GPCR/G Protein

Items 3651-3700 of 5455

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. βARK Substrate

    RESA peptide is a substrate for β-adrenergic receptor kinase (βARK) that facilitates βARK-mediated phosphorylation. Its N-terminal acidic residues enhance both the efficiency of phosphorylation and the binding affinity to the kinase. This peptide is valuable for studies investigating βARK signaling pathways and the regulation of adrenergic receptors, contributing to the understanding of cardiac function and other physiological processes.
  2. β1 Adrenergic Receptor Antagonist

    ICI 89406 is a selective β1 adrenergic receptor antagonist that can be labeled with positron emitters for positron emission tomography (PET) imaging. This compound is primarily utilized in cardiovascular research to study the effects of β1 adrenergic signaling, enabling insights into heart function and related disorders. Its ability to specifically target the β1 adrenergic receptor makes it a valuable tool for investigating therapeutic interventions in various cardiovascular conditions.
  3. Beta-adrenergic Receptor Agonist

    Metaterol is a selective beta-adrenergic receptor agonist that modulates adrenergic signaling pathways. It primarily exhibits bronchodilatory effects, making it valuable in respiratory research, particularly for studying asthma and chronic obstructive pulmonary disease (COPD). This compound can aid in understanding receptor dynamics and developing targeted therapeutic interventions.
  4. β2 Adrenergic Receptor Agonist

    Milveterol hydrochloride is a long-acting β2-adrenergic receptor agonist that primarily targets the β2 adrenergic receptor. It is utilized in research related to asthma and chronic obstructive pulmonary disease (COPD), facilitating studies on its therapeutic effects and mechanisms of action. This compound contributes to understanding bronchial relaxation and airway response in respiratory disorders.
  5. α1/β1-Adrenergic Receptor Inhibitor

    Amosulalol is a dual inhibitor of the α1 and β1-adrenergic receptors, demonstrating significant antihypertensive activity. By selectively inhibiting the α1-adrenergic receptor, Amosulalol effectively reduces blood pressure, while its β1-adrenergic receptor blockade leads to decreased reflex-induced heart rate and plasma renin activity in spontaneously hypertensive rats. This compound is valuable for research applications focused on cardiovascular physiology and the pharmacological modulation of blood pressure.
  6. Stable Isotope

    Yohimbine-13C,d3 is a deuterium and carbon-13 labeled version of Yohimbine, a potent and nonselective antagonist of alpha-2 adrenergic receptors. With an IC50 value of 0.6 μM, Yohimbine exhibits significant biological activity in modulating adrenergic signaling pathways. This stable isotope compound is valuable for research applications in pharmacokinetics, metabolic studies, and tracing within biological systems.
  7. β1 Adrenergic Receptor Antagonist

    Acebutolol is a selective β1 adrenergic receptor antagonist, primarily utilized in the study of cardiovascular conditions. It demonstrates significant antihypertensive and antiarrhythmic properties, making it suitable for research into hypertension, angina pectoris, and cardiac arrhythmias. This compound serves as an important tool in understanding the mechanisms underlying β1 adrenergic signaling in cardiac function.
  8. α1 AR Antagonist

    Upidosin is an α-1 adrenergic receptor (α-1 AR) antagonist with moderate selectivity for the α-1A AR subtype. It demonstrates uroselectivity, exhibiting a Kb value of 2-3 nM in the urethra and prostate, compared to Kb values of 20-100 nM in the ear artery and aorta. Upidosin effectively inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptors. This compound is a valuable tool for research focused on urethral obstruction and related conditions.
  9. Antiemetic

    Benzquinamide hydrochloride targets the α2 adrenergic receptors (α2-AR), binding with Ki values of 1,365, 691, and 545 nM for the α2A, α2B, and α2C subtypes, respectively. As an antiemetic, it exhibits significant efficacy in preventing nausea and vomiting. Additionally, benzquinamide inhibits P-glycoprotein-mediated drug efflux, thereby enhancing the cytotoxic effects of anticancer agents in multidrug-resistant cell lines, making it a valuable tool in cancer research and therapeutic development.
  10. Adrenergic Receptor Modulator

