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Titolo:
PHARMACOLOGICAL AND FUNCTIONAL-CHARACTERIZATION OF D-2, D-3 AND D-4 DOPAMINE-RECEPTORS IN FIBROBLAST AND DOPAMINERGIC CELL-LINES
Autore:
TANG L; TODD RD; HELLER A; OMALLEY KL;
Indirizzi:
WASHINGTON UNIV,SCH MED,DEPT ANAT & NEUROBIOL,660 S EUCLID AVE ST LOUIS MO 63110 WASHINGTON UNIV,SCH MED,DEPT ANAT & NEUROBIOL ST LOUIS MO 63110 UNIV CHICAGO,DEPT PHARMACOL & PHYSIOL SCI CHICAGO IL 60637
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 268, anno: 1994,
pagine: 495 - 502
SICI:
0022-3565(1994)268:1<495:PAFODD>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
ADENYLATE-CYCLASE; MOLECULAR-CLONING; EXPRESSION; CDNA; GENE; IDENTIFICATION; TRANSCRIPTS; ACTIVATION; SUBTYPES; D3;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
29
Recensione:
Indirizzi per estratti:
Citazione:
L. Tang et al., "PHARMACOLOGICAL AND FUNCTIONAL-CHARACTERIZATION OF D-2, D-3 AND D-4 DOPAMINE-RECEPTORS IN FIBROBLAST AND DOPAMINERGIC CELL-LINES", The Journal of pharmacology and experimental therapeutics, 268(1), 1994, pp. 495-502

Abstract

In order to study the properties of the D-2-like dopamine receptors, D-2, D-3 and D-4 clones were transfected into mouse Ltk(-) fibroblasts, CCL1.3, and a neuronal mesencephalic cell line, MN9D. Most of the derived antagonist and agonist inhibition constants were the same for a given receptor in either cell line as determined by saturation and competition binding experiments. The rank order potencies for antagonistsare: eticlopride, D-2 > D-3 > D-4; YM-09151-2, D-2 = D-4 > D-3; spiperone, D-2 = D-3 > D-4; (+)-butaclamol, D-2 > D-3 > D-4; clozapine, D-4> D-2 > D-3; and for agonists, quinpirole, D-3 = D-4 > D-2, 7-hydroxy-2-(di-n-propyl)-aminotetralin, D-3 > D-2 = D-4. Functionally, D-2 stimulation increases inositol phosphate levels in CCL1.3 cells but not in MN9D, whereas D-2 activation inhibits forskolin-stimulated cyclic AMP levels in both cell lines. D-4 stimulation has no effect on inositolphosphate metabolism in either cell type, but inhibits adenylate cyclase in MN9D cells. Both the D-2 and D-4 mediated decreases in cyclic AMP can be blocked by preincubation with pertussis toxin. D-3 does not couple to these pathways in either cell line. Reverse transcription/polymerase chain reaction techniques were used to determine the availability of cellular signalling systems. Both CCL1.3 and MN9D cells have high levels of G alpha(i2) expression, whereas neither cell expresses Galpha(i1) or G alpha(i3) These data imply that the D-2 receptor couples to the G alpha(i2) subtype in both cell lines, whereas D-4 does not. The differential coupling of D-2 and D-4 receptors demonstrates the utility of model central nervous system cell lines in addressing receptor-effector mechanisms.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 18:42:58