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Titolo:
Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT1B, 5-HT1D and dopamine D-2 and D-3 receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states
Autore:
Millan, MJ; Newman-Tancredi, A; Audinot, V; Cussac, D; Lejeune, F; Nicolas, JP; Coge, F; Galizzi, JP; Boutin, JA; Rivet, JM; Dekeyne, A; Gobert, A;
Indirizzi:
Ctr Rech Croissy, Inst Rech Servier, Dept Psychopharmacol, F-78290 CroissySur Seine, France Ctr Rech Croissy Croissy Sur Seine France F-78290 oissySur Seine, France Inst Rech Servier, Ctr Rech Croissy, Dept Mol & Cellular Pharmacol, F-78290 Paris, France Inst Rech Servier Paris France F-78290 Pharmacol, F-78290 Paris, France
Titolo Testata:
SYNAPSE
fascicolo: 2, volume: 35, anno: 2000,
pagine: 79 - 95
SICI:
0887-4476(200002)35:2<79:AAAAOY>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
FREELY-MOVING RATS; GAMMA-S BINDING; VENTRAL TEGMENTAL AREA; PLACEBO-CONTROLLED TRIAL; CENTRAL-NERVOUS-SYSTEM; CORTEX IN-VIVO; FRONTAL-CORTEX; PREFRONTAL CORTEX; EXTRACELLULAR DOPAMINE; ADRENERGIC-RECEPTOR;
Keywords:
frontal cortex; antidepressant; depression; yohimbine; SSRI; fluoxetine; [S-35]GTP gamma S binding;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
112
Recensione:
Indirizzi per estratti:
Indirizzo: Millan, MJ Ctr Rech Croissy, Inst Rech Servier, Dept Psychopharmacol, 125 Chem Ronde,F-78290 Croissy Sur Seine, France Ctr Rech Croissy 125 Chem Ronde Croissy Sur Seine France F-78290
Citazione:
M.J. Millan et al., "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT1B, 5-HT1D and dopamine D-2 and D-3 receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states", SYNAPSE, 35(2), 2000, pp. 79-95

Abstract

Herein, we evaluate the interaction of the alpha(2)-AR antagonist, yohimbine, as compared to fluparoxan, at multiple monoaminergic receptors and examine their roles in the modulation of adrenergic, dopaminergic and serotonergic transmission in freely-moving rats. Yohimbine displays marked affinity at human (h)alpha(2A)-, h alpha(2B)- and h alpha(2C)-ARs, significant affinity for h5-HT1A, h5-HT1B, h5-HT1D, and hD(2) receptors and weak affinity for hD(3) receptors. In [S-35] GTP gamma S binding protocols, yohimbine exerts antagonist actions at h alpha(2A)-AR, h5-HT1B, h5-HT1D, and h(D2) sites, yet partial agonist actions at h5-HT1A sites. In vivo, agonist actions of yohimbine at 5-HT1A sites are revealed by WAY100,635-reversible induction ofhypothermia in the rat. In guinea pigs, antagonist actions of yohimbine at5-HT1B receptors are revealed by blockade of hypothermia evoked by the 5-HT1B agonist, GR46,611. In distinction to yohimbine, fluparoxan shows only modest partial agonist actions at h5-HT1A sites versus marked antagonist actions at h alpha(2)-ARs. While fluparoxan selectively enhances hippocampal noradrenaline (NAD) turnover, yohimbine also enhances striatal dopamine (DA)turnover and suppresses striatal turnover of 5-HT. Further, yohimbine decreases firing of serotonergic neurones in raphe nuclei, an action reversed by WAY100,635. Fluparoxan increases extracellular levels of DA and NAD, but not 5-HT, in frontal cortex. In analogy, yohimbine enhances FCX levels of DA and NAD, yet suppresses those of 5-HT: the latter effect being antagonized by WAY100,635. The induction by fluoxetine of FCX levels of 5-HT, DA, andNAD is potentiated by fluparoxan. Yohimbine likewise facilitates the influence of fluoxetine upon DA and NAD levels, but not those of 5-HT. In conclusion, the alpha(2)-AR antagonist properties of yohimbine increase DA and NAD levels both alone and in association with fluoxetine. However, in contrast to the selective alpha(2)-AR antagonist, fluparoxan, the 5-HT1A agonist actions of yohimbine suppress 5-HT levels alone and underlie its inability to augment the influence of fluoxetine upon 5-HT levels. (C) 2000 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 12:47:34