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Titolo:
Differential occupancy of somatodendritic and postsynaptic 5HT(1A) receptors by pindolol: A dose-occupancy study with [C-11]WAY 100635 and positron emission tomography in humans
Autore:
Martinez, D; Hwang, DR; Mawlawi, O; Slifstein, M; Kent, J; Simpson, N; Parsey, RV; Hashimoto, T; Huang, YY; Shinn, A; Van Heertum, R; Abi-Dargham, A; Caltabiano, S; Malizia, A; Cowley, H; Mann, JJ; Laruelle, M;
Indirizzi:
New York State Psychiat Inst, Dept Neurosci, Div Brain Imaging, New York, NY 10032 USA New York State Psychiat Inst New York NY USA 10032 New York, NY 10032 USA Columbia Univ Coll Phys & Surg, Dept Psychiat, New York, NY 10032 USA Columbia Univ Coll Phys & Surg New York NY USA 10032 w York, NY 10032 USA Columbia Univ Coll Phys & Surg, Dept Radiol, New York, NY 10032 USA Columbia Univ Coll Phys & Surg New York NY USA 10032 w York, NY 10032 USA SmithKline Beecham Pharmaceut, Addenbrookes Ctr Clin Investigat, Cambridge, England SmithKline Beecham Pharmaceut Cambridge England gat, Cambridge, England
Titolo Testata:
NEUROPSYCHOPHARMACOLOGY
fascicolo: 3, volume: 24, anno: 2001,
pagine: 209 - 229
SICI:
0893-133X(200103)24:3<209:DOOSAP>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
PLACEBO-CONTROLLED TRIAL; SEROTONIN REUPTAKE INHIBITORS; ADRENOCEPTOR BLOCKING-AGENTS; IN-VIVO MICRODIALYSIS; DORSAL RAPHE NEURONS; 5-HT1A RECEPTORS; RAT-BRAIN; MAJOR DEPRESSION; DOUBLE-BLIND; BINDING-SITES;
Keywords:
5HT(1A) receptors; positron emission tomography; [C-11]WAY 100635; pindolol; SSRI; mood disorders;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
94
Recensione:
Indirizzi per estratti:
Indirizzo: Martinez, D New York State Psychiat Inst, Dept Neurosci, Div Brain Imaging, 1051 Riverside Dr,Box 42, New York, NY 10032 USA New York State Psychiat Inst 1051 Riverside Dr,Box 42 New York NY USA 10032
Citazione:
D. Martinez et al., "Differential occupancy of somatodendritic and postsynaptic 5HT(1A) receptors by pindolol: A dose-occupancy study with [C-11]WAY 100635 and positron emission tomography in humans", NEUROPSYCH, 24(3), 2001, pp. 209-229

Abstract

Augmentation of selective serotonin reuptake inhibitors (SSRIs) therapy bythe 5-HT1A receptor agent pindolol may reduce the delay between initiationof antidepressant treatment and clinical response. This hypothesis is based on the ability of pindolol to block 5-HT1A autoreceptors in the dorsal raphe nuclei (DRN) and to potentiate the increase in 5-HT transmission induced by SSRIs. However, placebo-controlled clinical studies of pindolol augmentation of antidepressant therapy have reported inconsistent results. Here, we evaluated the occupancy of 5-HT1A receptors during treatment with pindolol controlled release (CR) in nine healthy volunteers with Positron Emission Tomography and [C-11]WAY 100635. Subjects were studied four times: at baseline,following one week of pindolol CX 7.5 mg/day (4 and 10 hrs post dose), and following one dose of pindolol CR 30 mg(4 hrs post dose). Occupancy of the DRN was 40 +/- 29% on scan 2, 38 +/- 26% on scan 3, and 64 +/- 15% onscan 4. The average occupancy in all other regions was significantly lowerat each doses (18 +/- 15% on scan 2, 12 +/- 3% on scan 3, and 42 +/- 4% onscan 4). These results suggest that the blockade in the DRN reached in clinical studies (7.5 mg/day might be too low and variable to consistently augment the therapeutic effect of SSRIs. However, these data indicate that pindolol exhibits in vivo selectivity for the DRN 5-HT1A autoreceptors. As DRNselectivity is desirable for potentiation of 5-HT function, this observation represents an important proof of concept for the development 5-HT1A agents in this application. (C) 2001 American College of Neuropsychopharmacology. Published by Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/01/20 alle ore 16:55:37