Adrenergic Receptors

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  1. Arrestin-3 Modulator

    Arrestin-3 modulator-1 is a selective modulator that interacts with arrestin-3 at the interdomain interface. This compound enhances the recruitment of arrestin-3 to phosphorylation-deficient β2-adrenergic receptors, as evidenced by increased Förster resonance energy transfer (FRET) levels in cellular assays. Arrestin-3 modulator-1 is valuable for studying congenital disorders such as retinal degeneration, hyperthyroidism, and obesity, offering insights into the molecular mechanisms underlying these conditions.
  2. Adrenergic Receptor Activator

    (R)-Midodrine hydrochloride is an adrenergic receptor activator that primarily functions as a vasopressor. It demonstrates significant peripheral alpha(1)-adrenoreceptor agonistic activity, leading to arterial and venous vasoconstriction. This compound is particularly useful in the study and management of symptomatic postural hypotension and related cardiovascular research applications.
  3. β2 Adrenergic Receptor agonist

    Vilanterol acetate is a long-acting agonist of the β2 adrenergic receptor. It exhibits pEC50 values of 9.4 for β2-AR, and lower affinities for β1-AR and β3-AR at 6.4 and 6.1, respectively. By selectively activating airway β2 adrenergic receptors, Vilanterol acetate enhances cAMP levels, leading to relaxation of bronchial smooth muscle. This compound is valuable for research in asthma and related respiratory disorders.
  4. 5-HT Receptor Inhibitor

    Metrenperone is a selective inhibitor of the 5-HT2 receptor, exhibiting significant antagonist activity on α1 and α2 adrenergic receptors, as well as anti-H1 and anti-dopaminergic effects. It demonstrates notable biological activities, including the reduction of blood pressure, enhancement of bradycardia during peripheral ischemia, and inhibition of serotonin-induced platelet aggregation. Additionally, Metrenperone antagonizes serotonin-mediated vasoconstriction and is involved in promoting the repair of acutely damaged collagen tissue, making it valuable for various research applications in cardiovascular and vascular biology.
  5. M3 mAChR Antagonist

    p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes.
  6. α1-Adrenergic Receptor Antagonist

    A55453 is a potent α1-adrenergic receptor antagonist, structurally related to prazosin. It demonstrates high affinity for α1-adrenergic receptors and is utilized as a valuable probe in research applications focusing on cardiovascular function and pharmacological studies. The use of 125I-A55453 allows for enhanced detection and analysis of receptor interactions in various experimental settings.
  7. β3/β1 Adrenergic Receptor Agonist

    BMS-196085 is a potent and selective full agonist targeting the human β3 adrenergic receptor, exhibiting a Ki value of 21 nM. Additionally, it demonstrates partial agonist activity at the β1 receptor. This compound is valuable for research applications related to obesity and type-II diabetes, offering insights into adrenergic receptor modulation for therapeutic strategies.
  8. Antiprion Agent

    Chloroguanabenz acetate is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz. It effectively inhibits prion formation in both yeast and mammalian in vitro assays. Additionally, Chloroguanabenz acetate has been shown to decrease levels of the truncated Huntingtin derivative Htt48 in HEK293T cells, making it a valuable tool in the investigation of Huntington's disease.
  9. Stable Isotope

    Betaxolol-d7 hydrochloride is a deuterium-labeled analog of Betaxolol hydrochloride, functioning primarily as a selective beta-1 adrenergic receptor blocker. This stable isotope is instrumental in pharmacokinetic studies and metabolic investigations, particularly in the context of hypertension and glaucoma research. Its unique labeling enables precise tracking and quantification in various biological assays, facilitating advanced research into cardiovascular and ocular conditions.
  10. Stable Isotope

    Ractopamine-d6 is a deuterium-labeled analogue of Ractopamine, a potent β-adrenergic receptor (βAR) agonist with a Kd of approximately 25 nM for both pig β1AR and β2AR. This stable isotope enables detailed studies of protein metabolism and is instrumental in research focused on enhancing lean tissue growth and improving production efficiency in swine. Its application is crucial for understanding the biochemical pathways influenced by β-adrenergic signaling in agricultural and animal health settings.
  11. Adrenergic Receptor Inhibitor

