research Different Ligands of the TRPV3 Cation Channel Cause Distinct Conformational Changes as Revealed by Intrinsic Tryptophan Fluorescence Quenching
Different ligands change the shape of the TRPV3 ion channel in unique ways.
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research ς1Receptor-Related Neuroactive Steroids Modulate Cocaine-Induced Reward
Neuroactive steroids affect cocaine's rewarding effects through the ς1 receptor.
research Design, Synthesis and Anxiolytic Activity Evaluation of N-Acyltryptophanyl- Containing Dipeptides, Potential TSPO Ligands#
The compound GD-23 may reduce anxiety like diazepam by targeting the TSPO receptor.
research Ligand Based 3D-QSAR Study on a Series of Steroidal Human 5α-Reductase Inhibitors
research Synthesis and structure–activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands
The nature of the side chain in RU 58841 derivatives greatly affects its AR affinity, with the N-(iodopropenyl) derivative 13 showing the highest AR binding affinity, suggesting its potential for developing high-affinity radioiodinated AR radioligands.
![Synthesis, Biological Evaluation, and Molecular Docking of 4-Amino-2H-benzo[h]chromen-2-one Analogs Containing the Piperazine Moiety](/images/research/2ecf4eed-7dbe-4f1a-83db-739625546cdd/small/31808.jpg)
research Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety
Analog 23 is a promising compound for prostate cancer treatment.
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.
![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 Therapeutic anti-inflammatory potential of formyl-peptide receptor agonists
Formyl-peptide receptor agonists could be new anti-inflammatory drugs.
research Androgen binding profiles of two distinct nuclear androgen receptors in Atlantic croaker (Micropogonias undulatus)
Different types of androgens bind differently to two receptors, AR1 and AR2, in Atlantic croaker's brain and ovarian tissues, suggesting these receptors may control different androgen actions in fish.
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 Synthesis and structure–activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands
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 263 (-)-cannabidiol differentially influences hair growth
CBD can either promote or inhibit hair growth depending on the concentration used.
research Involvement of neurosteroids in the anxiolytic-like effects of AC-5216 in mice
AC-5216 reduces anxiety in mice through neurosteroids affecting GABAA receptors.
![Effect of C-Ring Modifications in Benzo[c]quinolizin-3-ones, New Selective Inhibitors of Human 5α-Reductase 1](/images/research/c687900f-ea40-4de1-8f0b-a5b818951b1c/small/15452.jpg)
research Effect of C-ring modifications in benzo[c]quinolizin-3-ones, new selective inhibitors of human 5α-reductase 1
Changing the C-ring structure in certain compounds can make them better at blocking a specific human enzyme.
research Modulating mechanosensory afferent excitability by an atypical mG luR
A compound named ZCZ90 can increase muscle spindle firing, potentially helping treat muscle spasms and hypertension.
research Effects of transient receptor potential (TRP) channel agonists and antagonists on slowly adapting type II mechanoreceptors in the rat sinus hair follicle
TRPA1 and TRPV1 channels don't affect mechanotransduction in rat sinus hair follicles.
research Sigma 1 receptor-related neuroactive steroids modulate cocaine-induced reward.
Neuroactive steroids affect cocaine's rewarding effects through the sigma1 receptor.
research Pharmacophore Modeling and Three Dimensional Database Searching for Drug Design Using Catalyst: Recent Advances
The document concludes that Catalyst software is effective for drug design, identifying potent compounds for various medical conditions.
research Quantification of the Vitamin D Receptor−Coregulator Interaction
Vitamin D receptor binds similarly to natural and synthetic ligands, affecting gene regulation.
research Application of histamine receptors H2R, H3R and H4R, but not H1R, in dermatology
Certain histamine receptors (H2R, H3R, H4R) have unique roles in treating skin diseases, with H2R helping with chronic urticaria and other conditions, H3R providing pain relief and allergy benefits, and H4R reducing inflammation and itchiness.
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 Activation of the Human Transient Receptor Potential Vanilloid Subtype 1 by Essential Oils
Certain essential oils can activate a human skin receptor, potentially helping with skin disorders.
research Crystallization and preliminary X-ray analysis of the human androgen receptor ligand-binding domain with a coactivator-like peptide and selective androgen receptor modulators
Scientists successfully created and analyzed the structure of a part of the human androgen receptor with specific modulators and a peptide to understand how it binds differently in various tissues.
research Non-canonical dimerization of the androgen receptor and other nuclear receptors: implications for human disease
Mutations in certain receptors can cause diseases and offer new treatment options.
![Benzo[c]quinolizin-3-ones Theoretical Investigation: SAR Analysis and Application to Untested Compounds](/images/research/6712367a-949f-47c7-a756-2bfe6316fc69/small/15331.jpg)
research Benzo[c]quinolizin-3-ones Theoretical Investigation: SAR Analysis and Application to Nontested Compounds
The research found a link between certain molecular features and the biological activity of BC3, which can help identify or create new active compounds.
research Computational Evaluation of Dibenzo Compounds as Potential Dual Inhibitors of Androgen Receptor and 5α-Reductase
Some dibenzo compounds might help treat cancer with fewer side effects.
research TRPV1 Function in Health and Disease
TRPV1 is involved in pain, various body functions, and diseases, but targeting it for treatment is challenging.
research 3,3-Diphenylpentane skeleton as a steroid skeleton substitute: Novel inhibitors of human 5α-reductase 1
A new compound effectively inhibits human 5α-reductase 1.
research Synthesis of novel andostane-N-cyclohexyl-17-carboxamides, and their effect on the 5α-reductase isoform 2, the androgen receptor, and androgen-dependent glands
New compounds were made and tested, with compound 6 showing potential for treating prostate-related diseases.