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A MONOHYDROXYLATED METABOLITE OF TAMOXIFEN WITH POTENT ANTIOESTROGENIC ACTIVITY
Abstract
The oestrogenic and antioestrogenic properties of tamoxifen and its monohydroxylated (monohydroxytamoxifen) and dihydroxylated (dihydroxytamoxifen) metabolites have been investigated in the immature rat. Whether administered orally or subcutaneously, monohydroxytamoxifen was more active than tamoxifen as an antioestrogen. Dihydroxytamoxifen was less active than tamoxifen as an antioestrogen, but this derivative alone was unable to induce a uterotrophic response. Both metabolites of tamoxifen were potent inhibitors of the binding of [3 H]oestradiol to oestrogen receptors in vitro. It is possible that the metabolites play a supportive role in the antioestrogenic activity of tamoxifen. The potent activity of monohydroxytamoxifen in vivo and in vitro suggests that this compound could be an important new tool for the subcellular investigation of oestrogenic and antioestrogenic events.
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Cited by
Patel, H. K., & Bihani, T. (2018) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.12.012 · Cited by 499
Jordan, V. C. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm020449y · Cited by 414
Self-citationJordan, V. C. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm020450x · Cited by 396
Self-citationDrug interactions in cancer therapy
Scripture, C. D., & Figg, W. D. (2006) · Nature Reviews Cancer · doi:10.1038/nrc1887 · Cited by 366
Goetz, M. P., Sangkuhl, K., Guchelaar, H., Schwab, M., Province, M., Whirl‐Carrillo, M., Symmans, W. F., McLeod, H. L., Ratain, M. J., Zembutsu, H., et al. (2018) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.1007 · Cited by 336
Metadata
- Authors
- JORDAN, V. C., COLLINS, M. M., ROWSBY, L., & PRESTWICH, G.
- Venue
- Journal of Endocrinology
- Publisher
- Bioscientifica
- Published
- 1977-11
- Volume
- 75
- Issue
- 2
- Pages
- 305-316
- ISSN
- 0022-0795 (ISSN-L)
- 1479-6805
- OpenAlex
- W2074335085
- Cited by
- 506
- References
- 0
- FWCI
- 7.74
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: A MONOHYDROXYLATED METABOLITE OF TAMOXIFEN WITH POTENT ANTIOESTROGENIC ACTIVITY. https://app.cochat.ai/papers/10.1677/joe.0.0750305
- The paper
- JORDAN, V. C., COLLINS, M. M., ROWSBY, L., & PRESTWICH, G. (1977). A MONOHYDROXYLATED METABOLITE OF TAMOXIFEN WITH POTENT ANTIOESTROGENIC ACTIVITY. Journal of Endocrinology. https://doi.org/10.1677/joe.0.0750305
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
