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Titolo:
DIFFERENTIAL-EFFECTS OF 5-HT1B (1D) RECEPTOR ANTAGONISTS IN DORSAL AND MEDIAN RAPHE INNERVATED BRAIN-REGIONS/
Autore:
ROBERTS C; BELENGUER A; MIDDLEMISS DN; ROUTLEDGE C;
Indirizzi:
SMITHKLINE BEECHAM PHARMACEUT,DEPT NEUROSCI,NEW FRONTIERS SCI PK,3RD AVE HARLOW CM19 5AW ESSEX ENGLAND SMITHKLINE BEECHAM PHARMACEUT,DEPT SEPARAT SCI HARLOW CM19 5AW ESSEX ENGLAND
Titolo Testata:
European journal of pharmacology
fascicolo: 2-3, volume: 346, anno: 1998,
pagine: 175 - 180
SICI:
0014-2999(1998)346:2-3<175:DO5(RA>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; 5-HT RELEASE; FRONTAL-CORTEX; HUMAN 5-HT1D-ALPHA; CEREBRAL-CORTEX; RAT DORSAL; AUTORECEPTORS; MICRODIALYSIS; GR127935; NUCLEUS;
Keywords:
MICRODIALYSIS; (GUINEA PIG); 5-HT1B/(1D) RECEPTOR ANTAGONIST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
39
Recensione:
Indirizzi per estratti:
Citazione:
C. Roberts et al., "DIFFERENTIAL-EFFECTS OF 5-HT1B (1D) RECEPTOR ANTAGONISTS IN DORSAL AND MEDIAN RAPHE INNERVATED BRAIN-REGIONS/", European journal of pharmacology, 346(2-3), 1998, pp. 175-180

Abstract

The effect of SE-224289 ]carbonyl}Furo[2,3-F]-indole-3-spiro-4'-piperidine oxalate) (4 mg/kg i.p., 5-HT1B receptor antagonist), GR 127935 thyl-1-piperizinyl)phenyl]-2'-methyl-4'-(5-methyl- 1,2,4-oxadiazole-3-yl)[1,1'-biphenyl]-carboxamide) (0.3 mg/kg i.p., 5-HT1B/(1D) receptor antagonist), and paroxetine(10 mg/kg p.o.) were investigated on extracellular 5-hydroxytryptamine (5-MT) levels in the frontal cortex, striatum and dentate gyrus of the freely moving guinea-pig with microdialysis. In the frontal cortex and striatum (dorsal raphe innervated areas),GR 127935 evoked a significant decrease in extracellular 5-HT, reaching minima of 41 +/- 12% and 32 +/- 6% of basal, respectively. This decrease may be explained by antagonism of inhibitory 5-HT1B/1D receptorson raphe cell bodies, leading to a local increase in 5-HT, which, in turn, stimulated 5-HT1A receptors to decrease cell firing, and hence 5-HT release from terminals. In contrast, 3B-224289 had no effect on 5-HT levels in either region. In the dentate gyrus (median raphe innervated area), GR 127935 and 3B-224289 significantly increased extracellular 5-HT, reaching maxima of 146 +/- 11% and 151 +/- 19% of basal, respectively. The ability of both compounds to increase 5-HT levels in thedentate gyrus suggests a lack of 5-HT(1B/1D)5-HT1B/1D receptors in the median raphe nucleus. Paroxetine produced a small but non-significant increase in extracellular 5-HT in the frontal cortex, and a small decrease in the dentate gyrus. The lack of effect of paroxetine in terminal areas may be due to the limiting effects of cell body 5-HT autoreceptors. In summary, the above data demonstrate that 5-HT1B/1D receptorantagonists increase 5-HT levels in the dentate gyrus, implying that acute administration of 5-HT1B/1D receptor antagonists will achieve a similar effect to chronic selective serotonin re-uptake inhibitor treatment administration of 5-HT in median raphe innervated areas. This, in turn, suggests that such compounds may be efficacious in the treatment of depression. (C) 1998 Elsevier Science B.V.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 00:24:00