Catalog No.
Product Name
Application
Product Information
Citations
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Adrenergic Receptor
Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine reuptake inhibitor that targets norepinephrine transporters in both the central and peripheral nervous systems. This compound has demonstrated efficacy in increasing urethral resistance and has been investigated for its therapeutic potential in stress urinary incontinence, as evidenced by a Phase IIa clinical study. Its peripheral selectivity allows for enhanced urethral closure while minimizing central nervous system penetration, making Esreboxetine a valuable tool for researchers exploring treatments for urinary incontinence and related conditions. -
Adrenergic Receptor Antagonist
Colterol acetate is a selective antagonist of β-adrenergic receptors, specifically targeting β1 and β2 subtypes. It exhibits notable biological activities, including the relaxation of tracheal smooth muscle and the reduction of subspastic contractions of tricholoma, primarily through β2 receptor modulation. Additionally, Colterol acetate enhances the contractility of left ventricular papillary muscles by engaging β1 receptors. This reagent is valuable for research into respiratory and cardiovascular pharmacology. -
β2AR Antagonist
β2AR antagonist 1 is a selective antagonist of the β2 adrenergic receptor (β2AR), acting primarily on its intracellular surface. This compound inhibits β2AR signaling pathways, making it valuable for studying β2AR-related physiological processes. Its applications include research into cardiovascular function, respiratory disease, and the mechanisms of beta-adrenergic antagonism in various biological systems. -
Adrenergic Receptor Antagonist
Adimolol free base is an antagonist of both β- and α-adrenergic receptors. It demonstrates Ki values of 5.2 x 10^-7 M at α1 and 1.3 x 10^-5 M at α2 adrenergic receptors. This compound is primarily utilized in research applications focused on antihypertensive studies, providing valuable insights into cardiovascular function and regulation. -
Adrenergic Receptor
Bupranolol hydrochloride acts as a non-selective β-adrenergic receptor antagonist, exhibiting significant membrane-stabilizing properties. This compound is known to effectively modulate the contractile activity of the non-pregnant human uterus and has demonstrated impactful effects on spontaneous uterine contractions in in vitro studies involving ovarian cancer patients. Bupranolol hydrochloride is rapidly and completely absorbed in vivo, with carboxybupranolol identified as its primary metabolite, making it a valuable tool for research focused on adrenergic signaling and related pathophysiological conditions. -
β2AR Ligand
β2AR ligand 1 is a homobivalent bitopic ligand that targets the β2 adrenergic receptor (β2AR) by binding to both the orthosteric binding site (OBS) and metastable binding sites (MBS). This compound exhibits specific affinity for β2AR, facilitating the study of receptor activation and signaling pathways. It is valuable in research applications focused on cardiovascular function, asthma, and other conditions where β2AR modulation is of interest. -
β3-adrenergic receptor Agonist
BRL 35135 is a selective agonist of the β3-adrenergic receptor, known for its ability to enhance energy expenditure and promote weight reduction primarily through fat loss while preserving muscle protein. This compound has demonstrated significant improvements in glucose tolerance and insulin sensitivity. BRL 35135 is useful for researchers investigating metabolic disorders such as obesity and diabetes. -
Stable Isotope
Harman-13C2,15N is a stable isotope-labeled derivative of Harmane, a known benzodiazepine receptor antagonist (IC50 = 7 μM). This compound exhibits notable affinity for various biological targets, including mACh (IC50 = 24 μM), Opioid Receptor (IC50 = 2.8 μM), MAO-A/B (IC50 = 0.5 μM), and the α2-adrenergic receptor (IC50 = 5 μM). Harmane is recognized for its diverse pharmacological activities, such as reducing blood pressure via I1 imidazoline receptor inhibition (IC50 = 30 nM), as well as demonstrating antidepressant, anti-anxiety, anticonvulsant, and analgesic properties. Additionally, it has been shown to affect dopamine biosynthesis and enhance mutagenic effects in specific cellular assays. -
β-adrenergic Receptors Agonist
Cimaterol-d7 is a deuterated derivative of Cimaterol, a potent agonist of β-adrenergic receptors, demonstrating pEC50 values of 8.13, 8.78, and 6.62 for human β1, β2, and β3 respectively. This compound enhances biological activity by modulating physiological responses related to these receptors. Cimaterol-d7 is utilized in research to investigate β-adrenergic signaling pathways and its effects on metabolism and growth, particularly in the context of muscle and fat deposition in agricultural applications. -
Stable Isotope
