Purinergic antagonists are a class of drugs that block the activity of purinergic receptors, which are proteins found on the surface of cells that respond to purines such as ATP and adenosine. These receptors play important roles in various physiological processes, including neurotransmission, inflammation, and cellular signaling.
Suramin är ett medically used antiparasitärt läkemedel, som primärt används för behandling av sjukdomen "Trypanosomiasis" (African sleeping sickness), som orsakas av parasiten Trypanosoma brucei. Suramin fungerar genom att störa parasitens metabolism och dess förmåga att replikera. Det bör noteras att användning av suramin är begränsad på grund av potentialen för allvarliga biverkningar, och det ska endast preskrivas och användas under en läkares övervakning.
Adenosin-5´-(tetravätetrifosfat). En adeninnukleotid innehållande tre fosfatgrupper som förestrats till en sockerdel. Adenosintrifosfat har en betydande roll i ämnesomsättningen och som neurotransmitt or.
Purinergic receivers är en typ av receptor som binder signalmolekyler kända som puriner, inklusive adenosin och ATP (Adenosintrifosfat). Dessa receptorer spelar en viktig roll i regleringen av olika cellulära processer såsom excitation, transmission av nervimpulser, immunresponser och celldöd. Purinergic receivers delas in i två huvudgrupper: P1-receptorer som primarily binds adenosin och P2-receptorer som binder ATP och dess nedbrytningsprodukter.
P2-receptorer är en typ av receptorer som binder adenosintrifosfat (ATP) och andra nukleotider. De är G-proteinkopplade receptorer och delas in i två undergrupper, P2Y-receptorer och P2X-receptorer. P2Y-receptorerna är metaboliskt sensitiva och aktiveras av nukleotider som ATP, ADP, UTP och UDP, medan P2X-receptorerna är jonkanaler som aktiveras av ATP. P2-receptorer spelar en viktig roll i regleringen av flera fysiologiska processer, såsom smärta, inflammation, blodtryck och excitation-kontraktionskoppling i hjärtat och skelettmusklerna.
Purinergic agonists are chemical substances that bind and activate purinergic receptors, which are a type of cell surface receptor found in many organs and tissues throughout the body. These receptors are involved in a variety of physiological processes, including neurotransmission, inflammation, and cellular signaling.
Purinergic P2X receptors are a type of ligand-gated ion channel that are activated by the binding of extracellular ATP (adenosine triphosphate) and other purinerglic agonists. These receptors play important roles in various physiological processes, including neurotransmission, pain perception, and immune response. Upon activation, P2X receptors allow for the flow of cations such as calcium, sodium, and potassium across the cell membrane, which can lead to changes in membrane potential and downstream signaling events. There are seven subtypes of P2X receptors (P2X1-7) that differ in their pharmacological properties, distribution, and functions.
Purinergic P2X7 receptor (P2X7R) är ett transmembrant protein som fungerar som en jonkanal för kationer och utgör en del av signalsystemet som kontrollerar cellers aktivitet och kommunikation. Det aktiveras främst av extracellulära ATP (adenosintrifosfat) och är involverat i en rad fysiologiska processer såsom immunresponser, inflammation och smärta. Överaktivering eller störningar i P2X7R har också visats vara relaterade till patofysiologiska tillstånd som neurodegenerativa sjukdomar, cancer och autoimmuna sjukdomar.
Purinergic P2Y2 receptors are a type of G-protein coupled receptor that bind to and are activated by extracellular nucleotides such as ATP and UTP. They play a role in various physiological processes, including regulation of inflammation, wound healing, and fluid secretion. These receptors have been found to be widely expressed in various tissues, including the respiratory, gastrointestinal, and urinary tracts, as well as the skin and central nervous system. They are also known to be involved in the development of certain diseases such as cancer and fibrosis.
