research Biological activity of novel progesterone derivatives having a bulky ester side chains at C-3
The more lipophilic the progesterone derivative, the better it binds to androgen receptors and has antiandrogenic effects.
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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.
research Monoclonal Antibody Against Prolactin Receptor: A Randomized Placebo-Controlled Study Evaluating Safety, Tolerability, and Pharmacokinetics of Repeated Subcutaneous Administrations in Postmenopausal Women
The drug BAY 1158061 is safe, well-tolerated, and shows potential for treating diseases related to prolactin.
research Implication of allopregnanolone in the antinociceptive effect of N -palmitoylethanolamide in acute or persistent pain
PEA reduces pain by increasing neurosteroid synthesis in the spinal cord.
![The Synthesis of (−)-4-Methyl-8-Chloro-Trans-1,2,3,4,4a,5,6,10b-Octahydrobenzo-[f]-Quinolin-3-One-[3-14C] (LY300502-14C) via a Circuitous Route](/images/research/73bab8dc-bdf0-45e3-8ef7-73d0d4b93cb1/small/21074.jpg)
research The synthesis of (−)-4-methyl-8-chloro-trans-1,2,3,4,4a,5,6,10b-octahydrobenzo-[f]-quinolin-3-one-[3-14C] (LY300502-14C]) via a circuitous route
Scientists made a carbon-14 labeled version of a drug with a 48% yield and over 99% purity.
research Non-competitive androgen receptor inhibition in vitro and in vivo
Two new compounds can block androgen receptor activity in different ways and may lead to new treatments for androgen-related diseases.
research P.1.g.019 RY-023, an inverse agonist at alpha5 GABAA receptors: the influence on spatial memory and spontaneous locomotor activity
RY-023, a specific drug, can improve early stage memory learning without affecting general activity in rats, but it's less effective for later learning stages and doesn't impact memory recall.
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 Experimental Assessment of 3-<i>meta</i>-Pyridine-1,2,4-Oxadiazole Deoxycholic Acid Derivative as a Prototype of 5-α-Reductase Inhibitors <i>in silico</i> and <i>in vivo</i> Models
The new compound is a promising, less toxic alternative to finasteride for treating prostate issues.
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 Novel 5α-Reductase Inhibitors: Synthesis, Structure−Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic Acids
A brominated phenoxy compound effectively inhibits a human enzyme and shows potential for clinical use.
research Synthesis and biological evaluation of esters of 16-formyl-17-methoxy-dehydroepiandrosterone derivatives as inhibitors of 5α-reductase type 2
Certain derivatives are more effective 5α-reductase type 2 inhibitors than finasteride.
research Analysis of metabolic characteristics of epristeride in zebrafish based on LC-Q-TOF MS and its potential applications in doping control
Epristeride's metabolism in zebrafish helps improve doping detection methods.
research Palmitoylethanolamide Stimulation Induces Allopregnanolone Synthesis in C6 Cells and Primary Astrocytes: Involvement of Peroxisome-Proliferator Activated Receptor-α
PEA boosts allopregnanolone production and reduces oxidative stress in brain cells.
research HPLC characterization, molecular docking, QSAR and molecular dynamics simulation of Alstonia boonei phytochemical analogs as potent 5-alpha reductase inhibitors
Alstonia boonei phytochemicals show promise as alternative treatments for BPH with fewer side effects than current drugs.
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 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 Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: Relation of their systemic activity to the formation of a common metabolite
Two non-steroidal antiandrogens, RU 58841 and RU 56187, form a common metabolite at different rates, which may influence their effects; RU 56187 could be used for prostate cancer treatment and RU 58841 for acne treatment.
research Synthesis of mimics of steroid A ring as potential enzyme inhibitors
Mimicking the steroid A-ring may help create effective enzyme inhibitors for prostate disease treatment.
research 223 Canonical and Dominant Negative Peroxisome Proliferator-Activated Receptor γ Isoforms are Differentially Expressed in Human Skin and Skin Appendages
Different types of PPARγ are found in varying amounts in human skin and its parts, which could affect how skin treatments work.
research Recent Progress and Morphological Distribution of Polydopamine-Based Biomaterials and Their Applications
Polydopamine is promising for personalized medicine and biomedical technology due to its strong adhesion and biocompatibility.
research Pharmacophore and Atom Based 3D QSAR Studies on the Novel 5-Alpha-Reductase Inhibitors
The developed model can predict effective 5-alpha-reductase enzyme inhibitors.
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 Abstract 5561: 20(S)-Protopanaxadiol-aglycone downregulates full-length and ligand-independent splice variants of androgen receptor
20(S)-Protopanaxadiol-aglycone may help prevent and treat prostate cancer by reducing androgen receptor activity.
research Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor
Neuroactive steroids show promise for treating mental and neurological disorders by targeting GABA_A receptors.
research Platelet-Rich Concentrates in the Management of Lichen Planus—A Comprehensive Review
Platelet-rich concentrates can be an alternative treatment for oral lichen planus, especially when steroids don't work.
research Molecular Interactions of New Pregnenedione Derivatives
The new progesterone derivatives effectively inhibit 5α-reductase and bind to the androgen receptor.
research Neuroactive Steroids: Functions, Mechanisms of Action and Physiologic Relevance
Allopregnanolone may enhance alcohol's effects on dopamine neurons, influencing addiction risk.
research Anxiolytic activity of progesterone in progesterone receptor knockout mice
Progesterone reduces anxiety without needing progesterone receptors.
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.