Catalog No.
Product Name
Application
Product Information
Citations
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β1-Receptor Blocker
Bisoprolol fumarate is a selective β1-adrenergic receptor blocker, primarily acting on the β1-receptors with minimal influence on β2-receptors. This compound is utilized in research related to hypertension, coronary artery disease, and stable ventricular dysfunction, due to its efficacy in reducing heart rate and myocardial oxygen demand. Its oral bioavailability makes it a valuable tool for studies investigating cardiovascular pharmacology and treatment strategies. -
β-Adrenergic Agonist
Ritodrine is a selective β-adrenergic agonist that serves as an effective smooth muscle and uterine relaxant. Its primary mechanism involves the stimulation of β-adrenergic receptors, which leads to the inhibition of uterine contractions. Ritodrine is utilized in research applications focused on the pharmacological management of premature labor. -
Adrenergic Receptor Agonist
Bitolterol is a β2-adrenergic receptor agonist known for its bronchodilator properties. As a prodrug, it is primarily utilized in the management of respiratory conditions such as asthma and chronic obstructive pulmonary disease. Bitolterol is demonstrated to be safe for breastfeeding, as minimal quantities are transferred into breast milk. -
α1-adrenergic Receptor Antagonist
(±)-WB 4101 is a highly selective antagonist of the α1-adrenergic receptor, effectively inhibiting norepinephrine-induced contraction in vascular smooth muscle. This activity leads to antihypertensive effects and relief of symptoms associated with benign prostatic hyperplasia (BPH). It serves as a valuable tool for research focused on hypertension and BPH, contributing to a deeper understanding of therapeutic strategies in cardiovascular and urological conditions. -
ADRB2 Agonist
Indacaterol acetate is an orally active ultra-long-acting agonist of the β2 adrenergic receptor (ADRB2). It exhibits anti-inflammatory properties by inhibiting NF-κB activity in a β-arrestin2-dependent manner, thereby mitigating lung damage and enhancing lung function in chronic obstructive pulmonary disease (COPD). Additionally, Indacaterol acetate serves as a valuable reagent in cardiovascular disease research. -
Dopamine Prodrug
Docarpamine is an orally active dopamine prodrug that is metabolized to active dopamine through hydroxylation in the small intestine and liver. This compound primarily targets D1-like receptors in peripheral blood vessels, leading to decreased blood pressure and heart rate in spontaneous hypertension. Additionally, Docarpamine influences hemodynamic responses by activating D1-like receptors, vasopressin V1 receptors, and α-adrenergic receptors under normal blood pressure conditions. It is suitable for research into renal vascular dilation and diuresis. -
α2 AR Agonist
RWJ52353 hydrochloride is a selective agonist for the α2D adrenergic receptor, exhibiting a binding affinity with a Ki value of 1.5 nM. This compound has demonstrated significant analgesic properties in animal models, including efficacy in abdominal pain tests and reduced agitation in rodents as assessed by the hot plate and tail flick tests. Additionally, RWJ52353 hydrochloride influences the activity of organic cation transporters, effectively inhibiting rOCT1 and rOCT2, while activating rOCT3, which impacts the transport of [3H]-1-methyl-4-phenylpyridinium in cellular systems. -
β-AR inhibitor
β-AR antagonist 2 functions as a selective antagonist of β-adrenergic receptors, exhibiting an IC50 value of 0.17 μM. This compound has demonstrated significant inhibitory effects on the growth of mouse A549 xenograft tumors and exhibits cardioprotective properties in a model of doxorubicin-induced heart failure in C57 mice. Its applications in cancer research and cardiovascular studies make it a valuable tool for investigating β-AR signaling pathways. -
Beta-Adrenergic Blocker
Flestolol sulfate is a competitive, ultra-short-acting beta-adrenergic blocker. With a half-life of approximately 6.5 minutes, it effectively inhibits beta-adrenergic receptors, making it a valuable reagent for investigating cardiovascular pharmacology. Flestolol sulfate is particularly relevant in research applications focused on chest pain and related cardiovascular conditions. -
α2-AR Agonist
Rezatomidine is a potent and selective α2-adrenergic receptor (α2-AR) agonist that exerts significant analgesic effects. It is primarily utilized in research focused on diabetic neuropathy and neuropathic pain. This compound provides insights into the therapeutic potential of α2-AR modulation in pain management and related disorders. -
α2-Adrenergic Receptor Agonist
Lidamidine hydrochloride is an α2-adrenergic receptor agonist known for its antidiarrheal properties. This compound has been utilized in research to explore its effects on gastrointestinal motility and its potential therapeutic applications in managing diarrhea. Its ability to selectively engage α2-adrenergic receptors makes it a valuable tool for studying adrenergic signaling pathways in various biological contexts. -
Adrenergic Receptor Antagonist
Agaridoxin is an adrenergic receptor antagonist derived from mushrooms, specifically targeting catecholamine receptors. This compound effectively inhibits adrenergic alpha-type receptors, leading to modulation of signaling pathways. Research applications include studies on neuroendocrine regulation and investigations into the role of adrenergic signaling in physiological and pathological processes. Agaridoxin has demonstrated the ability to activate adenylyl cyclase in rat hypothalamic membrane granules in the presence of guanosyl imide diphosphate, contributing to its mechanistic profile. -
Stable Isotope
Alfuzosin-d7 hydrochloride is a deuterium-labeled derivative of Alfuzosin hydrochloride, which functions as an α1 adrenergic receptor antagonist. This compound is primarily used in research applications related to benign prostatic hyperplasia (BPH) and pharmacokinetic studies. The stable isotope label allows for enhanced tracking and analysis of drug metabolism and distribution in various biological systems. -
Adrenergic Receptor
R-(-)-Oxaprotiline is an antidepressant that primarily targets adrenergic receptors, exhibiting both anticholinergic and sympathostimulatory activities. This compound effectively blocks norepinephrine uptake while demonstrating anticholinergic properties, resulting in physiological effects such as increased heart rate and arterial blood pressure. R-(-)-Oxaprotiline also inhibits salivation, aligning with its anticholinergic effects. Its rapid onset of action makes it a valuable tool for research into the mechanisms of depression and the physiological responses to adrenergic receptor modulation. -
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.