(S)-Carvedilol-d4 is a deuterium-labeled variant of (S)-Carvedilol, a non-selective β-adrenergic and α-1 adrenergic receptor blocker. This compound is utilized in studies investigating the cardioprotective effects against the vascular and cardiac toxicity induced by Doxorubicin (DOX). Its stable isotope labeling enables precise tracking in metabolic studies and pharmacokinetic research applications. -
Adrenergic Receptor Activator
ACTH (1-14) is a peptide fragment of adrenocorticotropic hormone (ACTH) that primarily activates adrenergic receptors. This compound plays a critical role in regulating cortisol and androgen synthesis, making it valuable for studies related to adrenal function and stress response. ACTH (1-14) is applicable in research investigating hormonal pathways, stress-related disorders, and the physiological effects of adrenal hormones. -
Adrenergic Receptor Antagonist
L-771688 hydrochloride is a highly potent and selective α1A-adrenoceptor antagonist, exhibiting a Kd of 43-90 pM. It demonstrates strong affinity for cloned human, rat, and canine α1A-adrenergic receptors, with a Ki of less than 1 nM and over 500-fold selectivity against the α1B and α1D isoforms. L-771688 effectively blocks norepinephrine-induced responses, making it useful for studying adrenergic signaling pathways. Its ability to inhibit contractions induced by phenylephrine or A-61603 in various animal models further underscores its applications in cardiovascular research. -
Adrenergic Receptor Antagonist
Aldioxa is an adrenergic receptor antagonist with a primary mechanism of antagonizing α-2 adrenergic receptors. It has demonstrated efficacy in improving delayed gastric emptying and gastric compliance, which are significant factors in functional dyspepsia (FD). Aldioxa has shown the ability to partially reverse delays in gastric emptying induced by clonidine or restraint stress, making it a valuable candidate for further research into therapeutic interventions for FD. -
Stable Isotope
Vilanterol-d4 trifenatate is a deuterium-labeled analog of Vilanterol, a long-acting β2-adrenergic receptor agonist. It selectively binds to β2 adrenergic receptors, leading to increased intracellular cAMP levels and subsequent relaxation of bronchial smooth muscle. This reagent is valuable for research into asthma and related airway diseases, providing a stable isotope for pharmacokinetic and metabolic studies. -
β-adrenergic Receptor Blocker
ent-Levobunolol hydrochloride is a competitive β-adrenergic receptor blocker that primarily targets β-adrenergic receptors. This compound effectively inhibits sympathetic nerve impulse transmission, decreases aqueous humor production, and induces vasoconstriction in ocular tissues, leading to reduced intraocular pressure. It is a valuable reagent for research focused on ocular hypertension conditions, including glaucoma. -
Quinazoline Derivative
DL-017 is a Quinazoline derivative that exhibits potent inhibition of α1-adrenergic receptors, with an IC50 of approximately 0.90 nM, and Na+ channels, with an IC50 of 404 nM. Its robust antihypertensive activity makes DL-017 a valuable reagent for studying cardiovascular mechanisms and exploring therapeutic avenues for hypertension. This compound serves as a crucial tool in pharmacological research and drug development focused on adrenergic modulation and ion channel interactions. -
Stable Isotope
Oxprenolol-d7 is a deuterated form of Oxprenolol, a selective β-adrenergic receptor antagonist exhibiting a Ki of 7.10 nM as determined by radioligand binding assays in rat heart muscle. This stable isotope-labeled compound is primarily used in pharmacokinetic studies and metabolic research to trace β-AR activity in various biological systems. Its application in isotope labeling enables enhanced detection and quantification in advanced analytical techniques. -
Adrenergic Receptor
JTH-601 Free Base is a selective alpha1-adrenoceptor antagonist that effectively inhibits phenylephrine-induced contractions in lower urinary tract tissues. This compound demonstrates greater potency in competitively antagonizing alpha1-adrenoceptor-mediated contractile responses compared to commonly used agents. JTH-601 Free Base holds potential for therapeutic applications in addressing urinary outlet obstruction associated with benign prostatic hyperplasia. -
β3-AR Ligand
SB-206606 is a selective beta 3-adrenergic receptor (β3-AR) ligand, exhibiting a significantly higher affinity for β3-AR, being 76 times more potent than for beta 1 and beta 2-adrenergic receptors. This compound serves as a valuable tool for studying β3-AR-mediated pathways and their implications in metabolic processes. Its specificity makes it essential for research into obesity, diabetes, and cardiovascular diseases. -
Beta-AR Antagonist
