research Pantolactams as androgen receptor antagonists for the topical suppression of sebum production
Pfizer found that pantolactam-based compounds can reduce sebum (skin oil) production when applied topically.
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research Modulation of the 6-position of benzopyran derivatives and inhibitory effects on the insulin releasing process
Changing the 6-position on benzopyran molecules affects insulin release, with some compounds showing strong inhibitory effects.
![Benzo[c]quinolizin-3-ones: A Novel Class of Potent and Selective Nonsteroidal Inhibitors of Human Steroid 5α-Reductase 1](/images/research/ff6e6cbe-cb9c-4d11-87ef-671d28ffd4fa/small/15506.jpg)
research Benzo[c]quinolizin-3-ones: A Novel Class of Potent and Selective Nonsteroidal Inhibitors of Human Steroid 5α-Reductase 1
Benzo[c]quinolizin-3-ones are effective nonsteroidal inhibitors of human steroid 5α-reductase 1.
research Relative binding affinity of novel steroids to androgen receptors in hamster prostate
New steroids were effective in blocking male hormone receptors in hamster prostates.
research Growth inhibition of mouse skin tumor by serine protease inhibitor ONO-3403.
ONO-3403 effectively reduces mouse skin tumor growth without side effects.
research The 5-alpha reductase inhibitor finasteride reduces dyskinesia in a rat model of Parkinson’s disease
Finasteride reduces movement issues in Parkinson's disease rats.
research 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production
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.
research Rational Design of a Topical Androgen Receptor Antagonist for the Suppression of Sebum Production with Properties Suitable for Follicular Delivery
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.
research Enzyme Inhibitors from Gorgonians and Soft Corals
Marine compounds from gorgonians and soft corals show promise for drug development, especially for chronic disorders.
research Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes
New compounds with carborane showed anti-androgen effects similar to flutamide.
research Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development
The document concludes that adenosine receptor agonists have potential for treating various conditions, but only a few are approved due to challenges like side effects and the need for selective activation.
research Design, Synthesis, and Biological Characterization of Metabolically Stable Selective Androgen Receptor Modulators
Researchers developed new compounds that target the androgen receptor effectively with fewer side effects.
research Virtual Screening of Potential Inhibitors for SARS-CoV-2 Main Protease
The document concluded that certain compounds might strongly bind to and potentially inhibit a key SARS-CoV-2 protein, but further testing is needed.
research Allopregnanolone is required for prepulse inhibition deficits induced by D1 dopamine receptor activation
Allopregnanolone is needed for certain brain processing issues caused by D1 dopamine receptor activation.
research Monovalent antibody-conjugated lipid-polymer nanohybrids for active targeting to desmoglein 3 of keratinocytes to attenuate psoriasiform inflammation
The targeted nanohybrids effectively reduced psoriasis symptoms and improved skin health.
research EFFECTS OF FESOTERODINE, A NOVEL ANTIMUSCARINIC, ALONE AND IN COMBINATION WITH AN α-RECEPTOR BLOCKER, DOXAZOSIN, ON BLADDER FUNCTION IN OBSTRUCTED RATS
Combination therapy with fesoterodine and doxazosin improves bladder function and delays BPH progression.
research Novel modulatory effects of neurosteroids and benzodiazepines on excitatory and inhibitory neurons excitability: a multi-electrode array recording study
Neurosteroids and benzodiazepines reduce neuron excitability, with lasting effects on inhibitory neurons.
research 557 A peptide derivative with known anti-wrinkle properties was identified as potent dipeptiylpeptidase-4 inhibitor
A peptide known for reducing wrinkles also effectively inhibits an enzyme linked to skin inflammation and acne.
research In Vitroandin VivoStructure-Activity Relationships of Novel Androgen Receptor Ligands with Multiple Substituents in the B-Ring
Certain changes to the B-ring of androgen receptor ligands can increase their effectiveness for potential treatments of muscle and bone conditions.
research Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates
Selective androgen receptor modulators (SARMs) are a promising type of drug for various health conditions due to their targeted actions.
research Charting the Bromodomain BRD4: Towards the Identification of Novel Inhibitors with Molecular Similarity and Receptor Mapping
Researchers identified promising inhibitors for the BRD4 protein, including finasteride and amentoflavone.
research Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production
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 Experiences with Smo antagonist vismodegib for the treatment of locally advanced basal cell carcinoma
Vismodegib effectively treats advanced basal cell carcinoma but requires careful management of serious side effects.
research Synthetic studies toward the development of novel minoxidil analogs and conjugates with polyamines
New minoxidil compounds with better water solubility were made, but their full effects and safety need more research.
research Design, synthesis and anti-tumor evaluation of novel thiohydantoin congeners as androgen receptor antagonists with in vivo study.
A new compound, 3a, effectively fights prostate cancer better than finasteride.
research Identification of xenobiotics interfering with 5 α -reductase (SRD5A2) activity
MK-0773 is a moderate inhibitor of the SRD5A2 enzyme.
![Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968)](/images/research/d743d32f-3115-48ff-9697-2f2d56130701/small/14175.jpg)
research Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968)
The document confirms the structures of major metabolites of the CRTh2 antagonist Setipiprant and identifies minor metabolites.
research Androgen Receptor Ligands: Agonists and Antagonists
Different substances that activate or block the androgen receptor can affect male development and treat conditions like prostate cancer.
research Androgen receptor modulators: a review of recent patents and reports (2012-2018)
New androgen receptor modulators show promise for treating diseases like prostate cancer and muscle wasting.
research 2-Substituted 4-(Thio)chromenone 6-O-Sulfamates: Potent Inhibitors of Human Steroid Sulfatase
New compounds were made that block an enzyme linked to breast cancer better than existing treatments.