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@ARTICLE{Sihver:1695,
      author       = {Sihver, W. and Schulze, A. and Wutz, W. and Stüsgen, S.
                      and Olsson, R. A. and Bier, D. and Holschbach, M. H.},
      title        = {{A}utoradiographic comparison of in vitro binding
                      characteristics of various tritiated adenosine {A}2{A}
                      receptor ligands in rat, mouse and pig brain and first ex
                      vivo results},
      journal      = {European journal of pharmacology / Environmental toxicology
                      and pharmacology},
      volume       = {616},
      issn         = {0926-6917},
      address      = {Amsterdam},
      publisher    = {Elsevier},
      reportid     = {PreJuSER-1695},
      year         = {2009},
      note         = {Record converted from VDB: 12.11.2012},
      abstract     = {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.},
      keywords     = {Adenosine A2 Receptor Agonists / Animals / Autoradiography
                      / Blood-Brain Barrier: metabolism / Brain: metabolism / Cell
                      Membrane: metabolism / Chromatography, High Pressure Liquid
                      / Female / Ligands / Mice / PC12 Cells / Protein Binding /
                      Rats / Receptor, Adenosine A2A: metabolism / Swine /
                      Tritium: chemistry / Xanthines: chemistry / Xanthines:
                      metabolism / Adenosine A2 Receptor Agonists (NLM Chemicals)
                      / Ligands (NLM Chemicals) / MSX 2 compound (NLM Chemicals) /
                      Receptor, Adenosine A2A (NLM Chemicals) / Xanthines (NLM
                      Chemicals) / Tritium (NLM Chemicals) / J (WoSType)},
      cin          = {INB-4},
      ddc          = {610},
      cid          = {I:(DE-Juel1)VDB807},
      pnm          = {Funktion und Dysfunktion des Nervensystems},
      pid          = {G:(DE-Juel1)FUEK409},
      shelfmark    = {Pharmacology $\&$ Pharmacy},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:19545560},
      UT           = {WOS:000269933100017},
      doi          = {10.1016/j.ejphar.2009.06.025},
      url          = {https://juser.fz-juelich.de/record/1695},
}