    Meranzin is an adrenergic receptor modulator derived from the Traditional Chinese Medicine Chaihu-Shugan-San (CSS), isolated from the leaves of Murraya exotica L. It primarily regulates the alpha 2-adrenoceptor and influences the AMPA-ERK1/2-BDNF signaling pathway. Meranzin exhibits potential beneficial effects in preventing the co-occurrence of atherosclerosis and depression, making it a valuable tool for research in neurovascular health and related disorders.
  11. Adrenergic receptor α2B Antagonist

    BAY-6096 is a selective antagonist for the adrenergic receptor α2B, demonstrating a potent inhibitory effect with an IC50 of 14 nM. This compound is characterized by its high water solubility and has been shown to effectively reduce α2B receptor agonist-induced vascular contractions in rat models. BAY-6096 serves as a valuable tool for studying vascular physiology and the role of adrenergic receptors in cardiovascular research.
  12. β-adrenoceptor Antagonist

    Carazolol hydrochloride is a potent β-adrenoceptor antagonist that primarily targets β1 and β2 adrenergic receptors. In addition to its antagonistic properties, it serves as a selective agonist for the β3-adrenoceptor. This compound is primarily utilized in research focused on hypertension and related cardiovascular studies, enabling investigations into β-adrenergic signaling pathways and therapeutic interventions.
  13. β1 Adrenergic Receptor Antagonist

    (Rac)-Nebivolol is a racemic isomer of Nebivolol, a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. This compound exhibits protective effects against ethanol-induced cardiac toxicity by inhibiting the up-regulation of Nox2/NADPH oxidase and reducing lipoperoxidation. Additionally, it demonstrates vasodilatory activity, making it valuable for research in cardiovascular pharmacology and related studies.
  14. β-adrenergic Blocker

    Bunitrolol is an orally active β-adrenergic blocker with a strong affinity for β-adrenergic receptors. It exhibits significant β-receptor antagonist activity alongside weak α1-blocking effects. This compound is primarily utilized in research on cardiovascular disorders, including hypertension and angina pectoris, and has applications in studies related to placental transport mechanisms.
  15. Adrenergic Receptor Agonist

    Broxaterol is a selective agonist of the β2 adrenergic receptor, primarily targeting smooth muscle tissues. This compound exhibits significant bronchodilatory effects, making it valuable in the study of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). Researchers utilize Broxaterol to investigate therapeutic approaches and mechanisms related to airway function and management of respiratory conditions.
  16. Adrenergic Receptor Agonist

    Xamoterol is a selective and potent agonist of the beta-1 adrenergic receptor. It serves as a valuable tool in research exploring arrhythmogenesis and its mechanistic links. Additionally, Xamoterol can be utilized to investigate the relationship between beta-1 adrenergic stimulation and the rapid delayed rectifier potassium current (IKr), facilitating a deeper understanding of cardiac electrophysiology.
  17. α2A-AR Agonist

    α2A-AR agonist 1 is a selective agonist that targets the α2-adrenergic receptor (α2A-AR) with an EC50 of 0.23 nM. This compound demonstrates a significant hypnotic effect, as evidenced by an ED50 of 0.138 mg/kg in loss of righting reflex (LORR) studies. Notably, α2A-AR agonist 1 also shows metabolic stability in mouse liver microsomes, making it a valuable tool for research in pharmacology and neurobiology.
  18. Adrenergic Receptor Antagonist

    L-771688 is a highly selective antagonist of the α1A-Adrenoceptor, exhibiting a Ki of 0.43±0.02 nM. This compound demonstrates potent inhibition of α1A-mediated responses, making it valuable for investigating adrenergic signaling pathways. It is useful in research applications focused on cardiovascular physiology and pharmacology, as well as studies aimed at understanding the role of α1A receptors in various pathological conditions.
  19. α2 Adrenergic Receptor Agonist

    Romifidine is an α2 adrenergic receptor agonist that exerts sedative effects in vivo. It is commonly utilized in veterinary medicine for its ability to induce sedation and anxiety relief in animals. This compound is instrumental in research applications that explore adrenergic receptor pharmacology and the modulation of central nervous system functions.
  20. β-Adrenergic Agonist

    Cimbuterol is a β-adrenergic agonist that functions primarily by activating β-adrenergic receptors, leading to bronchodilation and relaxation of uterine smooth muscle. This compound is utilized in research to investigate its effects on promoting growth and enhancing respiratory function. Its applications extend to studies focused on the treatment of respiratory conditions and the regulation of smooth muscle contraction in various biological systems.
  21. Stable Isotope

