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Titolo:
Selective delta-opioid receptor ligands: Potential PET ligands based on naltrindole
Autore:
Clayson, J; Jales, A; Tyacke, RJ; Hudson, AL; Nutt, DJ; Lewis, JW; Husbands, SM;
Indirizzi:
Univ Bath, Dept Pharm & Pharmacol, Bath BA2 7AY, Avon, England Univ Bath Bath Avon England BA2 7AY harmacol, Bath BA2 7AY, Avon, England Univ Bristol, Sch Chem, Bristol, Avon, England Univ Bristol Bristol Avon England stol, Sch Chem, Bristol, Avon, England Univ Bristol, Dept Psychopharmacol, Bristol, Avon, England Univ Bristol Bristol Avon England sychopharmacol, Bristol, Avon, England
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 7, volume: 11, anno: 2001,
pagine: 939 - 943
SICI:
0960-894X(20010409)11:7<939:SDRLPP>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
EFFICIENT SYNTHESIS; ANTAGONISTS; RADIOLIGAND; BINDING; N1'-(METHYL)NALTRINDOLE; SERIES; BRAIN; MICE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
20
Recensione:
Indirizzi per estratti:
Indirizzo: Husbands, SM Univ Bath, Dept Pharm & Pharmacol, Bath BA2 7AY, Avon, England Univ Bath Bath Avon England BA2 7AY h BA2 7AY, Avon, England
Citazione:
J. Clayson et al., "Selective delta-opioid receptor ligands: Potential PET ligands based on naltrindole", BIOORG MED, 11(7), 2001, pp. 939-943

Abstract

Two series of delta -selective ligands related to the prototypic delta -antagonist naltrindole have been prepared and evaluated in opioid binding assays with the aim of developing new PET ligands for the delta -opioid receptor. One compound (5d) had significantly here selectivity than naltrindole, but with substantially reduced binding affinity. For those compounds retaining similar affinity to naltrindole. those having ethyl and fluoroethyl substituents afforded the highest levels of selectivity. However, none of the compounds combined the high level of affinity and selectivity ideally suited to the development of an imaging agent. (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 06/04/20 alle ore 02:01:40