    Bamosiran is a small interfering RNA that specifically targets the β-adrenergic receptor 2. This compound is recognized for its ability to significantly reduce intraocular pressure, making it valuable in the study of ocular conditions. Its role as an adrenergic receptor inhibitor aids in investigating therapeutic strategies for glaucoma and other eye disorders.
  12. β2-adrenergic Receptor Agonist

    β2AR agonist 3 is a selective agonist of the β2-adrenergic receptor, involved in mediating various physiological responses. This compound has demonstrated potential in the modulation of metabolic pathways and holds promise for research in type 2 diabetes. Its application may facilitate investigations into β2AR-related mechanisms and therapeutic approaches in metabolic disorders.
  13. α1 Adrenergic Receptors Antagonist

    Doxazosin-d8 is a deuterium-labeled derivative of Doxazosin, a selective antagonist of postsynaptic α1 adrenergic receptors. This compound exhibits potent inhibitory effects on α1 receptor-mediated pathways, making it valuable for studying cardiovascular function and related pharmacological effects. Doxazosin-d8 can be utilized in research applications focusing on hypertension, benign prostatic hyperplasia, and other conditions influenced by α1 adrenergic signaling.
  14. Alpha 2-adrenergic Receptor Antagonist

    Vatinoxan is an alpha 2-adrenergic receptor antagonist that selectively inhibits α2-adrenergic receptors, primarily affecting the peripheral nervous system due to limited central nervous system penetration. By binding to these receptors, Vatinoxan mitigates cardiovascular responses typically induced by α2-adrenergic agonists. This compound is valuable in research related to cardiovascular physiology, sedation, and analgesia.
  15. β-Adrenergic Receptor Blocker

    Proxodolol free base is a selective β-adrenergic receptor blocker. It exhibits efficacy in reducing blood pressure and may be utilized in research focused on arterial hypertension and related cardiovascular conditions. This compound can aid in elucidating the mechanisms of β-adrenergic signaling and its impact on cardiovascular health.
  16. Stable Isotope

    Guanfacine-13C,15N3 is a stable isotope-labeled form of Guanfacine, an orally active noradrenergic α2A adrenergic receptor agonist. This compound exhibits high selectivity for the α2A receptor subtype, contributing to its pharmacological effects such as hypotension and sedation. Guanfacine-13C,15N3 serves as a valuable tool in research applications focused on prefrontal cortex cognitive disorders, including Tourette's syndrome and attention deficit hyperactivity disorder (ADHD).
  17. Drug Derivative

    Photoazolol-1 is a β-adrenergic receptor (βAR) blocker derivative that exhibits unique light-dependent activity. Upon photoactivation, Photoazolol-1 transitions from an inverse agonist to a neutral antagonist, making it a valuable tool for studies involving receptor modulation. This compound's distinct photochemical properties enable innovative research applications in drug development and receptor behavior analysis.
  18. α1-AR Antagonist

    RS-100329 is a selective antagonist of the α1-adrenergic receptor (α1-AR), demonstrating effective inhibition of α1-AR-mediated contractions in lower urinary tract tissues both in vitro and in vivo. This compound is valuable for research applications related to the symptomatic management of benign prostatic hyperplasia, facilitating studies on urinary tract dynamics and receptor signaling pathways.
  19. β3-Adrenergic Receptor Agonist

    Fasobegron is a potent β3-adrenergic receptor agonist, exhibiting a human EC50 of 4.8 nM. Additionally, it demonstrates an EC50 of 250 nM for human β1-adrenergic receptors. This compound is primarily utilized in research related to the treatment of overactive bladder.
  20. β2AR Blocker

    Todralazine is a β2 adrenergic receptor (β2AR) blocker that exhibits antioxidant properties and free radical scavenging activity. This compound demonstrates potential in the regulation of blood pressure through its anti-hypertensive effects. It is a valuable reagent for research applications focused on cardiovascular physiology and the modulation of adrenergic signaling pathways.
  21. Inotropic Compound

