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Titolo:
Effect of flibanserin (BIMT 17), fluoxetine, 8-OH-DPAT and buspirone on serotonin synthesis in rat brain
Autore:
Brambilla, A; Baschirotto, A; Grippa, N; Borsini, F;
Indirizzi:
Boehringer Ingelheim Italia, Dept Biol, I-20139 Milan, Italy Boehringer Ingelheim Italia Milan Italy I-20139 ol, I-20139 Milan, Italy
Titolo Testata:
EUROPEAN NEUROPSYCHOPHARMACOLOGY
fascicolo: 1, volume: 10, anno: 1999,
pagine: 63 - 67
SICI:
0924-977X(199912)10:1<63:EOF(1F>2.0.ZU;2-J
Fonte:
ISI
Lingua:
ENG
Soggetto:
5-HT2A RECEPTOR ANTAGONIST; DORSAL RAPHE NEURONS; CEREBRAL-CORTEX; AGONIST; ANTIDEPRESSANT; 5-HYDROXYTRYPTAMINE; RESPONSES; BINDING; RELEASE; NUCLEI;
Keywords:
flibanserin; 5-HT1A agonists; 5-HT uptake blockers; 5-HT synthesis; rat;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
31
Recensione:
Indirizzi per estratti:
Indirizzo: Brambilla, A Boehringer Ingelheim Italia, Dept Biol, Via Lorenzini 8, I-20139 Milan, Italy Boehringer Ingelheim Italia Via Lorenzini 8 Milan Italy I-20139
Citazione:
A. Brambilla et al., "Effect of flibanserin (BIMT 17), fluoxetine, 8-OH-DPAT and buspirone on serotonin synthesis in rat brain", EUR NEUROPS, 10(1), 1999, pp. 63-67

Abstract

In male rats, the effects of the administration of the novel serotonergic agent flibanserin on the synthesis of 5-HT were evaluated in the frontal cortex (FC), hippocampus (Hip) and brainstem (Br). The selective serotonergicuptake blocker, fluoxetine, and two serotonin,, (5-HT1A) agonists, 8-hydroxy-2-(di-n-propylamino)tetraline (8-OH-DPAT) and buspirone, were used as reference compounds. The synthesis of 5-HT was assessed by measuring the accumulation of 5-hydroxytryptophan (5-HTP) after blockade of aromatic amino acid decarboxylase induced by m-hydroxybenzylhydrazine (NSD-1015), at 100 mg/kg i.p., 30 min before sacrifice. Flibanserin, 8-OH-DPAT and buspirone weregiven 15 min before NSD-1015, while fluoxetine 120 min before NSD-1015. Inour experimental conditions, a different efficacy, expressed as percentageof maximal inhibition (Max) of 5-HTP accumulation, and a different potency, expressed in terms of minimal effective dose (MED), were observed in different brain areas with tested compounds. Flibanserin (1-32 mg/kg) decreased5-HT synthesis with preferential activity in the FC, compared to the Hip and Br, both in terms of potency (MED=2 mg/kg in FC, 16 mg/kg in Hip and Br)and efficacy (Max=65% in FC, 44% in Hip and 29% in Br). Fluoxetine (1-30 mg/kg) decreased 5-HT synthesis with preferential activity in FC than in Hipand Br, only in terms of potency (MED=3 mg/kg in FC, 10 mg/kg in Hip and Br), this result brings similar to that observed for flibanserin. In contrast, it showed greater efficacy both in FC and Hip (Max about 60%), than in Br (Max=49%). On the contrary, 8-OH-DPAT (0.3-3 mg/kg) decreased 5-HT synthesis with the same potency in all brain regions (MED=3 mg/kg) and showed thegreatest efficacy in FC than in Hip and Br (Max=56% in FC, 49% in Hip and 40% in Br). Furthermore, buspirone (3-30 mg/kg), while inhibiting 5-HTP accumulation in all areas with the same efficacy (Max about 30%), seemed to have higher potency in Br than in FC and Hip (MED=3 mg/kg in Br, 10 mg/kg in FC and Hip). The results in terms of regional differences are discussed. (C) 1999 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 12:19:41