Oxprenolol is a potent β-adrenergic receptor (β-AR) antagonist, exhibiting a Ki value of 7.10 nM in radioligand binding assays with rat heart muscle. This compound demonstrates significant biological activity in modulating cardiovascular responses and is primarily utilized in research investigating heart rate and blood pressure regulation. Oxprenolol is valuable for studying adrenergic signaling pathways and exploring therapeutic strategies for heart-related conditions. -
Adrenergic Receptor Agonist
Phenylephrone-d3 hydrochloride is a deuterium-labeled derivative of phenylephrine, functioning as an adrenergic receptor agonist. This compound is primarily used in research applications focusing on mydriatic effects and can serve as a safe and effective agent in phenylephrine chemical delivery systems. Its labeling with deuterium allows for enhanced tracking and analysis in pharmacokinetic studies. -
Adrenergic Receptor Inhibitor
Napitane is an adrenergic receptor inhibitor that primarily targets α-adrenergic receptors, leading to enhanced catecholamine availability. This compound has demonstrated significant potential in antidepressant research, highlighting its efficacy in modulating neurochemical pathways associated with mood regulation. Napitane serves as a valuable tool for investigating mechanisms underlying depression and exploring novel therapeutic approaches for mood disorders. -
Stable Isotope
Ractopamine-13C6 is a stable isotope-labeled derivative of Ractopamine, a potent β-adrenergic receptor (βAR) agonist known for its high affinity with a Kd of approximately 25 nM for pig β1AR and β2AR. Additionally, Ractopamine acts as a mTAAR1 agonist with an EC50 of 16 μM. This compound plays a crucial role in promoting muscle mass development, reducing fat deposition, and enhancing feed efficiency in swine. Ractopamine-13C6 is ideal for research focused on increasing lean tissue growth and improving production efficiency in livestock. -
β-adrenoceptor Agonist
Arbutamine hydrochloride is a potent, short-acting nonselective β-adrenoceptor agonist. It primarily targets β1-, β2-, and β3-adrenergic receptors, leading to increased heart rate, enhanced cardiac contractility, and elevated systolic blood pressure. This compound is valuable for research applications involving cardiac stress testing and investigating adrenergic signaling pathways. -
Stable Isotope
Tamsulosin-d4 hydrochloride is a deuterium-labeled derivative of Tamsulosin, a selective α1-adrenergic receptor inhibitor. This stable isotope is utilized in pharmacokinetic studies and metabolic research related to prostatic hyperplasia. Additionally, Tamsulosin has demonstrated effects in attenuating the growth of abdominal aortic aneurysms in experimental models, making it relevant for studies in vascular biology and urology. -
Adrenergic Receptor
(R)-Dabelotine acts as an adrenergic receptor agonist, specifically the R-isomer of Dabelotine. This compound has been investigated for its potential neuroprotective effects, particularly in the context of dementia research. Its ability to engage adrenergic pathways may offer insights into therapeutic strategies for neurodegenerative disorders. -
Adrenergic Receptor
FMS586 free base is a selective antagonist of the neuropeptide Y Y5 receptor, exhibiting oral bioactivity. It effectively inhibits the hPP-induced increase in adrenocorticotropic hormone (ACTH) and cortisol levels, and reverses the upregulation of corticotropin-releasing hormone (CRF) and vasopressin (AVP) mRNA expression following central administration of hPP. This compound offers valuable insights into the role of Y5 receptors in activating the hypothalamic-pituitary-adrenal (HPA) axis, making it a significant tool for studying neuroendocrine regulation. -
Adrenaline Receptor Antagonists
Cyclazosin hydrochloride is an α1B-adrenergic receptor antagonist that exhibits high specificity for α-adrenergic receptors, with reported pKi values ranging from 9.23 to 9.57 for O/1A and 8.18 to 8.41 for OflB receptors. This compound is utilized in research to study the role of α-adrenergic signaling in various physiological processes and to explore potential therapeutic applications in conditions influenced by adrenergic activity. However, Cyclazosin hydrochloride does not differentiate between cloned alb and alo adrenergic receptor subtypes, exhibiting similar affinity profiles. -
β-adrenoceptor Blocker
Nifenalol is a selective β-adrenoceptor blocker, primarily targeting β-adrenergic receptors. This compound has demonstrated the ability to inhibit β-adrenoceptor differentiation in various tissues, including the right atrium, diaphragm, and adipose tissue in rat models. Its pharmacological profile makes Nifenalol a valuable tool for studying cardiovascular function and metabolic processes in research applications. -
Adrenergic Receptor Antagonist
