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Titolo:
INHIBITION OF STRIATAL DOPAMINE TRANSPORTER ACTIVITY BY 17-BETA-ESTRADIOL
Autore:
DISSHON KA; BOJA JW; DLUZEN DE;
Indirizzi:
NE OHIO UNIV,COLL MED,DEPT ANAT,4209 STATE ROUTE 44,POB 95 ROOTSTOWN OH 44272 NE OHIO UNIV,COLL MED,DEPT ANAT ROOTSTOWN OH 44272 NE OHIO UNIV,COLL MED,DEPT PHARMACOL ROOTSTOWN OH 44272
Titolo Testata:
European journal of pharmacology
fascicolo: 2, volume: 345, anno: 1998,
pagine: 207 - 211
SICI:
0014-2999(1998)345:2<207:IOSDTA>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-KINASE-C; MPTP-INDUCED NEUROTOXICITY; H-3 GBR-12935 BINDING; UPTAKE SITES; NUCLEUS-ACCUMBENS; SEX-DIFFERENCES; ESTROUS-CYCLE; ESTRADIOL; RELEASE; BRAIN;
Keywords:
DOPAMINE TRANSPORTER; UPTAKE INHIBITION; ESTRADIOL; STRIATAL SYNAPTOSOME; GONADAL STEROID HORMONE; PROGESTERONE; NIGROSTRIATAL;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
51
Recensione:
Indirizzi per estratti:
Citazione:
K.A. Disshon et al., "INHIBITION OF STRIATAL DOPAMINE TRANSPORTER ACTIVITY BY 17-BETA-ESTRADIOL", European journal of pharmacology, 345(2), 1998, pp. 207-211

Abstract

Striatal synaptosomes from ovariectomized rats were prepared to examine the effect of 17 beta-estradiol on [H-3]dopamine uptake. Estradiol inhibited [H-3]dopamine uptake in a dose-dependent manner, with an IC50 of 7.3 mu M. Use of identical concentrations of progesterone had no effect on [H-3]dopamine uptake. The effects of estradiol were exerted by decreasing the affinity of the transporter for dopamine, as revealed by a dose-dependent increase in the K-m. The K-m values for 0 (control), 10, and 100 mu M estradiol were 108 +/- 11, 258 +/- 44 and 415 +/- 40 nM, respectively, with each of the three concentrations tested being significantly different among each other. No statistically significant differences were obtained for the V-max, with values for the three increasing doses being 9.2 +/- 0.8, 8.3 +/- 0.5 and 7.3 +/- 0.8 pmol/min per mg protein. These results demonstrate that estradiol, but notprogesterone, inhibits striatal dopamine uptake by decreasing the affinity of the transporter fur dopamine. Such a mechanism may serve as one of the bases for the modulatory effects of estradiol upon the nigrostriatal dopaminergic system. (C) 1998 Elsevier Science B.V.

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Documento generato il 08/07/20 alle ore 07:57:29