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Effects of estrogen agonists on amphetamine‐stimulated striatal dopamine release
Author(s) -
Xiao Li,
Becker Jill B.
Publication year - 1998
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/(sici)1098-2396(199808)29:4<379::aid-syn10>3.0.co;2-m
Subject(s) - estrogen , striatum , chemistry , amphetamine , dopamine , estriol , endocrinology , diethylstilbestrol , medicine , estrone , estrogen receptor , pharmacology , biology , cancer , breast cancer
Based upon the observation that estrogen acts in the striatum to rapidly modulate dopamine (DA) neural transmission and DA‐mediated behaviors, it has been postulated that these effects of estrogen are mediated by a specific, membrane‐bound receptor mechanism. To further characterize the pharmacological specificity of the estrogen binding site, the present experiments examine effects of various estrogen agonists on amphetamine (AMPH)‐induced DA release from striatal tissue of ovariectomized female rats, using a superfusion method. Catechol estrogens 4‐, and 2‐hydroxyestradiol, but not 2‐methoxyestradiol, significantly enhance AMPH‐induced striatal DA release. Estrogen metabolites, estrone and estriol, and the non‐steroidal estrogen analog, diethylstilbestrol, are without effects. Estradiol conjugated to bovine serum albumin (BSA) mimics the effect of estradiol to enhance stimulated striatal DA release. These results indicate that the steroidal configuration and hydroxylation on the A‐ring of estrogenic compounds may be important determinants of ligand binding to the putative estrogen binding site in the striatum. Furthermore, the effectiveness of the estradiol conjugated to BSA reinforces the idea of an external membrane‐bound receptor binding site in the striatum. Synapse 29:379–391, 1998. © 1998 Wiley‐Liss, Inc.