research Direct Vasodilators and Sympatholytic Agents
Direct vasodilators and sympatholytic agents are still useful for certain conditions despite being less common due to side effects and newer drugs.
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30-60 / 1000+ results![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 Identification of xenobiotics interfering with 5 α -reductase (SRD5A2) activity
MK-0773 is a moderate inhibitor of the SRD5A2 enzyme.
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 Towards the Development of AgoKirs: New Pharmacological Activators to Study Kir2.x Channel and Target Cardiac Disease
New compounds may help treat heart disease by activating specific potassium channels.
research Anti-invasive effects of minoxidil on human breast cancer cells: combination with ranolazine
Minoxidil and ranolazine together can reduce the spread of certain breast cancer cells.
research Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications
PF-998425 is a new, effective, and non-phototoxic treatment for skin conditions related to androgens.
research Minoxidil prevents 3,4-methylenedioxymethamphetamine-induced serotonin depletions: role of mitochondrial ATP-sensitive potassium channels, Akt and ERK
Minoxidil prevents serotonin loss from MDMA by affecting potassium channels and increasing Akt phosphorylation.
research Drug repurposing of cyclin-dependent kinase inhibitors for neutrophilic acute respiratory distress syndrome and psoriasis
CDK inhibitors may help treat ARDS and psoriasis but need more testing for safety and effectiveness.
research Anti-anginal and beta-adrenoceptor blocking drugs
Beta-blockers and anti-anginal medications have various side effects and interactions that require careful monitoring and individualized treatment.
research Structural characterization and dissolution profile of mycophenolic acid cocrystals
The MPA-ISO cocrystal improved solubility and dissolution rate, while the others did not.
research Profound bradycardia after addition of diltiazem to a beta blocker.
Adding diltiazem to a beta blocker can cause dangerously slow heart rates.
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 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 The action of diazoxide and minoxidil sulphate on rat blood vessels: a comparison with cromakalim
Diazoxide, minoxidil sulphate, and cromakalim relax rat blood vessels by opening K+ channels, with some differences in their actions.
research The Bis(1,2,3,4-tetrahydroisoquinoline) Alkaloids Cepharanthine and Berbamine Are Ligands of SK Channels
Cepharanthine and berbamine may affect SK channels, influencing their therapeutic effects.
research Benzothiazepines, diltiazem and JTV-519, exert an anxiolytic-like effect via neurosteroid biosynthesis in mice
Benzothiazepines like diltiazem reduce anxiety in mice by making neurosteroids.
research Potassium channel openers: pharmacological and clinical aspects
Potassium channel openers could help treat cardiovascular diseases and asthma but require better targeting to specific tissues for effective use.
research Hormone receptor positive, HER2 negative metastatic breast cancer: Impact of CDK4/6 inhibitors on the current treatment paradigm
CDK4/6 inhibitors have improved treatment outcomes for certain advanced breast cancer patients.
research Inhibitory effect of M50054, a novel inhibitor of apoptosis, on anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia
M50054 may help treat hepatitis and hair loss from chemotherapy.
![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.
![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 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 Potassium channel openers: therapeutic potential in cardiology and medicine
Potassium channel openers show promise for treating heart disease and other conditions, but more research is needed to fully understand their effects and safety.
research Intracellular Calcium Mobilization in Response to Ion Channel Regulators via a Calcium-Induced Calcium Release Mechanism
Certain drugs increase calcium levels in cancer cells by triggering internal calcium release.
research Inhibition of 5α-reductase attenuates behavioral effects of D1-, but not D2-like receptor agonists in C57BL/6 mice
Finasteride reduces certain behaviors caused by D1-like receptor agonists but not by D2-like receptor agonists in mice.
research Structural Requirements of Minoxidil Analogs for Enhancing Lysyl Hydroxylase Inhibitory Activity
Minoxidil analogs can be improved for hair growth inhibition by modifying specific parts of their structure.
research Mechanism of action of minoxidil sulfate-induced vasodilation: a role for increased K+ permeability.
Minoxidil sulfate relaxes muscle by increasing potassium flow, making it a unique muscle relaxer.
research 576 INTASYL PH-762: Intratumoral immunotherapy targeting PD-1
PH-762 shows promise in treating skin cancer by effectively targeting and silencing PD-1 in tumors with minimal side effects.
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.