Hauptseite > Publikationsdatenbank > Autoradiographic comparison of in vitro binding characteristics of various tritiated adenosine A2A receptor ligands in rat, mouse and pig brain and first ex vivo results > print

001     1695
005     20180208225327.0
024 7 _ |2 pmid
|a pmid:19545560
024 7 _ |2 DOI
|a 10.1016/j.ejphar.2009.06.025
024 7 _ |2 WOS
|a WOS:000269933100017
037 _ _ |a PreJuSER-1695
041 _ _ |a eng
082 _ _ |a 610
084 _ _ |2 WoS
|a Pharmacology & Pharmacy
100 1 _ |a Sihver, W.
|b 0
|u FZJ
|0 P:(DE-Juel1)VDB17596
245 _ _ |a Autoradiographic comparison of in vitro binding characteristics of various tritiated adenosine A2A receptor ligands in rat, mouse and pig brain and first ex vivo results
260 _ _ |a Amsterdam
|b Elsevier
|c 2009
300 _ _ |a
336 7 _ |a Journal Article
|0 PUB:(DE-HGF)16
|2 PUB:(DE-HGF)
336 7 _ |a Output Types/Journal article
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336 7 _ |a Journal Article
|0 0
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336 7 _ |a ARTICLE
|2 BibTeX
336 7 _ |a JOURNAL_ARTICLE
|2 ORCID
336 7 _ |a article
|2 DRIVER
440 _ 0 |a European Journal of Pharmacology
|x 0926-6917
|0 21162
|y 1
|v 616
500 _ _ |a Record converted from VDB: 12.11.2012
520 _ _ |a The adenosine A(2A) receptor in the basal ganglia is involved in the control of movement and plays a role in movement disorders such as Parkinsonism. Developing ligands to evaluate that receptor by noninvasive methods such as positron emission tomography has a high priority. In vitro radioligand binding guides the selection of ligands for in vivo application. This study measured the binding of the adenosine A(2A) receptor antagonist [(3)H]MSX-2 (3-(3-hydroxypropyl)-8-m-methoxystyryl)-7-methyl-1-propargylxanthine) to rat, mouse and pig brain by autoradiography. Other studies measured binding to membranes from PC12 pheochromocytoma cells. Those binding parameters were compared to those of the adenosine A(2A) receptor antagonist [(3)H]ZM241385 (4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino)ethyl)phenol), the adenosine A(2A) receptor agonist [(3)H]CGS21680 (2-[p-(2-carboxyethyl)-phenethylamino]-5'-N-ethylcarboxamidoadenosine) and the unselective adenosine receptor agonist [(3)H]NECA (5'N-ethylcarboxamido)adenosine). The potency order (K(d)) in the three species was [(3)H]ZM241385<[(3)H]MSX-2<[(3)H]NECA<[(3)H]CGS21680. The density of [(3)H]MSX-2 binding sites was greater in the striatum than in the cortex. Preliminary ex vivo experiments showed that by 10min after iv injection, [(3)H]MSX-2 and [(3)H]CGS21680 crossed the blood-brain barrier to the extent of almost 1% ID/g brain tissue, but [(3)H]NECA and [(3)H]ZM241385 to only 0.2% ID/g. The prior administration of unlabeled ZM241385 significantly lowered brain uptake of [(3)H]MSX-2. In conclusion, [(3)H]MSX-2 has a high affinity and sufficient selectivity for the adenosine A(2A) receptor. It penetrates the blood-brain barrier. Sensitivity to photoisomerization is a limitation. Further investigations assess its suitability as a ligand for imaging the brain adenosine A(2A) receptor.
536 _ _ |a Funktion und Dysfunktion des Nervensystems
|c P33
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588 _ _ |a Dataset connected to Web of Science, Pubmed
650 _ 2 |2 MeSH
|a Adenosine A2 Receptor Agonists
650 _ 2 |2 MeSH
|a Animals
650 _ 2 |2 MeSH
|a Autoradiography
650 _ 2 |2 MeSH
|a Blood-Brain Barrier: metabolism
650 _ 2 |2 MeSH
|a Brain: metabolism
650 _ 2 |2 MeSH
|a Cell Membrane: metabolism
650 _ 2 |2 MeSH
|a Chromatography, High Pressure Liquid
650 _ 2 |2 MeSH
|a Female
650 _ 2 |2 MeSH
|a Ligands
650 _ 2 |2 MeSH
|a Mice
650 _ 2 |2 MeSH
|a PC12 Cells
650 _ 2 |2 MeSH
|a Protein Binding
650 _ 2 |2 MeSH
|a Rats
650 _ 2 |2 MeSH
|a Receptor, Adenosine A2A: metabolism
650 _ 2 |2 MeSH
|a Swine
650 _ 2 |2 MeSH
|a Tritium: chemistry
650 _ 2 |2 MeSH
|a Xanthines: chemistry
650 _ 2 |2 MeSH
|a Xanthines: metabolism
650 _ 7 |0 0
|2 NLM Chemicals
|a Adenosine A2 Receptor Agonists
650 _ 7 |0 0
|2 NLM Chemicals
|a Ligands
650 _ 7 |0 0
|2 NLM Chemicals
|a MSX 2 compound
650 _ 7 |0 0
|2 NLM Chemicals
|a Receptor, Adenosine A2A
650 _ 7 |0 0
|2 NLM Chemicals
|a Xanthines
650 _ 7 |0 10028-17-8
|2 NLM Chemicals
|a Tritium
650 _ 7 |a J
|2 WoSType
653 2 0 |2 Author
|a Adenosine A(2A) receptor
653 2 0 |2 Author
|a [H-3]ZM241385
653 2 0 |2 Author
|a [H-3]CGS21680
653 2 0 |2 Author
|a [H-3]MSX-2
653 2 0 |2 Author
|a [H-3]NECA
653 2 0 |2 Author
|a Brain imaging
700 1 _ |a Schulze, A.
|b 1
|u FZJ
|0 P:(DE-Juel1)VDB17597
700 1 _ |a Wutz, W.
|b 2
|u FZJ
|0 P:(DE-Juel1)VDB12398
700 1 _ |a Stüsgen, S.
|b 3
|u FZJ
|0 P:(DE-Juel1)VDB59407
700 1 _ |a Olsson, R. A.
|b 4
|0 P:(DE-HGF)0
700 1 _ |a Bier, D.
|b 5
|u FZJ
|0 P:(DE-Juel1)VDB2513
700 1 _ |a Holschbach, M. H.
|b 6
|u FZJ
|0 P:(DE-Juel1)VDB20516
773 _ _ |a 10.1016/j.ejphar.2009.06.025
|g Vol. 616
|q 616
|0 PERI:(DE-600)2143075-5
|t European journal of pharmacology / Environmental toxicology and pharmacology
|v 616
|y 2009
|x 0926-6917
856 7 _ |u http://dx.doi.org/10.1016/j.ejphar.2009.06.025
909 C O |o oai:juser.fz-juelich.de:1695
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913 1 _ |k P33
|v Funktion und Dysfunktion des Nervensystems
|l Funktion und Dysfunktion des Nervensystems
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914 1 _ |y 2009
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