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GlossaryAndrogen Receptor Antagonists

block male hormones like testosterone from affecting tissues

Androgen Receptor Antagonists, also known as antiandrogens, are medications that block the action of androgens, which are male sex hormones like testosterone. These drugs work by binding to androgen receptors, preventing androgens from exerting their effects on tissues, and are commonly used in the treatment of conditions like prostate cancer, androgenic alopecia (male-pattern baldness), and certain types of acne.

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Synthesis and Biological Evaluation of Amino-Pyridines as Androgen Receptor Antagonists for Stimulating Hair Growth and Reducing Sebum Production

research Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production

17 citations , August 2007 in “Bioorganic & Medicinal Chemistry Letters”

A compound made by Pfizer can potentially stimulate hair growth and reduce oil production, making it a good candidate for topical use.

research Mineralocorticoid Receptor Antagonists—A New Sprinkle of Salt and Youth

8 citations , October 2016 in “Journal of Investigative Dermatology”

MR antagonists may improve skin health and wound healing, especially in aging.

research Pantolactams as androgen receptor antagonists for the topical suppression of sebum production

5 citations , September 2011 in “Bioorganic & Medicinal Chemistry Letters”

Pfizer found that pantolactam-based compounds can reduce sebum (skin oil) production when applied topically.

research Mineralocorticoid Receptor Antagonists Stimulate Human Hair Growth ex vivo

1 citations , January 2019 in “Skin Pharmacology and Physiology”

Eplerenone, a mineralocorticoid receptor antagonist, was found to promote hair growth in human hair follicles.

research Androgen Receptor Ligands: Agonists and Antagonists

2 citations , November 2017 in “Elsevier eBooks”

Different substances that activate or block the androgen receptor can affect male development and treat conditions like prostate cancer.

Androgen Receptor Antagonists Structure-Activity Relationships

research Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships

204 citations , February 2000 in “Current Medicinal Chemistry”

Antiandrogens like flutamide are effective in treating conditions like prostate cancer and hair loss, but there's a need for more potent versions. Understanding their structure can help develop better treatments.

research Neuronal model of tactile allodynia produced by spinal strychnine: effects of excitatory amino acid receptor antagonists and a μ-opiate receptor agonist

80 citations , December 1996 in “Pain”

Disruption of glycinergic circuits increases pain sensitivity, suggesting new pain treatment options.

research Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes

45 citations , August 2005 in “Bioorganic & medicinal chemistry”

New compounds with carborane showed anti-androgen effects similar to flutamide.

research CRF Receptor Antagonist Astressin-B Reverses and Prevents Alopecia in CRF Over-Expressing Mice

29 citations , February 2011 in “PloS one”

Astressin-B can reverse and prevent hair loss in stressed mice.

(1R,2S)-4-(2-Cyano-Cyclohexyl-Oxy)-2-Trifluoromethyl-Benzonitrile, A Potent Androgen Receptor Antagonist For Stimulating Hair Growth And Reducing Sebum Production

research (1R,2S)-4-(2-Cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production

14 citations , August 2007 in “Bioorganic & Medicinal Chemistry Letters”

The compound (1R,2S)-4-(2-Cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile can stimulate hair growth and reduce oil production when applied topically.

Highly Efficient Nucleophilic Addition of Alkyl Grignard Reagents to 17-Ketosteroids in the Presence of Cerium(III) Chloride: Synthesis of 17α-Propyl-17β-Hydroxy-4-Androsten-3-One, an Androgen Receptor Antagonist

research Highly efficient nucleophilic addition of alkyl Grignard reagents to 17-ketosteroids in the presence of cerium(III) chloride: Synthesis of 17α-propyl-17β-hydroxy-4-androsten-3-one, an androgen receptor antagonist

14 citations , February 1994 in “Tetrahedron Letters”

Adding cerium(III) chloride to Grignard reagents improves the making of compounds that could treat prostate issues and hair loss.

Rational Design of a Topical Androgen Receptor Antagonist for the Suppression of Sebum Production with Properties Suitable for Follicular Delivery

research Rational Design of a Topical Androgen Receptor Antagonist for the Suppression of Sebum Production with Properties Suitable for Follicular Delivery

11 citations , May 2010 in “Journal of Medicinal Chemistry”

A new compound was created in 2010 that can control oil production when applied to the skin, and its effects are completely reversible after two weeks.

4-(Alkylthio)- and 4-(Arylthio)-Benzonitrile Derivatives as Androgen Receptor Antagonists for the Topical Suppression of Sebum Production

research 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production

11 citations , March 2009 in “Bioorganic & Medicinal Chemistry Letters”

Chemicals called 4-(alkylthio)- and 4-(arylthio)-benzonitrile derivatives can potentially reduce oil production on skin, which could help treat conditions like acne and hair loss.

