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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.

research Alleviation of Mechanical Allodynia by 14,15-Epoxyeicosatrienoic Acid in a Central Poststroke Pain Model: Possible Role of Allopregnanolone and δ-Subunit-Containing Gamma-Aminobutyric Acid A Receptors

16 citations , November 2018 in “The journal of pain/Journal of pain”

14,15-EET may help reduce poststroke pain by affecting certain brain proteins.

Human Type 3 5α-Reductase Is Expressed in Peripheral Tissues at Higher Levels Than Types 1 and 2 and Its Activity Is Potently Inhibited by Finasteride and Dutasteride

research Human type 3 5α-reductase is expressed in peripheral tissues at higher levels than types 1 and 2 and its activity is potently inhibited by finasteride and dutasteride

45 citations , August 2010 in “Hormone Molecular Biology and Clinical Investigation”

Type 3 5α-reductase is more common and finasteride and dutasteride strongly inhibit it.

research 3,3-Diphenylpentane skeleton as a steroid skeleton substitute: Novel inhibitors of human 5α-reductase 1

13 citations , August 2007 in “Bioorganic & medicinal chemistry letters”

A new compound effectively inhibits human 5α-reductase 1.

research Fesoterodine: Pharmacological properties and clinical implications

5 citations , May 2018 in “European journal of pharmacology”

Fesoterodine is effective and safe for elderly patients with overactive bladder.

research Relative binding affinity of novel steroids to androgen receptors in hamster prostate

5 citations , January 2005 in “Journal of Enzyme Inhibition and Medicinal Chemistry”

New steroids were effective in blocking male hormone receptors in hamster prostates.

research Review: Adding α₁-blockers to 5α-reductase inhibitors improves lower urinary tract symptoms in men

March 2014 in “Annals of Internal Medicine”

Combining α1-blockers with 5α-reductase inhibitors improves urinary symptoms in men.

research Design, Synthesis, and Biological Characterization of Metabolically Stable Selective Androgen Receptor Modulators

129 citations , January 2004 in “Journal of medicinal chemistry”

Researchers developed new compounds that target the androgen receptor effectively with fewer side effects.

Synthesis and Structure–Activity Investigation of Iodinated Arylhydantoins and Arylthiohydantoins for Development as Androgen Receptor Radioligands

research Synthesis and structure–activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands

6 citations , November 2004 in “Bioorganic & Medicinal Chemistry Letters”

Scientists created iodinated arylhydantoins and arylthiohydantoins that could potentially be used for imaging prostate cancer. Some versions with specific side-chains showed high potential for this use.

research 52243 AH-001: An Emerging Androgen Receptor Degrader Showing Therapeutic Potential in Addressing Androgenetic Alopecia (AGA)

September 2024 in “Journal of the American Academy of Dermatology”

AH-001 could be a safer and more effective treatment for hair loss.

research Steroid 5α-Reductase Inhibitors

42 citations , May 2003 in “Mini-reviews in Medicinal Chemistry”

New steroidal compounds could be effective for treating conditions related to 5α-reductase enzyme activity.

research Topical adenosine increases the proportion of thick hair in Caucasian men with androgenetic alopecia

10 citations , October 2015 in “Journal of Dermatology”

Adenosine treatment thickens hair in Caucasian men with hair loss.

Alpha-1 Adrenergic Receptor Agonist Induced Piloerection Protects Against the Development of Traction Alopecia

research α₁-AR agonist induced piloerection protects against the development of traction alopecia

5 citations , December 2015 in “Dermatologic Therapy”

Using a certain drug on the skin can help prevent hair loss caused by pulling on the hair.

research FDA declines approval of testosterone drug for third time

2 citations , August 2013 in “The Lancet. Diabetes & endocrinology”

The FDA rejected a testosterone drug again due to safety concerns.

research Generation of comparative pharmacophoric model for steroidal 5α-reductase I and II inhibitors: A 3D-QSAR study on 6-azasteroids

13 citations , January 2015 in “Steroids”

The study created a model to help design new inhibitors for steroidal 5α-reductase enzymes.

Realizing the Therapeutic Potential of Neuroactive Steroid Modulators of the GABAA Receptor

research Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor

40 citations , December 2019 in “Neurobiology of Stress”

Neuroactive steroids show promise for treating mental and neurological disorders by targeting GABA_A receptors.

research Hormonal manipulation of benign prostatic hyperplasia

18 citations , November 2012 in “Current opinion in urology”

Finasteride and dutasteride are equally effective and safe for treating benign prostatic hyperplasia.

research Allopregnanolone is required for prepulse inhibition deficits induced by D1 dopamine receptor activation

12 citations , June 2019 in “Psychoneuroendocrinology”

Allopregnanolone is needed for certain brain processing issues caused by D1 dopamine receptor activation.

research Caffeic acid N-[3,5-bis(trifluoromethyl)phenyl] amide as a non-steroidal inhibitor for steroid 5α-reductase type 1 using a human keratinocyte cell-based assay and molecular dynamics

December 2022 in “Scientific Reports”

Compound 4 is a promising treatment for hair loss with low toxicity.

Influence of the Alkylsulfonylamino Substituent Located at the 6-Position of 2,2-Dimethylchromans Structurally Related to Cromakalim: From Potassium Channel Openers to Calcium Entry Blockers?

research Influence of the alkylsulfonylamino substituent located at the 6-position of 2,2-dimethylchromans structurally related to cromakalim: From potassium channel openers to calcium entry blockers?

6 citations , April 2014 in “European journal of medicinal chemistry”

New compounds similar to cromakalim were less effective at inhibiting insulin release but improved in solubility and one acted as a calcium entry blocker, not a potassium channel opener.

Drug Repurposing: A Promising Approach for Patients With Angina and Non-Obstructive Coronary Artery Disease (ANOCA)

research Drug repurposing—a promising approach for patients with angina but non-obstructive coronary artery disease (ANOCA)

June 2023 in “Frontiers in Cardiovascular Medicine”

Using existing drugs for new purposes could be a cost-effective way to treat chest pain and non-clogged heart arteries, with some drugs for lung blood pressure showing promise but needing more testing.