    Butopamine hydrochloride is an orally active inotropic compound that primarily targets beta-adrenergic receptors. It is known to enhance cardiac output by increasing heart rate and contractility, making it a valuable tool in cardiovascular research. Its potency may surpass that of Dobutamine, positioning it as an important agent for studies focused on heart function and related conditions.
  22. Beta 3 Receptor Agonist

    BMS-194449 is a selective agonist for the beta-3 adrenergic receptor, exhibiting a binding affinity characterized by a Ki value of 160 nM. This compound is instrumental for research into metabolic disorders, particularly obesity and non-insulin dependent diabetes. Its activation of beta-3 receptors plays a critical role in regulating energy expenditure and lipid metabolism, making it a valuable tool for investigations in these areas.
  23. β-Adrenergic Receptor Blocker

    Proxodolol is a β-adrenergic receptor blocker that inhibits β-adrenergic signaling pathways. It is primarily used in research to investigate its effects on arterial hypertension and related cardiovascular conditions. This compound serves as a valuable tool in studying the physiological implications of β-blockade in various therapeutic contexts.
  24. β2-AR Agonist

    Arformoterol maleate is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a half-maximal effective concentration (Kd) of 2.9 nM. This compound is primarily utilized in research related to chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilation and improving airflow in affected individuals. Its pharmacological properties make it valuable for studying respiratory diseases and the underlying mechanisms of β2-AR signaling.
  25. Adrenergic Receptor

    Parethoxycaine hydrochloride is an anesthetic that acts primarily on the adrenergic receptors, exhibiting nerve conduction blocking activity. It demonstrates non-selective inhibitory effects on the responses of various stimulants in smooth muscle tissues, such as the rat vas deferens and guinea pig ileum. This compound also enhances the action of norepinephrine and its derivatives influence calcium transport processes, displaying distinct effects on calcium dose-response relationships. Parethoxycaine hydrochloride is valuable for research applications involving the modulation of adrenergic signaling and calcium dynamics in neuronal and smooth muscle systems.
  26. I2 Ligand

    Metrazoline is an imidazoline I2 receptor ligand with low affinity for adrenergic receptors. This compound is used in research to study its role in modulating neuroprotective and antihypertensive effects. It serves as a valuable tool for investigating the physiological and pharmacological functions associated with imidazoline receptors in both in vitro and in vivo settings.
  27. 4-Hydroxypropranolol Metabolite

    (±)-4-Hydroxy propranolol β-D-glucuronide is a glucuronidated metabolite of the β-adrenergic receptor antagonist, 4-Hydroxypropranolol. It primarily serves as a marker for metabolic studies involving propranolol administration. This compound is valuable for research exploring drug metabolism, pharmacokinetics, and the therapeutic effects of β-blockers in cardiovascular studies.
  28. Adrenergic Receptor

    (3aR,9aR)-Fluparoxan is a highly selective and potent antagonist of the α2B adrenergic receptor. This compound demonstrates significant potential in neurodevelopmental disorder and neurodegenerative disease research by promoting neurological recovery and function. Its unique mechanism of action positions (3aR,9aR)-Fluparoxan as a valuable tool in neuroscience studies, facilitating the exploration of related therapeutic pathways.
  29. α2-Adrenoceptor Ligand

    TDIQ hydrochloride is a selective ligand for the α2-adrenergic receptors, exhibiting high affinity with Ki values of 75 nM, 95 nM, and 65 nM for the α2A, α2B, and α2C subtypes, respectively. This compound serves as a valuable tool for studying the physiological roles of α2-adrenoceptors and their potential therapeutic applications in various neuropsychiatric and cardiovascular disorders. Its specificity makes it suitable for pharmacological investigations and drug development in receptor-targeted therapies.
  30. Vasorelaxant Agent

    Vasorelaxant agent-2 is an effective vasorelaxant agent that targets the α1A-adrenergic receptor, displaying an affinity of pD2=5.4. This compound demonstrates notable vasodilatory activity, evidenced by an EC50 of 0.79 μM in rat aortic rings. It is a valuable tool for research on vascular function and the modulation of blood pressure.
  31. α2-adrenoceptor Antagonist

