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Titolo:
Lack of stereoselectivity of 8-hydroxy-2(di-N-propylamino)tetralin-mediated inhibition of forskolin-stimulated adenylyl cyclase activity in human pre- and post-synaptic brain regions
Autore:
Palego, L; Giromella, A; Marazziti, D; Giannaccini, G; Borsini, F; Bigazzi, F; Naccarato, AG; Lucacchini, A; Cassano, GB; Mazzoni, MR;
Indirizzi:
Univ Pisa, Dipartimento Psichiatria Neurobiol Farmacol & Bio, I-56100 Pisa, Italy Univ Pisa Pisa Italy I-56100 urobiol Farmacol & Bio, I-56100 Pisa, Italy Univ Pisa, Dipartimento Oncol, I-56100 Pisa, Italy Univ Pisa Pisa Italy I-56100 sa, Dipartimento Oncol, I-56100 Pisa, Italy
Titolo Testata:
NEUROCHEMISTRY INTERNATIONAL
fascicolo: 3, volume: 36, anno: 2000,
pagine: 225 - 232
SICI:
0197-0186(200003)36:3<225:LOSO8>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
NUCLEOTIDE REGULATORY PROTEINS; RECEPTOR ANTAGONISTS; 5-HT1A RECEPTORS; 5-HYDROXYTRYPTAMINE1A RECEPTORS; PARTIAL AGONIST; LIGANDS; DESENSITIZATION; ENANTIOMERS; DEPRESSION; RESPONSES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
35
Recensione:
Indirizzi per estratti:
Indirizzo: Palego, L Univ Pisa, Dipartimento Psichiatria Neurobiol Farmacol & Bio, Via Bonanno 6, I-56100 Pisa, Italy Univ Pisa Via Bonanno 6 Pisa Italy I-56100 I-56100 Pisa, Italy
Citazione:
L. Palego et al., "Lack of stereoselectivity of 8-hydroxy-2(di-N-propylamino)tetralin-mediated inhibition of forskolin-stimulated adenylyl cyclase activity in human pre- and post-synaptic brain regions", NEUROCHEM I, 36(3), 2000, pp. 225-232

Abstract

The stereoselectivity of the serotonin(1 A) (5-HT1 A) receptor compound 8-hydroxy-2(di-N-propylamino)tetralin (8-OH-DPAT) on forskolin-stimulated adenylyl cyclase activity was investigated in membranes from human 5-HT pre-synaptic (raphe nuclei) and post-synaptic (hippocampus and prefrontal cortex)regions of autopsy brains. After sample incubation with agonists and antagonists, results showed that both the racemic mixture of 8-OH-DPAT or its (+) and (-) enantiomers behaved as full agonists in the tested brain regions. Enantiomer potency (EC50, nM) and efficacy (percentage of maximal inhibition, %) values were similar in all regions under investigation. However, some inter and intra-region variations in racemic 8-OH-DPAT potency and efficacy have been observed. In particular, the potency of racemic 8-OH-DPAT was higher in the prefrontal cortex and raphe nuclei than in the hippocampus, where it was in fact lower than either single enantiomers. Agonist effects were competitively reversed by 5-HT1 A antagonists, although once again a different profile was revealed in the hippocampus. The data underscores the lack of stereospecificity of 8-OH-DPAT-mediated inhibition of adenylyl cyclase activity in either pre- or post-synaptic human brain regions. Moreover; such results have significant implication. as they support the notion that human 5-HT1 (A) receptors might vary from one brain region to the other. (C) 2000 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 18:33:40