ArticleEndocrinology2009
Preclinical characterization of a (S)-N-(4-cyano-3-trifluoromethyl-phenyl)-3-(3-fluoro, 4-chlorophenoxy)-2-hydroxy-2-methyl-propanamide: a selective androgen receptor modulator for hormonal male contraception.
Article in Endocrinology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 58 citations in OpenAlex.
- The Potential of SARMs and Antimyostatin Agents in Addressing Lean Body Mass Loss From GLP-1 Agonists: A Literature Review.Journal of diabetes · 2025Review
- Preclinical assessment of the selective androgen receptor modulator RAD140 to increase muscle mass and bone mineral density.Physiological reports · 2025Article
- Investigations Into the Urinary Metabolite Elimination Profile of the Selective Androgen Receptor Modulator S-23 in Studies Mimicking Contaminated Product Ingestion for Doping Control Purposes.Biomedical chromatography : BMC · 2025Article
- Metabolism-Guided Selective Androgen Receptor Antagonists: Design, Synthesis, and Biological Evaluation for Activity against Enzalutamide-Resistant Prostate Cancer.Journal of medicinal chemistry · 2023Article
- Medicinal Use of Testosterone and Related Steroids Revisited.Molecules (Basel, Switzerland) · 2021Review
- Exogenous testosterone replacement therapy versus raising endogenous testosterone levels: current and future prospects.F&S reviews · 2021Article
- Selective androgen receptor modulators: the future of androgen therapy?Translational andrology and urology · 2020Review
- Overcoming resistance to anabolic SARM therapy in experimental cancer cachexia with an HDAC inhibitor.EMBO molecular medicine · 2020Article
- Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications.Sexual medicine reviews · 2019Review
- Structural and Functional Evidence for Testosterone Activation of GPRC6A in Peripheral Tissues.Molecular endocrinology (Baltimore, Md.) · 2015Article
- Nuclear receptors and their selective pharmacologic modulators.Pharmacological reviews · 2013Review
- Male contraception.Indian journal of endocrinology and metabolism · 2012Article
- Nonsteroidal androgen receptor ligands: versatile syntheses and biological data.ACS medicinal chemistry letters · 2012Article
- Alanine aminotransferase regulation by androgens in non-hepatic tissues.Pharmaceutical research · 2012Article
- Hormonal approaches to male contraception.Current opinion in urology · 2010Review
- Nonsteroidal selective androgen receptor modulators enhance female sexual motivation.The Journal of pharmacology and experimental therapeutics · 2010Article
- On the pill.Nature medicine · 2010Article
- Mechanism of action of bolandiol (19-nortestosterone-3beta,17beta-diol), a unique anabolic steroid with androgenic, estrogenic, and progestational activities.The Journal of steroid biochemistry and molecular biology · 2010Article
- Understanding and managing the suppression of spermatogenesis caused by testosterone replacement therapy (TRT) and anabolic-androgenic steroids (AAS).Therapeutic advances in urologyReview
- Update on male hormonal contraception: is the vasectomy in jeopardy?International journal of impotence researchReview
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
The pharmacologic effects of (S)-N-(4-cyano-3-trifluoromethyl-phenyl)-3-(3-fluoro, 4-chlorophenoxy)-2-hydroxy-2-methyl-propanamide (S-23) were characterized in male rats as an animal model of hormonal male contraception. S-23 showed high binding affinity (inhibitory constant = 1.7 +/- 0.2 nm) and was identified as a full agonist in vitro. In castrated male rats, the ED50 of S-23 in the prostate and levator ani muscle was 0.43 and 0.079 mg/d, respectively. In intact male rats treated for 14 d, S-23 alone suppressed LH levels by greater than 50% at doses greater than 0.1 mg/d, with corresponding decreases in the size of the prostate but increases in the size of levator ani muscle. In intact male rats treated for up to 10 wk with S-23 and estradiol benzoate (EB; necessary to maintain sexual behavior in rats), S-23 showed biphasic effects on androgenic tissues and spermatogenesis by suppressing serum concentrations of LH and FSH. EB alone showed no effect on spermatogenesis. In the EB + S-23 (0.1 mg/d) group, four of six animals showed no sperm in the testis and zero pregnancies (none of six) in mating trials. After termination of treatment, infertility was fully reversible, with a 100% pregnancy rate observed after 100 d of recovery. S-23 increased bone mineral density and lean mass but reduced fat mass in a dose-dependent manner. This is the first study to show that a selective androgen receptor modulator combined with EB is an effective and reversible regimen for hormonal male contraception in rats. The beneficial effects of S-23 on the muscle, tissue selectivity, and favorable pharmacokinetic properties make it a strong candidate for use in oral male contraception.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.