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Titolo:
IN-VITRO AND IN-VIVO ACTIVITY OF 1-(1-NAPHTHYL)PIPERAZINE AT TERMINAL5-HT AUTORECEPTORS IN GUINEA-PIG BRAIN
Autore:
MORET C; BRILEY M;
Indirizzi:
CTR RECH PIERRE FABRE,17 AVE JEAN MOULIN F-81100 CASTRES FRANCE
Titolo Testata:
Naunyn-Schmiedeberg's archives of pharmacology
fascicolo: 4, volume: 351, anno: 1995,
pagine: 377 - 384
SICI:
0028-1298(1995)351:4<377:IAIAO1>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN CEREBRAL-CORTEX; FREELY-MOVING RATS; 5-HYDROXYTRYPTAMINE RELEASE; INVIVO MICRODIALYSIS; MEDIATING INHIBITION; SEROTONIN RECEPTORS; SPECIES-DIFFERENCES; FRONTAL-CORTEX; HYPOTHALAMUS; DIALYSIS;
Keywords:
1-(1-NAPHTHYL)PIPERAZINE; 5-HT RELEASE; TERMINAL 5-HT AUTORECEPTOR MICRODIALYSIS; GUINEA PIGS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
40
Recensione:
Indirizzi per estratti:
Citazione:
C. Moret e M. Briley, "IN-VITRO AND IN-VIVO ACTIVITY OF 1-(1-NAPHTHYL)PIPERAZINE AT TERMINAL5-HT AUTORECEPTORS IN GUINEA-PIG BRAIN", Naunyn-Schmiedeberg's archives of pharmacology, 351(4), 1995, pp. 377-384

Abstract

The effect of 1-(1-naphthyl)piperazine (NP) on the 5-HT terminal autoreceptor modulating 5-HT release was investigated in vitro and in vivo. In vitro 5-HT release was measured in slices of guinea-pig substantia nigra and hypothalamus prelabelled with H-3-5-HT, superfused with Krebs solution and depolarized electrically. NP, at 0.1 and 1 mu mol/l, did not modify the calcium-dependent release of 3H-5-HT elicited by electrical stimulation using a frequency of 5 Hz, however at 0.1 mu mol/l NP shifted to the right the inhibition curve of the non-selective autoreceptor agonist, 5-carboxamidotryptamine, in both regions. In hypothalamus when using lower frequencies (1 Hz or 0.2 Hz) or under pseudo-one-pulse stimulation, NP decreased the release of H-3-5-HT at 1 mu mol/l. In vivo microdialysis was used to measure extracellular levels ofendogenous 5-HT in the substantia nigra of freely moving guineapigs. The endogenous release of 5-HT was tetrodotoxin (TTX)-sensitive, indicating a neuronal origin of this efflux. NP, administered through the microdialysis probe (1-100 mu mol/l), increased the levels of extracellular 5-HT in concentration-dependent and TTX-sensitive manner. These results suggest that in vitro NP acts as a 5-HT autoreceptor partial (ant)agonist in the substantia nigra and hypothalamus of guinea-pigs, and as a full antagonist in vivo. However, NP administered systemically at 10 mg/kg i.p., did not modify the levels of extracellular 5-HT in the substantia nigra. This lack of systemic effect of NP probably results from its interaction at other receptors that modify 5-HT neurotransmission. In particular, NP is an agonist at 5-HT,, somatodendritic receptors in the raphe nucleus, an action which would decrease the release of 5-HT.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 05:39:50