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000824539 1001_ $$0P:(DE-Juel1)144437$$aKreft, Sabrina$$b0
000824539 245__ $$aNew potent A1 adenosine receptor radioligands for positron emission tomography
000824539 260__ $$aAmsterdam [u.a.]$$bElsevier Science$$c2017
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000824539 520__ $$a8-Cyclopentyl-3-(3-[18F]fluoropropyl)-1-propylxanthine ([18F]CPFPX) is meanwhile an accepted receptor ligand to examine the A1 adenosine receptor (A1AR) in humans by positron emission tomography (PET). A major drawback of this compound is its rather fast metabolic degradation in vivo.Therefore two new xanthine derivatives, namely 8-cyclobutyl-1-cyclopropymethyl-3-(3-fluoropropyl)xanthine (CBCPM; 5) and 1-cyclopropylmethyl-3-(3-fluoropropyl)-8-(1-methylcyclobutyl)xanthine (CPMMCB; 6) were designed and synthesized as potential alternatives to CPFPX. In membrane binding studies both compounds showed nanomolar affinity for the A1AR. In vitro autoradiographic studies of [18F]5 and [18F]6, using rat brain slices, showed the expected accumulation in regions known to have a high adenosine A1 receptor expression while exhibiting the necessary low unspecific binding. However, in vitro metabolite studies using human liver microsomes revealed a comparable metabolic degradation rate for both new xanthine derivatives and CPFPX.
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000824539 7001_ $$0P:(DE-Juel1)131810$$aBier, Dirk$$b1$$eCorresponding author
000824539 7001_ $$0P:(DE-Juel1)131824$$aHolschbach, Marcus$$b2
000824539 7001_ $$0P:(DE-Juel1)131847$$aSchulze, Annette$$b3
000824539 7001_ $$0P:(DE-Juel1)131816$$aCoenen, Heinrich Hubert$$b4
000824539 773__ $$0PERI:(DE-600)1498538-x$$a10.1016/j.nucmedbio.2016.09.004$$gVol. 44, p. 69 - 77$$p69 - 77$$tNuclear medicine and biology$$v44$$x0969-8051$$y2017
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