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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Binding of tritiated and radioiodinated ZM241,385 to brain A2A adenosine receptors.

Autoradiography on rat brain using tritiated (1*), mono- (2*) and di-radioiodinated (3*) derivatives of the A(2A) adenosine receptor antagonist ZM241,385 showed high receptor density in striatum. K(D)s of 1*, 2* and 3* were 0.4, 2.2 and 15 nM and nonspecific binding was 5, 40 and 50% of total binding. Striatal uptake of 2* in mice was approximately 0.2% ID/g 60 min post-injection; blocking by 2 was insignificant. Poor penetration of the blood brain barrier and high nonspecific binding make 2* unsuitable for imaging striatal receptors.[1]

References

  1. Binding of tritiated and radioiodinated ZM241,385 to brain A2A adenosine receptors. Sihver, W., Bier, D., Holschbach, M.H., Schulze, A., Wutz, W., Olsson, R.A., Coenen, H.H. Nucl. Med. Biol. (2004) [Pubmed]
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