    Formoterol-d3 is a deuterium-labeled form of Arformoterol, which is the (R,R)-enantiomer of Formoterol, acting as a long-acting β2-adrenergic receptor (β2-AR) agonist with a Kd of 2.9 nM. This stable isotope allows for enhanced tracking and analysis in pharmacokinetic studies. Formoterol-d3 is primarily utilized in research relating to chronic obstructive pulmonary disease (COPD) and can aid in understanding the pharmacodynamics and metabolism of β2-AR agonists.
  22. Stable Isotope

    Metoprolol-d7 is a deuterium-labeled form of Metoprolol, a selective β1 adrenergic receptor antagonist. It primarily targets β1 receptors to effectively manage conditions such as hypertension and heart failure. This stable isotope is useful in pharmacokinetic studies and metabolic research to trace the metabolic pathways and behavior of Metoprolol in biological systems.
  23. Stable Isotope

    Doxazosin-d8 hydrochloride is a deuterium-labeled derivative of Doxazosin hydrochloride, primarily utilized as a stable isotope in biochemical research. This compound retains the pharmacological activity of the parent molecule, targeting alpha-1 adrenergic receptors and providing insights into receptor dynamics and drug metabolism. Its application is particularly relevant in studies involving pharmacokinetics, enabling more accurate tracking and quantification in biological systems.
  24. Stable Isotope

    Lofexidine-d4 hydrochloride is a deuterium-labeled analog of Lofexidine hydrochloride, which selectively targets the α2-adrenergic receptor. This compound is primarily utilized in research to investigate the mechanisms underlying opioid withdrawal and the pharmacological properties of α2-agonists. Its stable isotope labeling allows for enhanced sensitivity in analytical techniques, facilitating studies in drug metabolism and receptor dynamics.
  25. Adrenergic Receptor Antagonist

    Lusaperidone is an α2 adrenergic receptor antagonist, exhibiting high affinity with Kis of 0.13 nM for α2A and 0.15 nM for α2C receptors. This compound demonstrates significant biological activity in modulating adrenergic signaling pathways, making it a valuable tool for research in neuropharmacology and the study of psychiatric disorders. Lusaperidone may also be utilized to explore its potential effects on the central nervous system and related therapeutic applications.
  26. α-adrenergic Receptor Agonist

    Xylometazoline is an α-adrenergic receptor agonist with a Ki range of 0.05-1.7 μM. This compound effectively induces vasoconstriction of nasal blood vessels, thereby enhancing nasal airflow. Xylometazoline is primarily utilized in research related to nasal congestion and rhinorrhea, facilitating studies on therapeutic interventions for upper respiratory conditions.
  27. α2 Receptor Agonist

    Guanoxabenz is an α2 adrenergic receptor agonist, exhibiting a Ki of 4000 nM and a fully activated form with an affinity of 40 nM for the α2A adrenoceptor. This compound is useful in research applications focusing on the modulation of neurotransmitter release, as well as examining the role of α2 adrenergic signaling in various physiological processes. Its properties make it a valuable tool for studies related to neuropharmacology and cardiovascular research.
  28. Beta Agonist

    Deterenol hydrochloride is a selective beta-agonist that primarily targets beta-adrenergic receptors. This compound exhibits significant biological activity by inducing vasodepressor effects, increasing heart rate, and facilitating respiratory responses. Deterenol hydrochloride is utilized in research applications focused on cardiovascular and respiratory systems, as well as studies investigating the physiological effects of beta-adrenergic modulation.
  29. Adrenergic Receptor

    O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine that acts primarily as an adrenergic receptor inhibitor, specifically targeting the α1 receptor. This compound is known for its ability to induce relaxation of the gastrointestinal tract, making it relevant for studies involving gastrointestinal motility and disorders. Its applications in research may include investigations of smooth muscle relaxation and adrenergic signaling pathways.
  30. β Blocking Agent

    Nafetolol is a selective β1-adrenergic antagonist that effectively targets cardiac β1-adrenoceptors. This orally active β-blocking agent is utilized in research related to cardiovascular physiology and pharmacology, particularly in studies involving heart rate modulation and blood pressure regulation. With a reported half-life of approximately 2 hours in canine models, Nafetolol serves as a valuable tool for investigating β-adrenergic receptor dynamics and therapeutic interventions in cardiac conditions.
  31. β2-adrenoceptor Agonist

