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Titolo:
THE PUTATIVE DOPAMINE D-3 RECEPTOR AGONIST 7-OH-DPAT - LACK OF MESOLIMBIC SELECTIVITY
Autore:
LIU JC; COX RF; GREIF GJ; FREEDMAN JE; WASZCZAK BL;
Indirizzi:
NORTHEASTERN UNIV,DEPT PHARMACEUT SCI,312 MUGAR HALL BOSTON MA 02115 NORTHEASTERN UNIV,DEPT PHARMACEUT SCI BOSTON MA 02115 BURROUGHS WELLCOME CO,CNS SECT RES TRIANGLE PK NC 27709
Titolo Testata:
European journal of pharmacology
fascicolo: 3, volume: 264, anno: 1994,
pagine: 269 - 278
SICI:
0014-2999(1994)264:3<269:TPDDRA>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
INSITU HYBRIDIZATION HISTOCHEMISTRY; SINGLE UNIT-ACTIVITY; RAT-BRAIN; DIFFERENTIAL VISUALIZATION; MOLECULAR-CLONING; NUCLEUS ACCUMBENS; MESSENGER-RNA; NEURONS; LOCALIZATION; BINDING;
Keywords:
DOPAMINE D-3 RECEPTOR; 7-OH-DPAT (7-HYDROXY-N,N-DI-N-PROPYL-2-AMINOTETRALIN); PATCH CLAMP; SUBSTANTIA NIGRA; VENTRAL TEGMENTAL AREA; CAUDATE-PUTAMEN; NUCLEUS ACCUMBENS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
J.C. Liu et al., "THE PUTATIVE DOPAMINE D-3 RECEPTOR AGONIST 7-OH-DPAT - LACK OF MESOLIMBIC SELECTIVITY", European journal of pharmacology, 264(3), 1994, pp. 269-278

Abstract

7-Hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OH-DPAT), an agonist with relative selectivity for the dopamine D-3 receptor, was examined in several electrophysiological assays to determine whether it exhibits preferential effects in the mesolimbic versus nigrostriatal dopamine systems. Extracellular single unit activities of substantia nigra pars compacta (A9) and ventral tegmental area (A10) dopamine neurons, and caudate-putamen and nucleus accumbens neurons, were recorded in male rats anesthetized with chloral hydrate. Intravenous (i)-7-OH-DPAT potently and completely inhibited the firing of both A9 and A10 dopamine neurons (ED(50)'s: 3.5 +/- 0.7 mu g/kg and 3.9 +/- 9 mu g/kg, respectively). The active enantiomer, (+)-7-OH-DPAT, was 2 to 3 times more potent than the racemic drug (ED(50)'s: 1.2 +/- 0.3 mu g/kg and 1.7 +/- 0.4 mu g/kg for A9 and A10 cells, respectively). There were no significant differences in potency for either form in inhibiting A9 and A10 dopamine neurons. In other studies, iontophoretically applied (+)-7-OH-DPAT caused current-dependent inhibitions of spontaneously active or glutamate-driven caudate-putamen and nucleus accumbens neurons (I-50 values,6.5 and 7.9 nA, respectively). Again, no difference in potency between cell populations was noted. Finally, in cell-attached patch-clamp recordings from freshly dissociated rat caudate-putamen neurons, an 85 pS K+ channel known to be activated by dopamine and the ''D-2-like'' agonist quinpirole was also observed with (+)-7-OH-DPAT (0.2-1 mu M) applied in the patch pipette. Although dopamine D-3 receptors have been thought to play an important role in limbic areas, these results suggest that 7-OH-DPAT behaves similarly to dopamine D-2 agonists and does not discriminate between nigrostriatal and mesolimbic systems.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 12:04:18