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Titolo:
PHARMACOLOGICAL IN-VITRO CHARACTERIZATION OF THE ARECOLINE BIOISOSTERE, LU 25-109-T, A MUSCARINIC COMPOUND WITH M-1-AGONISTIC AND M-2 M-3-ANTAGONISTIC PROPERTIES/
Autore:
MEIER E; FREDERIKSEN K; NIELSEN M; LEMBOL HL; PEDERSEN H; HYTTEL J;
Indirizzi:
H LUNDBECK & CO AS,MED RES,DEPT PHARMACOL SCREENING,OTTILIAVEJ 9 DK-2500 COPENHAGEN DENMARK H LUNDBECK & CO AS,RES DEPT COPENHAGEN DENMARK ST HANS PSYCHIAT HOSP ROSKILDE DENMARK
Titolo Testata:
Drug development research
fascicolo: 1, volume: 40, anno: 1997,
pagine: 1 - 16
SICI:
0272-4391(1997)40:1<1:PICOTA>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
SUPERIOR CERVICAL-GANGLION; CEREBELLAR GRANULE CELLS; ALZHEIMERS-DISEASE; NUCLEUS BASALIS; RAT-BRAIN; ACETYLCHOLINE-RECEPTORS; NEUROCHEMICAL PROFILE; PERIPHERAL-TISSUES; CORPUS STRIATUM; BINDING-SITES;
Keywords:
ARECOLINE BIOISOSTERE; MUSCARINIC RECEPTOR SUBTYPES; LU 25-109-T; XANOMELINE; R586; ALZHEIMERS DISEASE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
85
Recensione:
Indirizzi per estratti:
Citazione:
E. Meier et al., "PHARMACOLOGICAL IN-VITRO CHARACTERIZATION OF THE ARECOLINE BIOISOSTERE, LU 25-109-T, A MUSCARINIC COMPOUND WITH M-1-AGONISTIC AND M-2 M-3-ANTAGONISTIC PROPERTIES/", Drug development research, 40(1), 1997, pp. 1-16

Abstract

The arecoline bioisostere, Lu 25-109-T, displays a pharmacological profile of a partial muscarinic agonist with a several-fold higher affinity for cortical M-1 receptors than for brain stem M-2 receptors and salivary glands M-2 receptors. The compound is selective for muscarinicreceptors as it shows no or only low affinity for other receptor types. In functional assays Lu 25-109-T behaves as a partial agonist at the guinea pig ileum (M-1/M-2/M-3), at the rat superior cervical ganglion (M-1) and at cells transfected with cloned human mi muscarinic receptors and as an antagonist at guinea pig left atrium (M-2) and culturedcerebellar granule cells (M-3) Lu 25-109-T readily passes the blood-brain barrier in mice and has a bioavailability of 42% at oral administration although with a short half-life (t(1/2) = 41 min). The results indicate that Lu 25-109-T is acting selectively on muscarinic receptors. In functional in vitro assays Lu 25-109-T acts as an M-1 (and m1) partial agonist and at the same time as an M-2 and M-3 antagonist. (C) 1997 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/06/20 alle ore 23:45:10