    Mapenterol hydrochloride is a selective β2-adrenoceptor agonist that activates β2-adrenergic receptors, leading to smooth muscle relaxation and bronchodilation. It is primarily utilized in research settings to evaluate its potential therapeutic effects in pulmonary diseases, such as asthma and chronic obstructive pulmonary disease (COPD). Additionally, Mapenterol hydrochloride serves as a valuable tool for studying the signaling pathways associated with β2-adrenergic receptor activation in various biological systems.
  32. α2-AR Antagonist

    Idazoxan is a potent antagonist of the α2 adrenergic receptor (α2AR) and may also act as an agonist for I2 imidazoline receptors. This compound is relevant for research in the fields of depression and schizophrenia, allowing for investigations into adrenergic modulation and its effects on these mental health disorders. Idazoxan exhibits oral bioactivity, making it suitable for diverse preclinical studies.
  33. β-adrenergic Receptors Agonist

    Isoetharine is a selective agonist of β-adrenergic receptors, functioning primarily through the stimulation of cAMP production. This catechol-like agent effectively promotes the relaxation of smooth muscle cells, making it valuable in research on respiratory conditions such as emphysema and bronchitis. Isoetharine is utilized as a bronchodilator in various experimental applications to explore mechanisms of airway resistance and smooth muscle dynamics.
  34. β-block Agent

    Timolol hemihydrate functions as a non-selective β-blocker, primarily targeting beta-adrenergic receptors. It is commonly utilized for the reduction of intraocular pressure in conditions such as open-angle glaucoma and ocular hypertension, while also demonstrating cardioprotective effects. This compound serves as a valuable reagent in research exploring cardiovascular health and ocular therapeutics.
  35. Muscarinic Antagonist/β2 Agonist

    CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptor agonist, exhibiting pKi values of 10.4 and 11.4, respectively. Additionally, it serves as a weak calcium channel inhibitor with an IC50 of approximately 50 μM. CHF-6366 effectively inhibits bronchoconstriction in guinea pig models, making it a valuable tool for research into chronic obstructive pulmonary disease (COPD) and related respiratory conditions.
  36. α-adrenergic Receptor Antagonist

    (±)-Scopolamine serves as a potent antagonist of the α-adrenergic receptor. This racemic compound exhibits significant biological activity, with Ki values of 33 μM for the α1-adrenergic receptor and 7.25 nM for the muscarinic cholinergic receptor. Its inhibition of α-adrenergic receptor activity makes it valuable for research applications in neuropharmacology, the study of neurotransmitter systems, and the exploration of potential therapeutic interventions in various neurological disorders.
  37. Adrenoceptor Agonist

    Clenbuterol is a potent β2-adrenergic receptor agonist with an EC50 of 31.9 nM. This compound functions as an effective bronchodilator and demonstrates significant anti-inflammatory properties by inhibiting the lipopolysaccharide-induced release of pro-inflammatory cytokines TNF-α and IL-1β. Clenbuterol is valuable for research applications focused on respiratory disease models and inflammation-related studies.
  38. β-Adrenergic Receptor Blocker

    Sotalol is a non-selective β-adrenergic receptor blocker with oral bioavailability. This compound exhibits potent antiarrhythmic activity, making it valuable for the investigation of pediatric arrhythmias. In addition to its β-receptor blocking effects, Sotalol also inhibits potassium KCNH2 channels, contributing to its antiepileptic properties and expanding its relevance in cardiovascular and neurological research applications.
  39. β3-Adrenergic Receptor Antagonist

    Vemtoberant mesylate is a potent β3-adrenergic receptor antagonist, targeting the β3-adrenergic receptors involved in various physiological processes. This compound has demonstrated significant potential in research related to β3 adrenergic receptor-mediated disorders, particularly in the context of heart failure. Its ability to modulate β3 receptor activity makes it a valuable tool for exploring therapeutic strategies in cardiovascular and metabolic diseases.
  40. β1-AR Agonist

    Dobutamine tartrate is a selective β1-adrenergic receptor (β1-AR) agonist. It predominantly enhances cardiac output by stimulating β1-AR, leading to improved myocardial contractility and heart rate. This compound is widely utilized in cardiac research, particularly in studies focused on heart failure, hypoperfusion, and cardiac stress testing. Additionally, its relatively weak activity at α1-AR and β2-AR lends it a specific profile for evaluating β1-mediated effects in various physiological and pathological contexts.
  41. Stable Isotope

