Sex Hormones (Male): Analogs and Antagonists

Brueggemeier, Robert W.

doi:10.1002/3527600906.mcb.200500066

Cited by 5 publications

(6 citation statements)

References 465 publications

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“…Furthermore, they differ in their impact on blood glucose levels and the lipid profile (e.g., Sitruk-Ware, 2006). Importantly, older generation progestins (e.g., Levonorgestrel, desogestel, gestoden, norgestimat), are as derivates of 19-nortestosterone, a common anabolic steroid (Brueggemeier, 2006), able to activate androgen receptors and exert androgenic actions (Sitruk-Ware, 2006; Wiegratz and Kuhl, 2006). Newer progestins (e.g., dienogest, drospirenone) on the other hand, bind very specifically to the progesterone receptor and are anti-androgenic (Wiegratz and Kuhl, 2006).…”

Section: Effects Of Hormonal Contraceptives: “Feminizing” or “Masculimentioning

confidence: 99%

50 years of hormonal contraceptionâ€”time to find out, what it does to our brain

2014

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Hormonal contraceptives are on the market for more than 50 years and used by 100 million women worldwide. However, while endogenous steroids have been convincingly associated with change in brain structure, function and cognitive performance, the effects of synthetic steroids contained in hormonal contraceptives on brain and cognition have barely been investigated. In this article we summarize the sparse findings, describing brain structural, functional and behavioral findings from the literature and suggest that synthetic steroids may contribute to masculinizing as well as feminizing effects on brain and behavior. We try to identify methodological challenges, explain, how results on endogenous steroids may transfer into research on hormonal contraceptives and point out factors that need to be controlled in the study of hormonal contraceptive dependent effects. We conclude that there is a strong need for more systematic studies, especially on brain structural, functional and cognitive changes due to hormonal contraceptive use. The hormonal contraceptive pill is the major tool for population control. Hence, such behavioral changes could cause a shift in society dynamics and should not stay unattended.

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Section: Effects Of Hormonal Contraceptives: “Feminizing” or “Masculimentioning

confidence: 99%

50 years of hormonal contraceptionâ€”time to find out, what it does to our brain

2014

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“…Because of their anabolic effects, AAS are commonly abused by athletes (5,6,8,63). Many synthetic AAS have been developed in an attempt to alleviate some of the adverse androgenic and estrogenic effects while enhancing the anabolic properties.…”

Section: Anabolic-androgenic Steroidsmentioning

confidence: 99%

“…Testosterone is prototype for the development of new androgen receptor agonists; the goals of the development of synthetic AAS are to improve the pharmacologic properties of the compounds (63). For example, carbon 17-β esters of TEST have been manufactured; esterification of this site makes the steroid more fat soluble for parental use and delays its absorption.…”

Section: Anabolic-androgenic Steroidsmentioning

confidence: 99%

“…Testosterone alkyl derivatives at the carbon 17-α position resist metabolism in the liver and are orally active, but are also associated with severe liver toxicities. Modification of the A, B, or C rings of the steroid have several goals including slowing the metabolism (and decreasing affinity for metabolizing enzymes), enhancing affinity for the hAR and hGR, and causing resistance to aromatization (6,8,63). For example, the removal of carbon 19, reduction at the 5α carbon position, the replacement of carbon 2 with oxygen, and the addition of a heterocyclic ring to carbons 2 and 3 all increase anabolic activity.…”

Section: Anabolic-androgenic Steroidsmentioning

confidence: 99%

“…Following this discovery, several more nonsteroidal selective androgen receptor modulators (SARMs) were developed; all lacking a core steroid structure (69,71). SARMs have tissue selective activation of the hAR; they can be strong agonists in one tissue and antagonists or weak agonist in another (63). The ideal SARM has been described as a compound which exerts tissue-specific anabolic effects in vivo, with anabolic effects in muscle and bone but lesser effects in the prostate and seminal vesicles (72).…”

Section: Selective Androgen Receptor Modulators (Sarms)mentioning

confidence: 99%

See 2 more Smart Citations

The Androgen Receptor and Its Use in Biological Assays: Looking Toward Effect-Based Testing and Its Applications

Cadwallader

Lim

Rollins

et al. 2011

Journal of Analytical Toxicology

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Steroid abuse is a growing problem among amateur and professional athletes. Because of an inundation of newly and illegally synthesized steroids with minor structural modifications and other designer steroid receptor modulators, there is a need to develop new methods of detection which do not require prior knowledge of the abused steroid structure. The number of designer steroids currently being abused is unknown because detection methods in general are only identifying substances with a known structure. The detection of doping is moving away from merely checking for exposure to prohibited substance toward detecting an effect of prohibited substances, as biological assays can do. Cell-based biological assays are the next generation of assays which should be utilized by antidoping laboratories; they can detect androgenic anabolic steroid and other human androgen receptor (hAR) ligand presence without knowledge of their structure and assess the relative biological activity of these compounds. This review summarizes the hAR and its action and discusses its relevance to sports doping and its use in biological assays.

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In Silico Identification of Piperazine Linked Thiohydantoin Derivatives as Novel Androgen Antagonist in Prostate Cancer Treatment

Bhati

Kaushik

Singh

2018

Int J Pept Res Ther

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Sex Hormones (Male): Analogs and Antagonists

Cited by 5 publications

References 465 publications

50 years of hormonal contraceptionâ€”time to find out, what it does to our brain

50 years of hormonal contraceptionâ€”time to find out, what it does to our brain

The Androgen Receptor and Its Use in Biological Assays: Looking Toward Effect-Based Testing and Its Applications

In Silico Identification of Piperazine Linked Thiohydantoin Derivatives as Novel Androgen Antagonist in Prostate Cancer Treatment

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