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Titolo:
USE OF [H-3] CLOZAPINE AS A LIGAND OF THE DOPAMINE D-4 RECEPTOR SUBTYPE IN PERIPHERAL-TISSUES
Autore:
RICCI A; BRONZETTI E; ROSSODIVITA I; AMENTA F;
Indirizzi:
UNIV CAMERINO,DIPARTIMENTO SCI FARMACOL & MED SPERIMENTALE,SEZ ANAT UMANA,VIA SCALZINO 3 I-62032 CAMERINO ITALY UNIV CAMERINO,DIPARTIMENTO SCI FARMACOL & MED SPERIMENTALE,SEZ ANAT UMANA I-62032 CAMERINO ITALY UNIV ROMA LA SAPIENZA,DIPARTIMENTO SCI CARDIOVASC & RESP ROME ITALY
Titolo Testata:
Journal of autonomic pharmacology
fascicolo: 4, volume: 17, anno: 1997,
pagine: 261 - 267
SICI:
0144-1795(1997)17:4<261:UO[CAA>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
FUNCTIONAL-CHARACTERIZATION; MOLECULAR-CLONING; D4 RECEPTORS; CELL-LINES; EXPRESSION; GENE; BINDING; PHARMACOLOGY; CLOZAPINE; AFFINITY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
32
Recensione:
Indirizzi per estratti:
Citazione:
A. Ricci et al., "USE OF [H-3] CLOZAPINE AS A LIGAND OF THE DOPAMINE D-4 RECEPTOR SUBTYPE IN PERIPHERAL-TISSUES", Journal of autonomic pharmacology, 17(4), 1997, pp. 261-267

Abstract

1 Molecular biology studies have documented the presence of peripheral dopamine D-4 receptors. This site has not been characterized yet with classical radioligand binding assay techniques because of the lack of selective radioligands.2 The atypical neuroleptic clozapine labelledwith tritium ([H-3]-clozapine) has been proposed and sold as a radioligand for brain dopamine D-4 receptors. However, the selectivity of [H-3]-clozapine for D-4 receptor subtypes, and its specificity for braindopamine receptors, have been questioned. 3 In this study dopamine D-4 receptors were assayed in peripheral organs known to express them, such as rat atria and kidney, by using a radioligand binding assay technique with [H-3]-clozapine as the radioligand. Parallel experiments were performed using Chinese hamster ovary (CHO) cells transfected with the D-4 receptor clone (variant D-4.2) 4 [H-3]-Clozapine was bound to sections of rat atria and kidney. After appropriate blockade of sites other than dopamine receptors to which it can bind (i.e. muscarinic cholinergic, serotonergic and alpha-adrenergic receptors), the radioligand was bound to a site displaying a pharmacological profile similar tothat expressed by CHO cells transfected with the D-4 receptor. 5 The above findings indicate that with appropriate protocols, [H-3]-clozapine may represent a radioligand for peripheral dopamine D-4 receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 06:00:17