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Hume SP, Lammertsma AA, Opacka-Juffry J, et al. Quantification of in vivo binding of [3H]RX 821002 in rat brain: evaluation as a radioligand for central alpha 2-adrenoceptors. Int J Rad Appl Instrum B. 1992;19(8):841-9doi: 10.1016/0883-2897(92)90170-4.
Hume, S. P., Lammertsma, A. A., Opacka-Juffry, J., Ahier, R. G., Myers, R., Cremer, J. E., Hudson, A. L., Nutt, D. J., & Pike, V. W. (1992). Quantification of in vivo binding of [3H]RX 821002 in rat brain: evaluation as a radioligand for central alpha 2-adrenoceptors. International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology, 19(8), 841-9. https://doi.org/10.1016/0883-2897(92)90170-4
Hume, S P, et al. "Quantification of in vivo binding of [3H]RX 821002 in rat brain: evaluation as a radioligand for central alpha 2-adrenoceptors." International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology vol. 19,8 (1992): 841-9. doi: https://doi.org/10.1016/0883-2897(92)90170-4
Hume SP, Lammertsma AA, Opacka-Juffry J, Ahier RG, Myers R, Cremer JE, Hudson AL, Nutt DJ, Pike VW. Quantification of in vivo binding of [3H]RX 821002 in rat brain: evaluation as a radioligand for central alpha 2-adrenoceptors. Int J Rad Appl Instrum B. 1992 Nov;19(8):841-9. doi: 10.1016/0883-2897(92)90170-4. PMID: 1358860.
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Int J Rad Appl Instrum B. 1992 Nov;19(8):841-9. doi: 10.1016/0883-2897(92)90170-4.

Quantification of in vivo binding of [3H]RX 821002 in rat brain: evaluation as a radioligand for central alpha 2-adrenoceptors.

International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology

S P Hume, A A Lammertsma, J Opacka-Juffry, R G Ahier, R Myers, J E Cremer, A L Hudson, D J Nutt, V W Pike

Affiliations

  1. MRC Cyclotron Unit, Hammersmith Hospital, London, England.

PMID: 1358860 DOI: 10.1016/0883-2897(92)90170-4

Abstract

On the basis of its established in vitro characteristics, [3H]RX 821002 was evaluated in rats as an in vivo radioligand for central alpha 2-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 alpha 2-antagonists, idazoxan or yohimbine, the alpha 2-agonist, clonidine, or the alpha 1-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 alpha 2-adrenoceptors. The size and rate of expression of the specific signal encourage the development and assessment of [11C]RX 821002 for clinical PET studies.

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