Pantolactams as Androgen Receptor Antagonists for the Topical Suppression of Sebum Production

September 2011 in “ Bioorganic & Medicinal Chemistry Letters ”

Karen Elaine Sexton, Stephen Barrett, Katy L. Bridgwood, Matthew Carroll, Danielle Dettling, Daniel K. Du, Stephen A. Fakhoury, Victor Fedij, Lain-Yen Hu, Catherine R. Kostlan, David Pocalyko, N. Raheja, Yvonne E. Smith, Veerabahu Shanmugasundaram, Kimberly Jane Wade

pantolactams androgen receptor antagonists sebum production topical application wax esters Hamster Ear Model (+)-isomer AR antagonists

Studysummary This study identified pantolactam based compounds as effective topical antagonists of the androgen receptor, reducing sebum components in a hamster model.

Automatically generated from the study's abstract, not written by a person, and not a review of the full paper. Not medical advice or a treatment recommendation. Read the original study, and consult a qualified healthcare professional before changing treatment. Full disclaimer

View this study on sciencedirect.com →

Discuss this study in the Community →

Research cited in this study

9 / 9 results

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”

This study introduced a novel nonsteroidal androgen receptor antagonist that effectively controls sebum production in the golden Syrian hamster ear model through targeted follicular delivery.

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.

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”

This study reports that 4-(alkylthio)- and 4-(arylthio)-benzonitriles showed moderate sebum reduction as androgen receptor antagonists when applied topically in a validated animal model.

research Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications

23 citations , October 2008 in “Journal of medicinal chemistry”

This study suggests that PF-0998425 is an effective androgen receptor antagonist for sebum control and androgenetic alopecia with rapid metabolism reducing the risk of systemic side effects.

(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”

This study reported that the compound (1R, 2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile effectively stimulated hair growth in mice and reduced sebum production in hamsters.

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”

This study found that among the tested analogs, compound 4e was the most effective in inhibiting wax esters in vivo in the Golden Syrian hamster ear model.

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”

This study found that a specific amino-pyridine compound showed potent androgen receptor antagonist activity, stimulating hair growth in mice and reducing sebum production in a hamster model.

research Importance of Sebaceous Glands in Cutaneous Penetration of an Antiandrogen: Target Effect of Liposomes

62 citations , May 1997 in “Journal of Pharmaceutical Sciences”

This study concluded that sebaceous glands are the main pathway for the antiandrogen RU 58841 to permeate the skin, with liposomes enhancing localization in these glands.

research Treatment of Androgenic Disorders in Women: Acne, Hirsutism, and Alopecia

19 citations , July 1990 in “Cleveland Clinic journal of medicine”

This article reviews endocrine therapies for androgen excess disorders, emphasizing spironolactone, estrogen, and dexamethasone as effective treatments; it reports no new clinical results.