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GlossaryAntihistamines (H1 receptor antagonists)

medications that block histamine to relieve allergy symptoms

Antihistamines, also known as histamine blockers or H1 receptor antagonists, are medications that help alleviate allergy symptoms by blocking the action of histamine, a substance in the body that causes allergic reactions. They are commonly used to treat conditions such as hay fever, hives, and other allergic reactions, and can also be effective in managing symptoms of the common cold and motion sickness.

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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 Antagonists 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 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 Treatment of Female Pattern Hair Loss with the Androgen Receptor Antagonist Flutamide

30 citations, March 2011 in “Australasian Journal of Dermatology”

Flutamide improves female hair loss when other treatments fail, but may cause liver toxicity.

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 Estrogen 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 Androgens and Acne: Perspectives on Clascoterone, the First Topical Androgen Receptor Antagonist

9 citations, April 2021 in “Expert opinion on pharmacotherapy”

Clascoterone is a new, effective, and safe acne treatment without systemic side effects.

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 Cortexolone 17α-Propionate (Clascoterone) Is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro

4 citations, February 2019 in “PubMed”

Clascoterone may be an effective topical treatment for hair loss.

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.

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.

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

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.

research Emerging and Traditional 5-Alpha 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 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.

research P75 Neurotrophin Receptor Antagonist Retards Apoptosis-Driven Hair Follicle Involution (Catagen)

24 citations, January 2003 in “Journal of Investigative Dermatology”

Blocking a specific receptor slows down hair loss in mice.

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”

PF-998425 is a new, effective, and non-phototoxic treatment for skin conditions related to androgens.

research Failure of Topical Estrogen Receptor Agonists and Antagonists to Alter Murine Hair Follicle Cycling

8 citations, January 1998 in “Journal of Investigative Dermatology”

Topical estrogen treatments did not change hair growth in certain mouse strains, questioning previous findings on their role in hair growth control.

research A Topical Parathyroid Hormone/Parathyroid Hormone-Related Peptide Receptor Antagonist Stimulates Hair Growth in Mice

26 citations, December 2006 in “Endocrinology”

A cream with a specific hormone blocker increases hair growth in mice.

research 17β-Estradiol and ICI-182780 Regulate the Hair Follicle Cycle in Mice Through an Estrogen Receptor-α Pathway

71 citations, February 2000 in “Endocrinology and metabolism/American journal of physiology: endocrinology and metabolism”

Estradiol stops hair growth in mice, but an antagonist can reverse this effect.

research Androgen Receptor Modulators: A Review of Recent Patents and Reports (2012-2018)

23 citations, May 2019 in “Expert Opinion on Therapeutic Patents”

New androgen receptor modulators show promise for treating diseases like prostate cancer and muscle wasting.