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11C-Radiosynthesis and preliminary human evaluation of the disposition of the ACE inhibitor [11C]zofenoprilat (Articolo in rivista)

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11C-Radiosynthesis and preliminary human evaluation of the disposition of the ACE inhibitor [11C]zofenoprilat (Articolo in rivista) (literal)

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Alternative label

Matarrese M. 1, Salimbeni A. 2, Turolla E.A. 1, Turozzi D. 2, Moresco R.M. 1, Poma D. 2, Magni F. 3, Todde S. 1, Rossetti C. 1, Sciarrone M.T. 1, Bianchi G. 1, Kienle M.G. 3, Fazio F. 1 (2004)
11C-Radiosynthesis and preliminary human evaluation of the disposition of the ACE inhibitor [11C]zofenoprilat
in Bioorganic & medicinal chemistry (Print)
(literal)

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Matarrese M. 1, Salimbeni A. 2, Turolla E.A. 1, Turozzi D. 2, Moresco R.M. 1, Poma D. 2, Magni F. 3, Todde S. 1, Rossetti C. 1, Sciarrone M.T. 1, Bianchi G. 1, Kienle M.G. 3, Fazio F. 1 (literal)

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Sintesi e marcatura con Carbonio-11 e valutazione preliminare nelluomo del sodio zofenoprilato, ACE inibitore, per lo studio delle patologie cardiovascolari. (literal)

Note

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1. Institute of Molecular Bioimaging and Physiology-CNR; University of Milano/Bicocca, Institute San Raffaele, Milan, Italy 2. R&D Department, Lusochimica S.p.A., Lomagna (Lecco), Italy 3. University of Milano-Bicocca, DIMESAB, Monza (MI), Italy (literal)

Titolo

11C-Radiosynthesis and preliminary human evaluation of the disposition of the ACE inhibitor [11C]zofenoprilat (literal)

Abstract

(4S)-1-[(S)-3-Mercapto-2-methylpropanoyl]-4-phenylthio-L-proline (Zofenoprilat, 2), the active metabolite of the potent ACE inhibitor Zofenopril Calcium (1), was labelled with carbon-11 (t1/2=20.4 min) to evaluate its pharmacokinetics behaviour in human body using Positron Emission Tomography (PET). [11C]2 labelling procedures were based on the use of immobilized Grignard reagent and the acylation of (S)-4-phenylthio-L-proline methyl ester (5) with 11C-labelled methacryloyl chloride, followed by a Michael addition with thiobenzoic acid. The radiochemical yield was 5-10% (EOB, decay corrected) and specific radioactivity ranged from 0.5 to 1.5 Ci/micromol (18.5-55.5 GBq/micromol). Preliminary in vivo human evaluation of [11C]2 showed that the drug accumulates in organs which express high levels of ACE, like lungs and kidneys, and in organs involved in drug metabolism such as the liver and gall bladder. Results of the distribution of [11C]2 showed a measurable concentration of the drug in the target tissues such as the kidney and to a minor extent, the heart, where it can afford organ protection. (literal)

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