Fenmetozole hydrochloride is an adrenergic receptor antagonist, primarily targeting the α2-adrenergic receptor. This compound exhibits notable antidepressant effects and serves as an antagonist of ethanol. Its biological activity makes it relevant in research applications focused on mood disorders and the modulation of ethanol-related behaviors. -
α2-Adrenergic Receptor Agonist
Tiamenidine hydrochloride is an α2-adrenergic receptor agonist that exerts centrally acting hypotensive effects. By binding to these receptors, it regulates blood pressure and has potential applications in hypertension research. This compound is useful for investigating mechanisms of blood pressure modulation and evaluating therapeutic strategies for hypertension management. -
α1 Adrenergic Receptor Inhibitor
Conopeptide rho-TIA is a peptide originating from the venom of the predatory sea snail Conus tulipa, serving as a highly selective noncompetitive inhibitor of the human α1B-adrenergic receptor. It also acts as a competitive inhibitor for both the α1A- and α1D-adrenergic receptors. By selectively binding to these receptor subtypes, conopeptide rho-TIA offers valuable insights for the development of novel, subtype-selective α1-adrenergic receptor therapies. Its unique mechanism of action makes it a potent tool for cardiovascular and pharmacological research. -
Adrenoreceptor Agonist
Dabelotine is an adrenergic receptor agonist that selectively targets adrenoreceptors, contributing to the modulation of synaptic transmission. It exhibits potential neuroprotective effects and has been employed in research related to dementia and cognitive decline. Its applications extend to the investigation of neurodegenerative diseases, where understanding adrenergic signaling may reveal novel therapeutic strategies. -
adrenergic α antagonist
Proroxan hydrochloride is a non-selective adrenergic α-antagonist that primarily targets α-adrenergic receptors. This compound exhibits significant biological activity in inhibiting adrenergic signaling, making it valuable in research on hypertension and associated cardiovascular conditions. It serves as a useful tool for investigating the pharmacological effects of α-adrenergic blockade in various experimental models. -
α2-Adrenergic Receptor Antagonist
Fipamezole is a potent antagonist of the α2-adrenergic receptor, exhibiting Ki values of 9.2 nM, 17 nM, and 55 nM for the human α2A, α2B, and α2C receptors, respectively. This compound serves as an effective anti-dyskinetic agent, making it valuable for research applications in the study of Parkinson's disease and related movement disorders. Its oral bioavailability enhances its utility in various experimental settings. -
β-adrenergic Agonist
L-640,033 is a potent β-adrenergic agonist that activates β-adrenergic receptors, playing a crucial role in lipid metabolism and cellular growth. This compound is valuable for studying mechanisms related to energy homeostasis, adipogenesis, and cardiovascular function. Its application in research can provide insights into metabolic disorders and the physiological effects of adrenergic signaling. -
α2-adrenergic Agonist
Detomidine carboxylic acid is a primary urinary metabolite of Detomidine, functioning as an α2-adrenergic agonist. This compound exhibits significant biological activity by influencing cardiovascular and respiratory systems, as well as displaying an antidiuretic effect. It is useful in research applications focused on pharmacology and the investigation of adrenergic receptor mechanisms. -
Adrenergic Receptor
L-654284 is a selective α2-adrenergic receptor antagonist that effectively competes with the binding of radiolabeled 3H-clonidine and 3H-rauwolscine, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. This compound demonstrates the ability to block the effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. Additionally, L-654284 shows notable selectivity towards α2 and α1 adrenergic receptors, with a Ki of 110 nM against 3H-prazosin binding. In vivo studies reveal that L-654284 enhances norepinephrine turnover in the rat cerebral cortex, highlighting its potential applications in research related to central nervous system pharmacology. -
α1A Adrenergic Receptor Antagonist
SNAP5089 hydrochloride is a selective antagonist of the α1A adrenergic receptor. This compound exhibits significant biological activity in the modulation of adrenergic signaling pathways. It is primarily utilized in research related to hypertension and benign prostatic hyperplasia, providing valuable insights into these conditions and their underlying mechanisms. -
Dopamine receptor/α-adrenergic receptor antagonist/antiperoxidant
Bulbocapnine is an aporphine isoquinoline alkaloid that acts as an antagonist at dopamine and α-adrenergic receptors, alongside possessing anti-peroxidative properties. This compound has been shown to reduce intracellular dopamine levels and inhibit tyrosine hydroxylase activity with a Ki value of 0.20 mM. Additionally, Bulbocapnine decreases intracellular Ca2+ concentration and mitigates the dose-dependent inhibitory effects of dopamine on heart rate acceleration, making it a valuable tool for research in cardiovascular physiology and neurobiology. -
