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

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العنوان:	11C-Radiosynthesis and preliminary human evaluation of the disposition of the ACE inhibitor [11C]zofenoprilat
المؤلفون:	Marzia Galli Kienle, Ferruccio Fazio, Turozzi Damiano, Giuseppe Bianchi, Sergio Todde, E. Turolla, Fulvio Magni, Davide Poma, Claudio Rossetti, Aldo Salimbeni, Mario Matarrese, Rosa Maria Moresco, Maria Teresa Sciarrone
المساهمون:	Matarrese, M, Salimbeni, A, Turolla, E, Turozzi, D, Moresco, R, Poma, D, Magni, F, Todde, S, Rossetti, C, Sciarrone, M, Bianchi, G, Kienle, M, Fazio, F
المصدر:	Bioorganic & medicinal chemistry 12 (2004): 603–611. doi:10.1016/j.bmc.2003.10.054 info:cnr-pdr/source/autori: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/titolo:11C-Radiosynthesis and preliminary human evaluation of the disposition of the ACE inhibitor [11C]zofenoprilat/doi:10.1016%2Fj.bmc.2003.10.054/rivista:Bioorganic & medicinal chemistry (Print)/anno:2004/pagina_da:603/pagina_a:611/intervallo_pagine:603–611/volume:12
بيانات النشر:	Elsevier BV, 2004.
سنة النشر:	2004
مصطلحات موضوعية:	Male, Captopril, Clinical Biochemistry, Pharmaceutical Science, Angiotensin-Converting Enzyme Inhibitors, Pharmacology, Zofenopril Calcium, Zofenoprilato, Biochemistry, chemistry.chemical_compound, Pharmacokinetics, In vivo, Pharmachokinetic, PET, Zofenopril, ACE inhibitor, Drug Discovery, Humans, Tissue Distribution, Carbon Radioisotopes, Molecular Biology, Active metabolite, Molecular Structure, biology, Organic Chemistry, Radiosynthesis, Middle Aged, Zofenopril, PET, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, C-11 radiofarmaci, ACE inibitore, Drug metabolism, Tomography, Emission-Computed
الوصف:	(4 S )-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 ( t 1/2 =20.4 min) to evaluate its pharmacokinetics behaviour in human body using Positron Emission Tomography (PET). [ 11 C]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 11 C-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/μmol (18.5–55.5 GBq/μmol). Preliminary in vivo human evaluation of [ 11 C] 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 [ 11 C] 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.
تدمد:	0968-0896
الوصول الحر:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62fd8d9d2e891094efaa0990383a82ceTest https://doi.org/10.1016/j.bmc.2003.10.054Test
حقوق:	CLOSED
رقم الانضمام:	edsair.doi.dedup.....62fd8d9d2e891094efaa0990383a82ce
قاعدة البيانات:	OpenAIRE

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