    A 80426 mesylate is an α2-adrenoceptor antagonist that modulates neurotransmitter release by inhibiting presynaptic α2-adrenergic receptors. This compound demonstrates potential in the study of antidepressant mechanisms and is utilized in research exploring mood disorders and anxiety. Its ability to enhance noradrenergic neurotransmission makes it a valuable tool for investigating therapeutic strategies within the central nervous system.
  32. Vasopressor

    Mephentermine hemisulfate is a sympathomimetic amine that functions primarily as a vasopressor. It is utilized to increase blood pressure by stimulating adrenergic receptors, leading to vasoconstriction and increased heart rate. This compound has applications in cardiovascular research, particularly in studies related to blood pressure regulation and adrenergic signaling pathways.
  33. β Adrenergic Receptor Antagonist

    Soquinolol is a selective β adrenergic receptor antagonist primarily used in cardiovascular research. This compound exhibits significant inhibition of β-adrenergic signaling, making it valuable for studying cardiac dysfunction and heart failure mechanisms. Its application extends to investigations into therapeutic strategies for managing hypertension and arrhythmias.
  34. ADRB2 Agonist

    Mabuterol hydrochloride is a selective, orally active agonist of the beta-2 adrenergic receptor (ADRB2). This compound demonstrates key biological activity by inhibiting cell proliferation and reducing intracellular calcium levels induced by PDGF-BB. Additionally, Mabuterol hydrochloride downregulates protein expression of Drp-1, cyclin D1, and PCNA, while enhancing Mfn-2 expression in response to PDGF-BB. These properties make Mabuterol hydrochloride valuable for research in cellular signaling and related therapeutic applications.
  35. α1A-Adrenergic Receptor Agonist

    Cirazoline hydrochloride is a potent full agonist of the α1A-adrenergic receptor, exhibiting a competitive inhibition constant (Ki) of 120 nM. It also acts as a partial agonist at the α1B-adrenergic receptor with a Ki of 960 nM and the α1D-adrenergic receptor with a Ki of 660 nM. This compound is valuable for research applications involving α1-adrenergic signaling pathways and the study of cardiovascular and neurological conditions.
  36. α2 Receptor Agonist

    p-Iodoclonidine hydrochloride is a partial agonist of the α2-adrenergic receptor, primarily influencing adrenergic signaling pathways. It exhibits low levels of adenylate cyclase inhibition in platelet membranes and enhances ADP-induced platelet aggregation with an EC50 of 1.5 μM. This compound is useful for research applications focusing on adrenergic receptor physiology and platelet function.
  37. Ergot Derivatives

    Cianergoline is an ergot derivative primarily known for its ability to reduce intraocular pressure (IOP). Its action is mediated by the inhibition of sympathetic nervous function through interactions with both prejunctional (DA2) and postjunctional (α1) adrenergic receptors. This compound is valuable for research applications focused on glaucoma and the underlying mechanisms of ocular hypertension.
  38. Neuropeptide

    BNP(1-32), porcine is an atrial natriuretic peptide that primarily targets neuropeptide pathways. This cardiac hormone exhibits significant natriuretic, diuretic, and vasorelaxant effects, making it valuable for cardiovascular research. Furthermore, BNP(1-32) has been shown to influence passive avoidance learning in rodent models, highlighting its potential role in neurobiology studies involving dopaminergic and cholinergic systems, as well as adrenergic receptor interactions.
  39. mAChR Antagonist

    4-Piperidyl N-(2-biphenyl)carbamate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting notable selectivity for the M2 and M3 subtypes. With pKi values of 7.33 for M2 and 7.51 for M3, this compound demonstrates a markedly higher affinity compared to β2 adrenergic receptors, which has a pKi of 4.94. This specificity makes it a valuable tool for research into mAChR-related signaling pathways and potential therapeutic applications in various neurological disorders.
  40. Xylazine Metabolite

