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Titolo:
Synthesis of tropane and nortropane analogues with phenyl substitutions asserotonin transporter ligands
Autore:
Emond, P; Helfenbein, J; Chalon, S; Garreau, L; Vercouillie, J; Frangin, Y; Besnard, JC; Guilloteau, D;
Indirizzi:
Univ Tours, Lab Biophys Med & Pharmaceut, INSERM, U316, F-37200 Tours, France Univ Tours Tours France F-37200 eut, INSERM, U316, F-37200 Tours, France
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 7, volume: 9, anno: 2001,
pagine: 1849 - 1855
SICI:
0968-0896(200107)9:7<1849:SOTANA>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACID METHYL-ESTERS; NOR-BETA-CIT; HIGH-AFFINITY; DOPAMINE TRANSPORTER; ALZHEIMERS-DISEASE; IN-VITRO; BINDING; BRAIN; NOREPINEPHRINE; RADIOLIGAND;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
23
Recensione:
Indirizzi per estratti:
Indirizzo: Emond, P Univ Tours, Lab Biophys Med & Pharmaceut, INSERM, U316, 31 Ave Monge, F-37200 Tours, France Univ Tours 31 Ave Monge Tours France F-37200 37200 Tours, France
Citazione:
P. Emond et al., "Synthesis of tropane and nortropane analogues with phenyl substitutions asserotonin transporter ligands", BIO MED CH, 9(7), 2001, pp. 1849-1855

Abstract

The effects of structural modifications of 2 beta -carbomethoxy-3 beta -phenyl tropane analogues were evaluated on in vitro affinity to the dopamine (DAT) and serotonin (5-HTT) transporters in rat brain tissue. The introduction of a large alkyl group at the 4'-position of the phenyl ring, affording2 beta -carbomethoxy-3 beta-(4'-alkylphenyl) tropane, diminished the affinity for the DAT whereas moderate 5-HTT affinity was obtained. The introduction of an iodine at the 3'-position of the 4'-alkylphenyl. affording 2 beta-carbomethoxy-3 beta-(3'-iodo-4'-alkylphenyl) tropane, and N-demethylation, affording 2 beta -carbomethoxy-3 beta-(3'-iodo-4'-alkylphenyl) nortropane. improved affinity and specificity for the 5-HTT. It could be assumed fromthese results that the combination of these three modifications of tropanestructure yielded highly selective compounds for the 5-HTT. Of the new compounds synthesized, the most selective cocaine derivative, 2 beta -carbomethoxy-3 beta-(3'-iodo-4'-isopropylphenyl) nortropane (8d) labeled with iodine-123 or carbon-11, could be a potential ligand for exploration of the 5-HTtransporter by SPET or PET. (C) 2001 Published by Elsevier Science Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 04:52:43