Purinergic P2Y1 receptors are a type of G protein-coupled receptor that bind to and are activated by extracellular nucleotides such as adenosine triphosphate (ATP) and related compounds. These receptors play important roles in various physiological processes, including platelet activation, smooth muscle contraction, and neurotransmission. Specifically, the P2Y1 receptor is known to mediate platelet aggregation and vascular smooth muscle contraction, among other functions. It should be noted that the function of these receptors can vary depending on the cell type and context in which they are expressed.
'Purinergic P2X Receptor Antagonists' are a class of pharmaceutical compounds that block the activation of P2X receptors, which are ligand-gated ion channels found in various tissues throughout the body. These receptors are activated by purinergic signaling molecules such as ATP and ADP, and play important roles in a variety of physiological processes, including neurotransmission, inflammation, and pain perception.
'Purinergic P2 receptor antagonists' are a class of pharmaceutical compounds that block the activity of P2 receptors, which are proteins on the surface of cells that bind purinergic signaling molecules such as ATP and ADP. These receptors play important roles in various physiological processes, including neurotransmission, inflammation, and cardiovascular function. By blocking the activity of these receptors, P2 receptor antagonists can be used to treat a variety of medical conditions, such as chronic pain, inflammatory diseases, and neurological disorders.
Purinergic P2X3 receptors are a type of ligand-gated ion channel that is activated by the binding of adenosine triphosphate (ATP) and related nucleotides. These receptors are widely expressed in the nervous system, including sensory neurons, where they play important roles in pain transmission and modulation. P2X3 receptors are selectively activated by the binding of extracellular ATP, which leads to the opening of the ion channel and an influx of cations such as calcium and sodium ions. This ion flux can trigger a variety of cellular responses, including the initiation or enhancement of pain signals. P2X3 receptors have been implicated in various pain conditions, making them a potential target for the development of new analgesic drugs.
'Purinergic P2 receptor agonists' are substances that bind and activate purinergic P2 receptors, which are a type of cell surface receptor that respond to extracellular nucleotides such as ATP and ADP. These agents are used in medical research and therapy to stimulate various physiological responses, including smooth muscle contraction, platelet aggregation, and neurotransmission, depending on the specific P2 receptor subtype they target.
Purinergic P2X4 receptors are a type of ionotropic receptor that are activated by the binding of adenosine triphosphate (ATP) and related purines. These receptors are widely expressed in various tissues, including the central and peripheral nervous systems, immune cells, and smooth muscle cells. The P2X4 receptor is a trimeric protein composed of three subunits that form a ion channel permeable to cations such as calcium, sodium, and potassium. Activation of P2X4 receptors leads to the opening of the ion channel, resulting in the influx of cations and an increase in intracellular calcium concentration. This can lead to a variety of cellular responses, including neurotransmitter release, regulation of immune function, and modulation of pain perception.
Purinergic P2X receptor agonists are substances that bind and activate P2X receptors, which are ligand-gated ion channels found in the cell membrane of various cell types, including excitable cells such as neurons and smooth muscle cells. These receptors are activated by purinergic signaling molecules called ATP (adenosine triphosphate) and its analogs. Activation of P2X receptors leads to the opening of the ion channel, allowing the flow of cations such as calcium, sodium, and potassium across the cell membrane, which can subsequently trigger a range of physiological responses.
Purinergic P2Y receptors are a subtype of membrane receptors that bind extracellular purines and pyrimidines, such as ATP, ADP, UTP, and UDP. These receptors play important roles in various physiological processes, including neurotransmission, inflammation, and cell proliferation.
Purinergic P2X2 receptors are a type of ligand-gated ion channel that is activated by the binding of adenosine diphosphate (ADP) and adenosine triphosphate (ATP). These receptors play a role in various physiological processes, including neurotransmission, pain perception, and smooth muscle contraction. The P2X2 receptor is specifically known for its involvement in the transmission of sensory information in the peripheral nervous system. It is widely expressed in both the central and peripheral nervous systems, as well as in non-neuronal tissues such as the lungs, kidneys, and blood vessels. Once activated, P2X2 receptors allow the flow of cations (such as calcium, sodium, and potassium) across the cell membrane, which can lead to changes in membrane potential and the initiation of downstream signaling pathways.