Preparation of 4-Aryl-2-Trifluoromethylbenzonitrile Derivatives as Androgen Receptor Antagonists for Topical Suppression of Sebum Production

research Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production

11 citations , August 2007 in “Bioorganic & Medicinal Chemistry Letters”

Scientists made a chemical (compound 4e) that can be applied on skin to reduce oil production, which can help with acne, but it might cause skin sensitivity to light.

research Oestrogen receptor antagonist and hair regrowth in dogs with hair cycle arrest (alopecia X)

11 citations , January 2007 in “Veterinary dermatology”

Fulvestrant at 10 mg/kg does not promote hair regrowth in dogs with alopecia X.

research On the Effect of Estrogen Receptor Agonists and Antagonists on the Mouse Hair Follicle Cycle

11 citations , July 1998 in “Journal of Investigative Dermatology”

β-estradiol slows hair growth in mice.

research Association between Mineralocorticoid Receptor Antagonist and Mortality in SARS-CoV-2 Patients: A Systematic Review and Meta-Analysis

10 citations , March 2022 in “Healthcare”

Mineralocorticoid receptor antagonist therapy does not significantly reduce mortality in COVID-19 patients.

research CRH receptor antagonists from Pulsatilla chinensis prevent CRH‐induced premature catagen transition in human hair follicles

9 citations , February 2020 in “Journal of Cosmetic Dermatology”

Pulsatilla chinensis compounds may help prevent stress-related hair loss.

research Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production

7 citations , April 2009 in “Bioorganic & Medicinal Chemistry Letters”

Diphenyl ethers can potentially reduce excess oil production when applied on the skin, helping treat conditions like acne.

research Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists

3 citations , May 2017 in “Bioorganic & medicinal chemistry letters”

New compounds were made that are promising for prostate cancer therapy.

research Design, synthesis and anti-tumor evaluation of novel thiohydantoin congeners as androgen receptor antagonists with in vivo study.

May 2024 in “Journal of molecular structure”

A new compound, 3a, effectively fights prostate cancer better than finasteride.

Emerging and Traditional 5-Alpha Reductase Inhibitors and Androgen Receptor Antagonists for Male Androgenetic Alopecia

research Emerging and traditional 5-α reductase inhibitors and androgen receptor antagonists for male androgenetic alopecia

April 2024 in “Expert opinion on emerging drugs”

New treatments for male hair loss are being explored to improve effectiveness and reduce side effects.

research Glucocorticoid Receptor Antagonism Improves Glucose Metabolism in a Mouse Model of Polycystic Ovary Syndrome

December 2023 in “Journal of the Endocrine Society”

Blocking glucocorticoid receptors improves glucose metabolism in a PCOS mouse model.

Repurposing of H1-Receptor Antagonists Cetirizine, Loratadine, and Fexofenadine for Systematic Analysis of ClinicalTrials.gov Trials Using Semi-Automated Processes

research Repurposing of H1-receptor antagonists (levo)cetirizine, (des)loratadine, and fexofenadine as a case study for systematic analysis of trials on clinicaltrials.gov using semi-automated processes with custom-coded software

October 2023 in “Naunyn-Schmiedeberg's Archives of Pharmacology”

Custom software found that common allergy drugs might have new uses for various conditions and could improve survival in some cancers.

Corticotropin Releasing Factor-1 Receptor Antagonism Associated With Favorable Outcomes of Male Reproductive Health Biochemical Parameters

research Corticotropin releasing factor-1 receptor antagonism associated with favorable outcomes of male reproductive health biochemical parameters

May 2023 in “Frontiers in Endocrinology”

Blocking CRF1 receptors improved male hormone levels and reduced testicular tumor size in men with a specific adrenal condition.

research Androgen Biosynthesis Inhibitors and Androgen Receptor Antagonists

January 2004 in “Elsevier eBooks”

Anti-androgen drugs can treat conditions like prostate cancer and male pattern baldness by blocking effects of testosterone and DHT.

Discovery of (2S)-N-(6-Cyano-5-(Trifluoromethyl)Pyridin-3-Yl)-3-(6-(4-Cyanophenyl)-3,6-Diazabicyclo[3.1.1]Heptan-3-Yl)-2-Hydroxy-2-Methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment

research Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment

December 2023 in “Journal of Medicinal Chemistry”

A new topical treatment for hair loss shows strong hair growth effects with low toxicity.