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Titolo:
Synthesis and preliminary biological characterization of a new potential I-125-radioligand for dopamine and serotonin receptors
Autore:
Guarna, A; Menchi, G; Berti, G; Cini, N; Bottoncetti, A; Raspanti, S; Politi, A; Pupi, A;
Indirizzi:
Univ Florence, Dipartimento Chim Organ U Schiff, CNR, I-50121 Florence, Italy Univ Florence Florence Italy I-50121 chiff, CNR, I-50121 Florence, Italy Univ Florence, Ctr Studio Chim & Struttura Composti Eterociclici, CNR, I-50121 Florence, Italy Univ Florence Florence Italy I-50121 clici, CNR, I-50121 Florence, Italy Univ Florence, Dipartimento Fisiopatol Clin, Nucl Med Unit, I-50134 Florence, Italy Univ Florence Florence Italy I-50134 l Med Unit, I-50134 Florence, Italy
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 12, volume: 9, anno: 2001,
pagine: 3197 - 3206
SICI:
0968-0896(200112)9:12<3197:SAPBCO>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
CEREBRAL BLOOD-FLOW; RAT-BRAIN REGIONS; BINDING; RISPERIDONE; EXTRACTION; TOMOGRAPHY; LIGAND; SPECT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
32
Recensione:
Indirizzi per estratti:
Indirizzo: Guarna, A Univ Florence, Dipartimento Chim Organ U Schiff, CNR, Via G Capponi 9, I-50121 Florence, Italy Univ Florence Via G Capponi 9 Florence Italy I-50121 nce, Italy
Citazione:
A. Guarna et al., "Synthesis and preliminary biological characterization of a new potential I-125-radioligand for dopamine and serotonin receptors", BIO MED CH, 9(12), 2001, pp. 3197-3206

Abstract

The synthesis and a preliminary biological characterization of a new classof N-benzyl-aminoalcohols which have serotonin (5-HT2) and dopamine (D-2) receptor affinity is described. In vitro competition binding studies were conducted with the new molecules and H-3-spiperone on crude membrane preparation from rat striatum and frontal cortex. One of these compounds. 3-benzylamino-1-(4-fluoro-2-iodophenyl)-propan-1-ol (6f), whose IC50 values are in the micromolar range for both the D-2 and 5-HT2 receptors. was prepared in iodine-125 labelled form (6i) by nucleophilic substitution of the bromine atom of 3-benzylamino-1-(2-bromo-4-fluorophenvl)-propan-1-ol (6d). In the invivo studies. conducted on rats, the radiolabelled molecule 6i shows a good capacity to cross the blood-brain barrier (BBB) with a mean value of first pas., cerebral extraction (E) of ca. 50% when the regional cerebral bloodflow. measured with microsphere technique, is in the experimental animal'sphysiologic range (0.8-1 mL/min/g). A preliminary in vitro autoradiographic distribution on coronal rat brain slices of the radioiodinated molecule showed that it was preferentially localized in the striatum and in the cerebral regions rich in dopamine- and serotonin receptors, even if a high nonspecific binding was observed. (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 17/09/19 alle ore 23:14:44