    2,6-Dimethylphenylthiourea is a metabolite of xylazine, an established α2-adrenergic agonist. This compound serves as a valuable tool in pharmacological research, specifically in studies examining the metabolic pathways of xylazine and its effects on α2-adrenergic receptors. It provides insights into its pharmacokinetics and potential physiological implications.
  41. Drug Derivative

    (±)-p-Fluoro pseudoephedrine hydrochloride is a drug derivative associated with the pharmacological activity of pseudoephedrine. This compound exhibits decongestant properties, primarily functioning as a sympathomimetic agent that influences adrenergic receptors. Its biological activity is employed in studies related to respiratory distress, providing valuable insights into drug metabolism and therapeutic efficacy in treatments for nasal congestion.
  42. Clonidine Metabolite

    4-Hydroxyclonidine is a metabolite of Clonidine, primarily functioning as an alpha-2 adrenergic agonist. It exhibits comparable potency to Clonidine in displacing labeled Clonidine from specific antibodies. This compound is of significant interest in pharmacological research, particularly in studies examining adrenergic receptor interactions and the metabolic pathways of antihypertensive agents.
  43. Propranolol Active Metabolite

    Norpropranolol hydrochloride is the active metabolite of Propranolol, primarily targeting beta-adrenergic receptors. It exhibits significant cardiovascular effects, including the reduction of heart rate and blood pressure. This compound is used in research applications focused on studying cardiovascular pharmacology and the modulation of stress response pathways.
  44. Bufuralol Metabolite

    4-Hydroxybufuralol is a primary metabolite of Bufuralol, known for its significant role in pharmacokinetics. It exhibits interactions with beta-adrenergic receptors, contributing to cardiovascular research applications. This compound is essential for studies focused on drug metabolism and the pharmacological effects of beta-blockers.
  45. Alprenolol Metabolite

    4-Hydroxyalprenolol is a metabolite of the β-receptor blocker Alprenolol, known for its role in modulating adrenergic signaling. This compound exhibits biological activity related to cardiovascular function and may be utilized in research focused on the pharmacokinetics and pharmacodynamics of β-blockers. Its analysis can provide insights into the metabolism of therapeutic agents and their effects on β-adrenergic receptors.
  46. Metabolite of Acebutolol

    Diacetolol is an active metabolite of the beta-adrenoceptor antagonist Acebutolol. It exhibits pharmacological activity by selectively inhibiting β1-adrenergic receptors, which plays a significant role in cardiovascular research. Diacetolol is utilized to study beta-blocker pharmacodynamics and to explore its effects on heart rate and blood pressure regulation.
  47. Drug Metabolite

    3-Hydroxy Medetomidine is a primary metabolite of the α2-adrenergic receptor agonist medetomidine. This compound exhibits important biological activity as it participates in modulating adrenergic signaling pathways. Research applications include studies on drug metabolism and the pharmacokinetics of sedatives in both veterinary and medical contexts.
  48. Drug Metabolite

    Silodosin Glucuronide sodium is the sodium salt of Silodosin β-D-glucuronide, a metabolite of the selective α1A-adrenergic receptor antagonist Silodosin. It exhibits high affinity for the α1A-AR, facilitating a Ki value of 0.036 nM. This compound is crucial for studying the pharmacokinetics and metabolic pathways of Silodosin, contributing to research applications in urology and cardiovascular studies.
  49. Terbutaline Derivative

    Terbutalone is a derivative of terbutaline, targeting the β2-adrenergic receptors. As an orally active agonist, it demonstrates significant bronchodilator activity, making it a valuable tool in asthma and respiratory research. Terbutalone may also have applications in studying other β2-adrenergic receptor-mediated physiological responses.
  50. Drug Metabolite

    Carvedilol Glucuronide is a significant metabolite of the β/α-1 adrenergic receptor antagonist, Carvedilol. This compound demonstrates key biological activity by modulating β-adrenergic signaling and exhibits potential application in studying the metabolic pathway of Carvedilol. Research indicates that Carvedilol can inhibit lipid peroxidation and has properties as an antihypertensive agent, as well as an autophagy inducer that affects the NLRP3 inflammasome. Carvedilol Glucuronide serves as an important reagent for investigating drug metabolism and pharmacokinetics in cardiovascular research.

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