Catalogo Articoli (Spogli Riviste)

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Titolo:
Lead generation and lead optimisation approaches in the discovery of selective, non-peptide ORL-1 receptor agonists and antagonists
Autore:
Ronzoni, S; Peretto, L; Giardina, GAM;
Indirizzi:
SmithKline Beecham SPA, Dept Med Chem, I-20021 Baranzate Milano, Italy SmithKline Beecham SPA Baranzate Milano Italy I-20021 zate Milano, Italy
Titolo Testata:
EXPERT OPINION ON THERAPEUTIC PATENTS
fascicolo: 4, volume: 11, anno: 2001,
pagine: 525 - 546
SICI:
1354-3776(200104)11:4<525:LGALOA>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
NEUROPEPTIDE ORPHANIN FQ; HAMSTER OVARY CELLS; NEURONS IN-VITRO; OPIOID RECEPTOR; NOCICEPTIN/ORPHANIN FQ; DYNORPHIN-A; PHARMACOLOGICAL CHARACTERIZATION; NALOXONE BENZOYLHYDRAZONE; FQ/NOCICEPTIN RECEPTOR; ENDOGENOUS LIGAND;
Keywords:
anxiety; arylpiperidines; benzimidazopiperidines; cough; diaminoquinolines; morphinan hydroxamic acids; nociceptin; N/OFQ; opioid receptor like-1; orphanin FQ; pain; spiropiperidines;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
84
Recensione:
Indirizzi per estratti:
Indirizzo: Giardina, GAM SmithKline Beecham SPA, Dept Med Chem, Via Zambeletti, I-20021 Baranzate Milano, Italy SmithKline Beecham SPA Via Zambeletti Baranzate Milano Italy I-20021
Citazione:
S. Ronzoni et al., "Lead generation and lead optimisation approaches in the discovery of selective, non-peptide ORL-1 receptor agonists and antagonists", EXPERT OP T, 11(4), 2001, pp. 525-546

Abstract

The discovery of the opioid receptor like-1 (ORL-1) receptor and of its endogenous agonist nociceptin/orphanin FQ has attracted great interest in thescientific community giving rise, in the last five years, to a flurry of biological studies aimed at elucidating the role of this new receptor. Hence, the involvement of the ORL-1 receptor in many important processes, such as antinociception, learning and memory, feeding and anxiety, has been well documented. However, a clear understanding of the potential therapeutic value associated with the modulation of the ORL-1 receptor needs the development of selective non-peptide agonists and antagonists allowing systemic routes of administration. This review addresses the advances made by several research groups in the discovery of such compounds and discusses the medicinal chemistry strategies which, starting from the first non-selective ligandsNalBzoH and lofentanil, led to the disclosure of highly potent and selective agonists and antagonists, such as Ro 64-6198, J-113397 and JTC-801. Efforts have also focussed on the pharmacological characterisation of the newlydiscovered non-peptide tools, which represent a significant step forward in the understanding of the involvement of the ORL-1 receptor in a number ofpossible pathophysiological conditions.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/05/20 alle ore 02:19:53