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Titolo:
IMPORTANCE OF H5-HT1B RECEPTOR SELECTIVITY FOR 5-HT TERMINAL AUTORECEPTOR ACTIVITY - AN IN-VIVO MICRODIALYSIS STUDY IN THE FREELY-MOVING GUINEA-PIG
Autore:
ROBERTS C; PRICE GW; GASTER L; JONES BJ; MIDDLEMISS DN; ROUTLEDGE C;
Indirizzi:
SMITHKLINE BEECHAM PHARMACEUT,DEPT PSYCHIAT RES,NEW FRONTIERS SCI PK N,3RD AVE HARLOW CM19 5AW ESSEX ENGLAND SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM HARLOW CM19 5AW ESSEX ENGLAND
Titolo Testata:
Neuropharmacology
fascicolo: 4-5, volume: 36, anno: 1997,
pagine: 549 - 557
SICI:
0028-3908(1997)36:4-5<549:IOHRSF>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
DORSAL RAPHE NUCLEUS; PHARMACOLOGICAL CHARACTERIZATION; FRONTAL-CORTEX; BRAIN CORTEX; RELEASE; RAT; INHIBITION; MEMBRANES; GR127935; AGONIST;
Keywords:
GUINEA-PIG; 5-HT; MICRODIALYSIS; 5-HT1B/1D RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
33
Recensione:
Indirizzi per estratti:
Citazione:
C. Roberts et al., "IMPORTANCE OF H5-HT1B RECEPTOR SELECTIVITY FOR 5-HT TERMINAL AUTORECEPTOR ACTIVITY - AN IN-VIVO MICRODIALYSIS STUDY IN THE FREELY-MOVING GUINEA-PIG", Neuropharmacology, 36(4-5), 1997, pp. 549-557

Abstract

The importance of h5-HT1B receptor selectivity for 5-HT terminal autoreceptor activity was investigated with the selective h5-HT1B receptorligands SE 219085, SE 220272; SE 224289 and SE 216641. The studies employed measurement of compound affinity and efficacy in vitro and the measurement of extracellular 5-HT in the frontal cortex of the freely-moving guinea-pig using in vivo microdialysis. All compounds had high affinity and selectivity for the h5-HT1B receptor, with SE 224289 the most selective for h5-HT1B over h5-HT1D receptors. Compounds exhibiteda range of efficacies at both receptors: SE 224289 and SE 219085 wereinverse agonists, SE 220272 was an antagonist and SE 216641 was a partial agonist. SE 220272, SE 216641 and SE 224289 had no effect on extracellular 5-HT following systemic administration, however, SE 219085 produced a significant increase. The SE 219085-induced increase in extracellular 5-HT was attributed to the compounds non-specific releasing properties as it was also demonstrated to increase basal release of [H-3]5-HT from pre-loaded guinea-pig cortical slices. The lack of effectof the above h5-HT1B receptor selective compounds and the decrease inextracellular 5-HT elicited by the non-selective compounds GR 127935,GR125743 and methiothepin suggest that antagonism of 5-HT1D receptorsmay mediate this decrease in 5-HT levels. It is plausible that blockade of 5-HT1D receptors increases 5-HT levels in the raphe, this activates 5-HT1A receptors which results in an overall decrease in terminal 5-HT release. Definitive proof now awaits elucidation of the action ofa selective 5-HT1D receptor antagonist. (C) 1997 Elsevier Science Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/07/20 alle ore 07:19:29