| New evidence that the antiestrogen binding site may be a novel growth-promoting histamine receptor (?H3) which mediates the antiestrogenic and antiproliferative effects of tamoxifen |
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| 收稿时间： | 6 December 1985 |
New evidence that the antiestrogen binding site may be a novel growth-promoting histamine receptor (?H3) which mediates the antiestrogenic and antiproliferative effects of tamoxifen |
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| Authors: | L J Brandes R P Bogdanovic |
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| Institution: | 1. Department of Pharmaceutical Sciences, University of Milan, 20133 Milan, Italy;2. Dompé Pharmaceutici S.p.A., 67100 L’Aquila, Italy;3. IRCCS Humanitas Research Hospital, via Manzoni 56, Rozzano, 20089 Milan, Italy;4. Department of Medical Biotechnology and Translational Medicine, University of Milan, 20133 Milan, Italy |
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| Abstract: | Using as a probe 3H]-DPPE (N,N-diethyl-2-(4-phenylmethyl)phenoxy]ethanamine HCl), a novel compound selective for the antiestrogen binding site (AEBS), new evidence is presented that this site could be a growth-promoting histamine receptor of a type not previously described (?H3). In the rat uterus, DPPE alone at a concentration of 4 mg/kg acts as an estrogen antagonist, unlike TAM alone which is a partial estrogen agonist. In the presence of exogenous estradiol, both TAM and DPPE are partial antagonists. This suggests that the "antiestrogenic" effects of tamoxifen are mediated through AEBS/?H3 while the estrogenic effects are mediated through ER. |
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