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.
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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 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.
research Impact of One-Week Administration of Dihydrotestosterone in Rat Anterior Pituitary Gland
Dihydrotestosterone changes some hormone-related gene expressions in rat pituitary glands but doesn't affect the estrous cycle.
research Down-regulation of Melanocortin Receptor Signaling Mediated by the Amino Terminus of Agouti Protein in XenopusMelanophores
Agouti protein affects melanocortin receptors through competitive antagonism and receptor down-regulation.
research Progesterone and allopregnanolone enhance the miniature synaptic release of glycine in the rat hypoglossal nucleus
Progesterone and allopregnanolone increase glycine release in rat brain cells.
research Three-Month Treatment With a Long-Acting Gonadotropin-Releasing Hormone Agonist of Patients With Benign Prostatic Hyperplasia: Effects on Tissue Androgen Concentration, 5α-Reductase Activity and Androgen Receptor Content*
A three-month treatment with a GnRH agonist significantly lowered androgen levels and 5α-reductase activity in men with benign prostatic hyperplasia.
research Activity of steroid 4 and derivatives 4a–4f as inhibitors of the enzyme 5α-reductase 1
Compounds 4, 4b, and 4c effectively inhibit an enzyme linked to testosterone conversion without significant toxicity.
research Inhibitory influence of agmatine on catamenial-like seizure susceptibility in progesterone withdrawn female rats
Agmatine may help reduce seizures linked to hormone changes in female rats.
research Androgenic and anti-androgenic effects of progesterone derivatives with different halogens as substituents at the C-6 position
Different halogens on progesterone derivatives can either block or mimic male hormone effects, depending on their type and amount.
research ADT-G as a promising biomarker for peripheral hyperandrogenism in adult female acne
ADT-G may be a useful indicator of increased androgen levels in women with acne and can be lowered with certain birth control pills.
![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 Changes in expression of the δ subunit of the GABAAreceptor and in receptor function induced by progesterone exposure and withdrawal
Progesterone affects GABAA receptor function by altering δ subunit levels.
research Epitestosterone—an endogenous antiandrogen?
Epitestosterone may act as a weak antiandrogen and can inhibit an enzyme involved in testosterone metabolism.
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 BIOLOGICAL ACTIVITY OF ANTIANDROGENS
Antiandrogens may help treat conditions like excessive hair growth, prostate tumors, male baldness, and acne by blocking male hormone effects.
research Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines
New steroidal compounds moderately block an enzyme related to testosterone conversion, less effectively than finasteride.
![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 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.
research Mechanisms that regulate androgen receptor transcriptional activity
DHT enhances androgen receptor activity more than testosterone, and MAGE-11 influences this activity through specific interactions.
research Neuroactive steroids inhibit spinal reflex potentiation by selectively enhancing specific spinal GABAA receptor subtypes
Progesterone reduces spinal reflex activity by increasing certain GABA(A) receptor subtypes.
research 2‐Deoxy‐d ‐glucose enhances tonic inhibition through the neurosteroid‐mediated activation of extrasynaptic GABA A receptors
2-DG reduces seizures by enhancing brain inhibition through specific receptor activation.
research Inhibiting Biosynthesis and/or Metabolism of Progestins in the Ventral Tegmental Area Attenuates Lordosis of Rats in Behavioural Oestrus
Blocking certain brain processes reduces mating behavior in female rats.
research Neuroactive Steroids: Functions, Mechanisms of Action and Physiologic Relevance
Allopregnanolone may enhance alcohol's effects on dopamine neurons, influencing addiction risk.
research Membrane androgen receptors may mediate androgen reinforcement
Androgen self-administration might be controlled by membrane receptors, not nuclear ones.
research Antihormonal properties of some new A-homo-B, 19-dinor steroids of the androstane series
New A-homo-B, 19-dinor steroids showed strong antiandrogenic activity without affecting the enzyme 5α-reductase or androgen receptor binding.
research Molecular interactions of progesterone derivatives with 5α-reductase types 1 and 2 and androgen receptors
Certain progesterone derivatives can inhibit enzymes and reduce androgenic activity, potentially affecting prostate growth.
research Kinetic analysis of LY320236: competitive inhibitor of type I and non-competitive inhibitor of type II human steroid 5α-reductase
LY320236 is a strong blocker of two enzymes that change testosterone into dihydrotestosterone and might help treat conditions related to male hormones.
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 Thyroid receptor β: A promising target for developing novel anti-androgenetic alopecia drugs
Thyroid receptor β can help develop new drugs to treat hair loss.