'Purinergic P2Y Receptor Agonists' are substances that bind and activate purinergic P2Y receptors, which are a type of G-protein coupled receptors found on the cell membrane. These receptors are activated by endogenous nucleotides such as ATP (Adenosine triphosphate), ADP (Adenosine diphosphate), UTP (Uridine triphosphate) and UDP (Uridine diphosphate). Activation of P2Y receptors plays a role in various physiological processes, including platelet aggregation, smooth muscle contraction, neurotransmission, and inflammation. Synthetic P2Y receptor agonists are used in research and therapeutics to understand the function of these receptors and to develop potential treatments for various diseases.
Purinergic P2X5 receptors are a type of ionotropic receptor, which are membrane proteins that form ion channels. These receptors are activated by the binding of extracellular adenosine triphosphate (ATP) and are found in various tissues throughout the body, including the nervous system.
Uridintrifosfat (UTP) är ett nukleotid som består av en pentos sugar (ribos) kovalent bundet till en uracil bas och tre fosfatgrupper. Det är en viktig prekursor i celldelningen, cellandningen och syntesen av RNA. UTP kan också fungera som energibärare inom cellen.
Pyridoxalfosfat (PLP) är den aktiverade formen av vitamin B6 och fungerar som en koenzym i flera biologiska reaktioner, särskilt inom aminosyremetabolismen. Det hjälper till att katalysera dekarationen och transaminationen av aminosyror, neurotransmittorproduktion och hemgruppsyntes. Pyridoxalfosfat är väsentligt för cellers överlevnad och normal funktion i kroppen.
P1-receptorer är en typ av adenosinreceptorer, som är G-proteinkopplade receptorer som binder till neurotransmittorn adenosin i centrala nervsystemet och hjärtat. Dessa receptorer delas in i tre undergrupper: P1, P2X och P2Y. I detta fall refererar "P1" specifikt till de adenosinreceptorer som styrs av de subtyparna A1, A2A, A2B och A3. Dessa receptorer spelar en viktig roll i diverse fysiologiska processer, såsom sömnreglering, smärtkänslighet, hjärtfunktion och immunrespons.
Ett kalciumaktiverat enzym som katalyserar hydrolys av ATP till AMP och ortofosfat. Det verkar också på ADP och andra nukleosidtrifosfater och -difosfater. EC 3.6.1.5.
Purinergic P2X1 receptors are a type of ligand-gated ion channel that is activated by the binding of ATP (adenosine triphosphate), a signaling molecule found in many tissues throughout the body. These receptors play an important role in various physiological processes, including neurotransmission, smooth muscle contraction, and immune response.
Purinergic agents are substances that act on purinergic receptors, which are a type of cell surface receptor that bind to purines such as adenosine and ATP (adenosine triphosphate). These receptors play important roles in many physiological processes, including neurotransmission, cardiovascular function, and immune response. Purinergic agents can be either agonists or antagonists of these receptors, depending on whether they activate or block the receptor's activity. Examples of purinergic agents include drugs such as theophylline (a non-selective adenosine receptor antagonist) and dipyridamole (an adenosine uptake inhibitor), as well as naturally occurring compounds such as ATP and adenosine.
'Purinergic P1 receptor antagonists' are a class of pharmaceutical compounds that block the activity of purinergic P1 receptors, which are a type of G protein-coupled receptor found in many tissues throughout the body. These receptors are activated by the endogenous signaling molecules adenosine and related nucleotides, and play important roles in regulating a variety of physiological processes, including cardiovascular function, neurotransmission, and immune response.
Kemiska ämnen som hämmar de endokrina körtlarnas funktioner, biosyntesen av de hormoner de utsöndrar, eller blockerar hormonernas specifika verkan.
