The aim of this study is to assess the androgen receptor (AR) agonistic/antagonistic effects on various chemicals, which are used in household products including cleaning agents and wetted tissues by in vitro OECD test guideline No. 458 (using AR-EcoScreen™ cell line) and the me-too test method (using 22Rv1cell line), which was adopted as OECD project No. 4.99. All chemicals were not determined as AR agonists. However α-dodecyl-ω-hydroxypoly (oxyethylene) and 3-iodo-2-propynyl butylcarbamate have shown a weak AR antagonistic effects with IC values of 2.18 ± 0.12 and 4.26 ± 0.17 μg/ml via binding affinity to AR in only 22Rv1/mouse mammary tumor virus using AR transcriptional activation assay, because of their different cytotoxicity on each applied cell line. This report firstly provides information about agonistic/antagonistic effects against human AR of various chemicals including surfactants and biocides by OECD in vitro stably transfected transcriptional activation assays. However, further in vivo and human model studies are needed to confirm their adverse effects.
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http://dx.doi.org/10.1016/j.chemosphere.2017.10.084 | DOI Listing |
Ecotoxicol Environ Saf
December 2024
Area of Toxicology, Faculty of Pharmacy, University of Sevilla, Profesor García González nº 2, Sevilla 41012, Spain.
The potential endocrine disruption activity of cyanotoxins, particularly their effects on estrogen and androgen receptors (ER, AR), remains poorly understood. In the present study, the potential agonistic/antagonistic estrogenic and androgenic activities of MC-LR and CYN have been determined for the first time with validated OECD Test Guidelines No. 455 and 458, respectively.
View Article and Find Full Text PDFFront Endocrinol (Lausanne)
September 2023
Evestra, Inc., Corporate Headquarters, Schertz, TX, United States.
Introduction: The pharmacological target for progesterone, different progestins, and Selective Progesterone Receptor Modulators (SPRMs) is the nuclear progesterone receptor (PR). EC313 is a new member of a subgroup of SPRMs, mesoprogestins, which combine especially PR- agonistic and PR-antagonistic activities in one molecule.
Methods: The suitable -model for the differentiation of SPRMs from the subgroup of mesoprogestins is the estrogen-primed juvenile rabbit endometrium assay (McPhail Assay).
Plants (Basel)
January 2023
Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, Traian Vuia 6, 020956 Bucharest, Romania.
Diseases such as cancer, neurological pathologies and chronic pain represent currently unmet needs. The existing pharmacotherapeutic options available for treating these conditions are limited by lack of efficiency and/or side effects. Transient receptor potential vanilloid 1 ion channel emerged as an attractive therapeutic target for developing new analgesic, anti-cancer and antiepileptic agents.
View Article and Find Full Text PDFCurr Med Chem
June 2023
Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Ghudda, Bathinda (Pb), 151401, India.
Background: Breast cancer is considered to be 2most common cancer subtype investigated worldwide. It is mainly prevalent in postmenopausal women. Estrogen Receptor (ER) is a primary transcription factor for the survival and growth of tumors.
View Article and Find Full Text PDFMany case reports have demonstrated that using antidepressants and especially the selective serotonin reuptake inhibitors (SSRIs), and the noradrenergic and specific serotonergic antidepresants mirtazapine and mianserin can lead to restless legs syndrome (RLS). However, there are disagreements in the results of the limited number of investigations on the relationship of RLS with antidepressants. Trazodone is a frequently used antidepressant with complex agonistic/antagonistic effects on the serotonergic system and moderate blockage on the histamine receptor.
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