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Titolo:
Zaleplon displays a selectivity to recombinant GABA(A) receptors differentfrom zolpidem, zopiclone and benzodiazepines
Autore:
Damgen, K; Luddens, H;
Indirizzi:
Univ Mainz, Clin Res Grp, Dept Psychiat, D-55131 Mainz, Germany Univ Mainz Mainz Germany D-55131 , Dept Psychiat, D-55131 Mainz, Germany
Titolo Testata:
NEUROSCIENCE RESEARCH COMMUNICATIONS
fascicolo: 3, volume: 25, anno: 1999,
pagine: 139 - 148
SICI:
0893-6609(199911/12)25:3<139:ZDASTR>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
LORAZEPAM; PSYCHOMOTOR; DIAZEPAM;
Keywords:
recombinant GABA(A) receptors; zaleplon; zopiclone; zolpidem; lorazepam; Ro15-4513;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Damgen, K Univ Mainz, Clin Res Grp, Dept Psychiat, Untere Zahlbacher Str 8, D-55131 Mainz, Germany Univ Mainz Untere Zahlbacher Str 8 Mainz Germany D-55131 ermany
Citazione:
K. Damgen e H. Luddens, "Zaleplon displays a selectivity to recombinant GABA(A) receptors differentfrom zolpidem, zopiclone and benzodiazepines", NEUROSC R C, 25(3), 1999, pp. 139-148

Abstract

A chemically heterogeneous group of compounds acts at the benzodiazepine (BZ) recognition site of the gamma-aminobutyric acid type A (GABAA) receptorcomplex. Whereas most 1,4-BZs recognize all GABA(A)/BZ receptors with similar affinity, other compounds differentiate between the large number of native GABA(A) receptors which assemble from the more than 14 known subunits. Here we describe the in vitro binding properties of the BZs lorazepam and Ro 15-4513 plus the three hypnotics zaleplon, zolpidem and zopiclone to eight receptor subtypes. Lorazepam fits well into the general scheme for other1,4-BZs with respect to its receptor subtype selectivity in spite of its clinically different use. Zaleplon but not zolpidem recognizes alpha 2- and alpha 3-receptors that additionally contain a beta j and the gamma 3-subunit. We conclude that the hypnotic zaleplon displays a novel receptor selectivity different from other BZ receptor ligands in clinical use. Furthermore,our data indicate that the alpha 1 beta j gamma 2 receptor subtype may be the main mediator of the hypnotic properties of BZ receptor ligands.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 15:06:41