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Titolo:
Synthesis and characterization of fluorinated and iodinated pyrrolopyrimidines as PET/SPECT ligands for the CRF1 receptor
Autore:
Martarello, L; Kilts, CD; Ely, T; Owens, MJ; Nemeroff, CB; Camp, M; Goodman, MM;
Indirizzi:
Emory Univ, Sch Med, Emory Ctr Positron Emiss Tomog, Dept Radiol, Atlanta,GA 30322 USA Emory Univ Atlanta GA USA 30322 Tomog, Dept Radiol, Atlanta,GA 30322 USA Emory Univ, Sch Med, Emory Ctr Positron Emiss Tomog, Dept Psychiat & BehavSci, Atlanta, GA 30322 USA Emory Univ Atlanta GA USA 30322 sychiat & BehavSci, Atlanta, GA 30322 USA
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 2, volume: 28, anno: 2001,
pagine: 187 - 195
SICI:
0969-8051(200102)28:2<187:SACOFA>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
CORTICOTROPIN-RELEASING FACTOR; DEPRESSION; STRESS; ANTAGONIST; DISORDERS; ANXIETY;
Keywords:
CRF receptor; fluorine-18; iodine-123; radiolabeling;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Martarello, L Emory Univ, Sch Med, Emory Ctr Positron Emiss Tomog, Dept Radiol, 1634 Clifton Rd NE, Atlanta, GA 30322 USA Emory Univ 1634 Clifton Rd NE Atlanta GA USA 30322 30322 USA
Citazione:
L. Martarello et al., "Synthesis and characterization of fluorinated and iodinated pyrrolopyrimidines as PET/SPECT ligands for the CRF1 receptor", NUCL MED BI, 28(2), 2001, pp. 187-195

Abstract

Fluorine-18 labeled fluorobutyl[2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo [2,3-d] pyrimidin-4-yl]ethylamine (FBPPA) and iodine-123 labeled butyl[2,5-dimethyl-7-(4-iodo-2,6-dimethylphenyl)-7H-pyrrolo[2, 3-d] pyrimidin-4-yl]ethyl-amine (IBPPA) were synthesized in the development of a CRF receptor ligand. The methods of synthesis, in vitro binding assays, radiolabeling and in vivo tissue distribution in rats are described. Fluorine-18 labeled FBPPA was prepared with high specific activity (3 x 10(4) Ci/mmol) by nucleophilic displacement with an average radiochemical yield of 6% (EOB). Iodine-123 labeled IBPPA was prepared by electrophilic iododestannylation with good yield (60%) and high specific activity (3.3 x 10(3) Ci/mmol). The retention of FBPPA and IBPPA in the pituitary was good (1.16% i.d./g and 2.35% i.d./g respectively at 60 min). However, the accumulation of radioactivity in the brain for both radiotracers was very low at all time points of thestudy, which demonstrated the difficulties for these radiopharmaceuticals to penetrate the blood brain barrier (BBB). (C) 2001 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 11:03:14