    Bufuralol-d9 hydrochloride is a deuterated form of Bufuralol hydrochloride, serving as a stable isotope. Its primary mechanism involves selective beta-adrenergic receptor antagonism, which is crucial for research involving pharmacokinetics and metabolic studies. This reagent is particularly useful in tracing and quantifying drug metabolism and interactions in biological systems, facilitating advanced studies in cardiovascular and pharmacological research.
  42. Stable Isotope

    (S)-Metoprolol-d7 is a deuterated form of Metoprolol, a selective β1-adrenergic receptor antagonist. This stable isotope-labeled compound is primarily utilized in pharmacokinetic studies and drug metabolism research, providing insights into the pharmacological properties of Metoprolol in cardiovascular applications, particularly in hypertension treatment. Its incorporation of deuterium allows for enhanced tracking and analysis in various analytical techniques.
  43. Stable Isotope

    Alfuzosin-d3 hydrochloride is a deuterated form of Alfuzosin hydrochloride, targeting α1 adrenergic receptors. This stable isotope is utilized primarily in pharmacokinetic studies and drug metabolism research, enabling precise tracking of drug behavior in biological systems. It is particularly relevant in studies involving benign prostatic hyperplasia (BPH) therapies.
  44. Stable Isotope

    (R)-Metoprolol-d7 is a deuterium-labeled analog of Metoprolol, a selective β1 adrenergic receptor antagonist. This stable isotope is essential for pharmacokinetic studies and metabolic research, allowing for precise tracking and quantification of Metoprolol in biological systems. It is particularly valuable in investigations related to cardiovascular diseases, including hypertension and heart failure.
  45. Stable Isotope

    Medetomidine-d3 hydrochloride is a deuterated form of Medetomidine hydrochloride, targeting adrenergic alpha-2 receptors as an agonist. This stable isotope is useful for pharmacokinetic studies, enabling researchers to trace metabolic pathways and evaluate the efficacy of alpha-2 adrenergic receptor modulation in various biological systems. Its application is particularly valuable in drug discovery and development involving sedative and analgesic compounds.
  46. Stable Isotope

    Indacaterol-d3 is a deuterium-labeled form of Indacaterol, an inhaled beta-2 adrenergic receptor agonist. This stable isotope is utilized in pharmacokinetic studies and drug metabolism research, enabling precise tracking of drug behavior in biological systems. Its unique labeling allows for enhanced analytical sensitivity in studies involving respiratory conditions and therapeutic applications in chronic obstructive pulmonary disease (COPD) and asthma.
  47. Adrenergic Receptor

    Azepexole is a selective α2 adrenergic receptor agonist, exhibiting over 300-fold selectivity for α2 adrenergic receptors compared to α1 adrenergic receptors. This compound is utilized to investigate the biological functions of α2 adrenergic receptors and their involvement in various pathophysiological conditions. Additionally, Azepexole may contribute to mood regulation and enhancement of cognitive functions, making it a valuable tool in neuropharmacological research.
  48. Adrenergic Receptor Agonist

    Solabegron hydrochloride is a selective β3-adrenergic receptor agonist that stimulates the accumulation of cAMP in cells expressing the human β3-adrenergic receptor, exhibiting an EC50 value of 22 nM. This compound is primarily investigated for its therapeutic potential in treating overactive bladder and irritable bowel syndrome, making it a valuable reagent for research in urology and gastroenterology.
  49. α2-Adrenergic Receptor Agonist

    Tiamenidine is an orally active α2-adrenergic receptor agonist that exhibits significant antihypertensive effects. This compound is primarily utilized in hypertension research, where it aids in the investigation of blood pressure regulation and related cardiovascular mechanisms. Its ability to selectively target α2-adrenergic receptors makes Tiamenidine a valuable tool for studying adrenergic signaling pathways in various physiological and pathological conditions.
  50. Adrenergic Receptor Antagonist

    Fenmetozole acts as an antagonist of the α2-adrenergic receptor, exhibiting potential antidepressant effects. This compound is utilized in research focused on ethanol antagonism and the modulation of adrenergic signaling pathways. Its applications extend to studies investigating mood disorders and the potential therapeutic benefits of adrenergic receptor modulation.

Items 3651-3700 of 5455

Page
per page
Set Descending Direction