Purinergic P2Y12 receptors are a type of G protein-coupled receptor that bind to adenosine diphosphate (ADP) and play a crucial role in regulating platelet activation and aggregation, which are essential processes for hemostasis and thrombosis. These receptors are primarily expressed on the surface of platelets and megakaryocytes and are the target of antiplatelet drugs such as clopidogrel, prasugrel, and ticagrelor, which are used to prevent thrombotic events in patients with acute coronary syndrome or those undergoing percutaneous coronary intervention.
Läkemedel som binder till, men inte aktiverar receptorer för excitatoriska aminosyror, varvid agonistverkan blockeras.
"Sprague-Dawley råtta" är en typ av albino släthårig laboratorieråtta som vanligtvis används inom forskning på grund av deras förutsägbara och reproducerbara genetiska, fysiologiska och beteendemönster. De utvecklades under 1920-talet i USA av biologerna Robert Sprague och Harold Dawley och är idag en av de mest använda råttorna inom forskning världen över.
Läkemedel som binder till, men inte aktiverar dopaminreceptorer, varvid verkan av dopamin eller exogena stimulerare blockeras. Många läkemedel för behandling av psykotiska tillstånd är dopaminantagonister, även om deras terapeutiska effekt kanske mer beror på en långsam anpassning i hjärnan än på en omedelbar blockering av dopaminreceptorer. Dopaminantagonister har haft flera andra kliniska användningsområden, bl a som medel mot kräkningar och illamående, för behandling av Tourettes syndrom och mot hicka.
Purinergic P2Y receptor antagonists are a class of pharmaceutical compounds that block the activity of P2Y purinergic receptors, which are proteins on the surface of cells that bind to and respond to extracellular nucleotides such as ATP and ADP. These receptors play important roles in various physiological processes, including platelet aggregation, smooth muscle contraction, and neurotransmission. By blocking the activity of these receptors, P2Y receptor antagonists can be used to treat a variety of medical conditions, such as thrombosis, hypertension, and chronic pain.
Neurokinin-1 (NK-1) receptor antagonists are a class of drugs that block the action of substance P, a neuropeptide involved in pain signaling and inflammation. These drugs work by binding to NK-1 receptors found on nerve cells, preventing substance P from activating them and transmitting pain signals. NK-1 receptor antagonists have been studied for their potential use in treating various conditions associated with pain and inflammation, including migraines, depression, and irritable bowel syndrome. Examples of NK-1 receptor antagonists include aprepitant, fosaprepitant, and rolapitant.
Förhållandet mellan läkemedelsdos och kroppens/organismens gensvar på medlet.
Preparat som binds till, men inte aktiverar, kolinerga muskarinreceptorer, och därmed blockerar verkan av endogent acetylkolin eller exogena stimulanter. Muskarinantagonister har utbredd verkan, bl a på iris och ögats ciliarmuskel, hjärta och blodkärl, andningsvägarnas sekretion, spottkörtlarna, mag-tarmsystemet, tarmrörligheten, urinblåsespänningen och det centrala nervsystemet. Antagonister med förmåga att särskilja mellan olika muskarinreceptortyper och tillåta bättre kontroll av perifera och centrala verkningar håller på att utvecklas.
A narkotikablockerare, eller opioidantagonist, är ett läkemedel som blockerar effekterna av opiater (narkotika) på centrala nervsystemet, såsom smärtlindring, andningsdepression och eufori. Dessa mediciner används för att behandla opiatöverdos och beroende, samt för att diagnostisera och behandla opiatförgiftning. Exempel på narkotikablockerare är naloxon och naltrexon.
Läkemedel som selektivt binder till, men inte aktiverar histamin H2-receptorer, och därmed blockerar verkan av histamin. Deras viktigaste kliniska effekt är att de hämmar syrautsöndring vid behandling av magsår. De kan även påverka glatt muskulatur. Vissa av medlen i denna klass har kraftig effekt på det centrala nervsystemet, men dessa verkningsmekanismer är inte klarlagda.