Stable Isotope
(Rac)-Talinolol-d5 is a stable isotope of Talinolol, a long-acting, cardioselective β1-adrenergic receptor blocker. This compound demonstrates significant cardioprotective and antihypertensive properties. Additionally, Talinolol serves as a valuable probe substrate for investigating P-glycoprotein (P-gp) activity in pharmacokinetic studies. -
Stable Isotope
Isoprenaline-d7 hydrochloride is a deuterated analog of Isoprenaline, serving as a stable isotope for research applications. As a non-selective β-adrenergic receptor agonist, Isoprenaline exhibits significant peripheral vasodilatory, bronchodilator, and cardiac stimulatory effects. This compound is valuable for studying conditions such as bradycardia and bronchial asthma, providing insights into β-adrenergic signaling pathways and related therapeutic interventions. -
D2 dopamine receptor and β2-adrenocepto agonist
Sibenadet hydrochloride is a dual agonist of the D2 dopamine receptor and the β2-adrenoceptor. It exhibits significant bronchodilator activity and has been shown to effectively inhibit sensory nerve activity in animal models of chronic obstructive pulmonary disease (COPD). Research indicates that Sibenadet hydrochloride reduces reflex cough, mucus production, and tachypnoea, making it a valuable tool for studying respiratory disorders and potential therapeutic interventions. -
β3-Adrenergic Receptor Agonist
LY-377604 hydrochloride is a potent agonist of the human β3-adrenergic receptor, with an EC50 value of 2.4 nM. In addition to its agonistic properties, it functions as an antagonist at the β1- and β2-adrenergic receptors. This compound is primarily utilized in research focused on metabolic disorders, obesity, and cardiovascular disease, providing insights into β-adrenergic signaling pathways. -
Stable Isotope
4-Hydroxypropranolol-d7 is a deuterium-labeled derivative of the active metabolite 4-Hydroxypropranolol hydrochloride, which targets β1- and β2-adrenergic receptors with high affinity, exhibiting pA2 values of 8.24 and 8.26, respectively. This compound maintains comparable potency to Propranolol and displays intrinsic sympathomimetic activity, membrane-stabilizing properties, and potent antioxidant effects. 4-Hydroxypropranolol-d7 is instrumental for pharmacokinetic studies, providing valuable insights into drug metabolism and receptor activity in various biological assays. -
Adrenergic Receptor Stimulator
Butopamine is a selective stimulant of β1-adrenergic and β2-adrenergic receptors, exerting its biological effects primarily in skeletal muscle and adipose tissue. This compound is notable for its role in enhancing muscle growth and altering fat metabolism, making it a valuable tool in research related to anabolic processes and energy expenditure. Its unique mechanism of action provides insights into adrenergic signaling pathways and their implications in metabolic disorders and muscle physiology. -
Adrenergic Receptor Agonist
DL-Methyldopa is a centrally acting α2-adrenergic receptor agonist, primarily involved in the modulation of neurotransmitter biosynthesis. It exhibits significant biological activity by influencing adrenergic signaling pathways, making it relevant for studies in neurological diseases. This compound serves as a valuable tool in research aimed at understanding and treating conditions related to adrenergic dysfunction. -
β1 Adrenergic Receptor Antagonist
Acebutolol-d7 is a deuterium-labeled form of Acebutolol, a selective β1 adrenergic receptor antagonist. This compound exhibits key biological activity by inhibiting β1 adrenergic receptors, leading to potential therapeutic effects in conditions such as hypertension, angina pectoris, and cardiac arrhythmias. Acebutolol-d7 is valuable for research applications involving pharmacokinetics and metabolic studies of β1 adrenergic signaling pathways. -
α1-Adrenergic Receptor Antagonist
Quinazosin dihydrochloride is an α1-adrenergic receptor antagonist primarily utilized in hypertension management. Its mechanism of action includes the inhibition of granulopoiesis, leading to effects such as neutropenia and leukopenia. Additionally, Quinazosin dihydrochloride demonstrates dose-dependent myelosuppression connected to the duration of exposure, making it valuable for research on hematologic effects and cardiovascular therapies. -
β2AR Negative Allosteric Modulator
AP-7-168 is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). It functions by promoting β2AR homodimerization and inhibiting GRK5-mediated phosphorylation, thereby sustaining bronchorelaxation in both cell and tissue models. This compound is particularly valuable for research in inflammation and immunology, including studies related to asthma and other respiratory conditions.
