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- W2000734358 abstract "On the basis of its established in vitro characteristics, [3H]RX 821002 was evaluated in rats as an in vivo radioligand for central α2-adrenoceptors. Estimates for in vivo binding potential, obtained by compartmental analyses of time-radioactivity data, ranged between 1.9 for hypothalamus and 0.2 for cerebellum, with a regional distribution in brain which was similar to that observed in vitro. Selectivity and specificity of the signal were checked by predosing with either the α2-antagonists, idazoxan or yohimbine, the α2-agonist, clonidine, or the α1-antagonist, prazosin. Pretreatment of the rats with the selective neurotoxin, DSP-4, had no significant effect on [3H]RX 821002 binding, suggesting that the majority of labelled sites were situated post-junctionally. The studies indicate that [3H]RX 821002 can be used experimentally as an in vivo marker for central α2-adrenoceptors. The size and rate of expression of the specific signal encourage the development and assessment of [11C]RX 821002 for clinical PET studies." @default.
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- W2000734358 date "1992-11-01" @default.
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- W2000734358 title "Quantification of in vivo binding of [3H]RX 821002 in rat brain: Evaluation as a radioligand for central α2-adrenoceptors" @default.
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- W2000734358 doi "https://doi.org/10.1016/0883-2897(92)90170-4" @default.
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