The radiolabelling with the positron-emitter Carbon-11 and the biological evaluation in rats of 3-[2-[4-(2-[C-11]methoxyphenyl)piperazin-1 -yl]ethyl] pyrimido [5,4-b] indole-2,4-dione ([C-11]RN5), alpha(1)-adrenoceptor antagonist (K-i = 0.21 nM), as a putative radioligand for the noninvasive assessment of alpha(1)-adrenoceptors with positron emission tomography (PET) is reported. The radiosynthesis procedure consisted of O-methylation of des-methyl precursor with [C-11]methyl iodide in the presence of potassium hydroxide in dimethylformamide (DMF) at 80 degreesC. [C-11]RN5 was obtained in >99% radiochemical purity in 25 min with a radiochemical yield in the 20-30% range, end of synthesis (EOS) (non-decay corrected) and a specific radioactivity of 92.5 18.5 GBq/mumol. Pre-clinical studies in rats showed a high uptake of [C-11]RN5 in heart, spleen, adrenal gland. lung and kidney but not in the brain. Inhibition studies with high doses of different adrenergic antagonists indicate that more than 70% of myocardial uptake of [C-11]RN5 is due to specific binding to alpha(1)-adrenoceptors. Our results indicate that [C-11]RN5 is suitable to be further developed as a potential radioligand for the in vivo PET imaging of myocardial alpha(1)-adrenoceptors in humans. (C) 2002 Published by Elsevier Science B.V

Matarrese, M., Moresco, R., Romeo, G., Turolla, E., Simonelli, P., Todde, S., et al. (2002). [11C]RN5: A new agent for the in vivo imaging of myocardial α1-adrenoceptors. EUROPEAN JOURNAL OF PHARMACOLOGY, 453(2-3), 231-238 [10.1016/S0014-2999(02)02454-8].

[11C]RN5: A new agent for the in vivo imaging of myocardial α1-adrenoceptors

MORESCO, ROSA MARIA;SIMONELLI, PASQUALE;TODDE, SERGIO CAMILLO;MAGNI, FULVIO;KIENLE, MARZIA DONATELLA;FAZIO, FERRUCCIO
2002

Abstract

The radiolabelling with the positron-emitter Carbon-11 and the biological evaluation in rats of 3-[2-[4-(2-[C-11]methoxyphenyl)piperazin-1 -yl]ethyl] pyrimido [5,4-b] indole-2,4-dione ([C-11]RN5), alpha(1)-adrenoceptor antagonist (K-i = 0.21 nM), as a putative radioligand for the noninvasive assessment of alpha(1)-adrenoceptors with positron emission tomography (PET) is reported. The radiosynthesis procedure consisted of O-methylation of des-methyl precursor with [C-11]methyl iodide in the presence of potassium hydroxide in dimethylformamide (DMF) at 80 degreesC. [C-11]RN5 was obtained in >99% radiochemical purity in 25 min with a radiochemical yield in the 20-30% range, end of synthesis (EOS) (non-decay corrected) and a specific radioactivity of 92.5 18.5 GBq/mumol. Pre-clinical studies in rats showed a high uptake of [C-11]RN5 in heart, spleen, adrenal gland. lung and kidney but not in the brain. Inhibition studies with high doses of different adrenergic antagonists indicate that more than 70% of myocardial uptake of [C-11]RN5 is due to specific binding to alpha(1)-adrenoceptors. Our results indicate that [C-11]RN5 is suitable to be further developed as a potential radioligand for the in vivo PET imaging of myocardial alpha(1)-adrenoceptors in humans. (C) 2002 Published by Elsevier Science B.V
Articolo in rivista - Articolo scientifico
[C-11]RN5; alpha(1)-adrenoceptor antagonist; PET (positron emission tomography); biodistribution
English
2002
453
2-3
231
238
none
Matarrese, M., Moresco, R., Romeo, G., Turolla, E., Simonelli, P., Todde, S., et al. (2002). [11C]RN5: A new agent for the in vivo imaging of myocardial α1-adrenoceptors. EUROPEAN JOURNAL OF PHARMACOLOGY, 453(2-3), 231-238 [10.1016/S0014-2999(02)02454-8].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/13717
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