodinated DAA1106 analogues in post mortem autoradiography experiments on whole hemisphere human brain slices / Balázs Gulyás, Boglárka Makkai, Katalin Nagy, Ádám Vas, Péter Kása, Jan Andersson, Tetsuya Suhara, Kazutoshi Suzuki, Makato Higuchi, Zsuzsa Beliczai, Károly Gulya, László Csiba, Christer Halldin
Dátum:	2009
Tárgyszavak:	Orvostudományok Klinikai orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban peripheral benzodiazepine receptor (PBR) TSPO (18kDa translocator protein) vinpocetine DAA1106 human brain whole hemisphere autoradiography receptor binding radiopharmacon imaging biomarker
Megjelenés:	Current Radiopharmaceuticals. - 2 (2009), p. 42-48. -
További szerzők:	Makkai Boglárka Nagy Katalin (1960-) (orvosdiagnosztikai laboratóriumi analitikus) Vas Ádám Kása Péter Andersson, Jan Suhara, Tetsuya Suzuki, Kazutoshi Higuchi, Makato Beliczai Zsuzsa Gulya Károly Csiba László (1952-) (neurológus, pszichiáter) Halldin, Christer
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