Catalog No.
Product Name
Application
Product Information
Citations
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α-Adrenergic Receptor Agonist
Naphazoline nitrate is an α-adrenergic receptor agonist that effectively induces vasoconstriction and reduces vascular hyperpermeability. It has been shown to lower the levels of inflammatory mediators such as TNF-α, IL-1β, IL-6, as well as cytokines including IFN-γ and IL-4. Naphazoline nitrate is utilized in research related to non-bacterial conjunctivitis, providing insight into its effects on inflammation and vascular response. -
Antiarrhythmic Agent
Dronedarone is a class III antiarrhythmic agent primarily targeting ion channels to manage atrial fibrillation (AF) and atrial flutter. It effectively inhibits multiple ion currents, including potassium, sodium, and L-type calcium currents, while also displaying antiadrenergic properties through noncompetitive binding to β-adrenergic receptors. Additionally, Dronedarone acts as a moderate inhibitor and substrate for CYP3A4, making it valuable for pharmacological studies in cardiac rhythm disorders. -
Adrenergic Receptor Antagonist
Dibenamine is an alpha-adrenergic receptor antagonist that inhibits both basal and histamine-stimulated gastric acid secretion. Its primary pharmacological activity renders it useful in studying conditions characterized by excessive gastric acid production. Additionally, Dibenamine can be employed in research concerning adrenergic signaling pathways and their impact on gastric physiology. -
Dopamine Receptors Blocker
Trifluoperazine dihydrochloride is a dopamine receptor antagonist, primarily used in the study of schizophrenia. This compound demonstrates significant activity as an α1-adrenergic receptor blocker and acts as a potent inhibitor of NUPR1, exhibiting anticancer properties. Additionally, it functions as a calmodulin inhibitor and has been shown to inhibit P-glycoprotein, impacting multidrug resistance. Trifluoperazine dihydrochloride is also recognized for its reversible inhibition of influenza virus morphogenesis, making it valuable for various research applications in neuropharmacology and virology. -
Adrenergic Receptor Agonist
Salbutamol is a short-acting β2-adrenergic receptor agonist that primarily targets the β2-adrenergic receptor. It is well-known for its ability to promote relaxation of bronchial smooth muscle, making it a valuable tool in the study of bronchospasm related to asthma and chronic obstructive pulmonary disease. Additionally, Salbutamol has been implicated in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway, highlighting its relevance in cancer research. -
β/α-1 Blocker
Carvedilol phosphate hemihydrate is a non-selective β/α-1 adrenergic receptor blocker. It demonstrates significant biological activity by inhibiting lipid peroxidation with an IC50 of 5 μM and acts as a multiple-action antihypertensive agent, with potential applications in treating angina and congestive heart failure. Additionally, carvedilol phosphate hemihydrate has been identified as an autophagy inducer that suppresses the NLRP3 inflammasome, making it valuable for research in inflammation and cardiovascular diseases. -
Adrenergic Receptor Inhibitor
Penbutolol sulfate is a potent adrenergic receptor inhibitor, primarily acting as a β-adrenoceptor and 5-HT receptor antagonist, with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 regions, respectively. This compound demonstrates significant biological activity through modulation of neurotransmitter signaling pathways, making it valuable for research applications involving cardiovascular studies and neuropharmacology. -
Serotonin Receptor Antagonist
Setiptiline maleate is a serotonin receptor antagonist targeting multiple pathways in neurotransmitter regulation. As a tetracyclic antidepressant (TeCA), it functions primarily as a noradrenergic and specific serotonergic antidepressant (NaSSA), inhibiting norepinephrine reuptake and antagonizing α2-adrenergic receptors. Setiptiline maleate further interacts with serotonin receptor subtypes, including 5-HT2A, 5-HT2C, and/or 5-HT3, while also acting as an H1 receptor inverse agonist, demonstrating potential utility in depression and anxiety research. -
5-HT1A Receptor Agonist
Tandospirone citrate is a selective partial agonist of the 5-HT1A receptor, exhibiting a binding affinity with a Ki value of 27 nM. It demonstrates significant selectivity over other serotonin and adrenergic receptors, including SR-2, SR-1C, α1, α2, D1, and D2, with Ki values ranging from 1300 to 41000 nM. This compound is primarily used in research related to psychiatric disorders and anxiety management, making it a valuable tool for exploring serotonergic pathways and their implications in mental health. -
5-HT1AR Agonist/α1-Adrenergic Receptor Antagonist
Enciprazine is an orally active non-benzodiazepine anxiolytic that primarily functions as a 5-HT1A receptor agonist and an α1-adrenergic receptor antagonist. This compound has demonstrated the ability to modulate electroencephalogram activity by decreasing δ and θ wave power while increasing α and fast β wave power. With its anti-aggressive properties, Enciprazine exhibits minimal sedative and ataxic side effects. Additionally, it influences plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis, making it a valuable tool for research into anxiety disorders, generalized anxiety syndrome, and psychosis. -
Adrenergic Receptor Antagonist
Tertatolol is a potent antagonist of beta-adrenoceptors and 5-HT receptors. It exhibits unique renal vasodilatory effects, making it a valuable tool for investigating cardiovascular and renal physiology. Tertatolol is utilized in research applications focusing on the modulation of adrenergic signaling and its implications in various pathological conditions. -
Stable Isotope
Pindolol-d7 is a deuterated form of Pindolol, primarily targeting the 5-HT 1A (Ki=33 nM) and 5-HT 1B receptors, as well as β1/β2-adrenergic receptors. This stable isotope is utilized in research to investigate the pharmacokinetics and metabolic pathways of Pindolol. The compound demonstrates significant anti-anxiety and antidepressant activities, making it valuable for studies related to psychiatric disorders and neuropharmacology. -
Stable Isotope
Melperone-d4 hydrochloride is a deuterium-labeled derivative of Melperone hydrochloride, a butyrophenone with atypical antipsychotic properties. It acts as a multireceptor antagonist, exhibiting binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Additionally, Melperone-d4 displays weak interactions with several other receptors and inhibits CYP2D6. This reagent is particularly valuable for investigating schizophrenia and managing agitation in geriatric populations. -
Adrenergic Receptor Antagonist
(4E)-SUN9221 is a potent antagonist of the α1-adrenergic receptor and the 5-HT2 receptor, demonstrating significant biological activity in modulating cardiovascular responses. This compound exhibits antihypertensive effects and inhibits platelet aggregation, making it a valuable tool for research in hypertension and thrombosis. Its ability to selectively target these receptors provides insights into adrenergic signaling and related pathological conditions. -
5-HT1/5-HT2/adrenergic (α1) Receptors Antagonist
Centpropazine is a non-selective antagonist of serotonin (5-HT1/5-HT2) and adrenergic (α1) receptors. It modulates monoamine neurotransmission by reducing the reuptake of serotonin and norepinephrine, leading to antidepressant effects. This compound is valuable for research into depression and related mood disorders, facilitating insights into neurotransmitter dynamics and their role in mental health. -
Triple Reuptake Inhibitor
Tedatioxetine is a serotonin and norepinephrine-preferring triple reuptake inhibitor (TRI) that also functions as an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors. This compound exhibits significant biological activity in modulating neurotransmitter levels, making it relevant for research in neuropharmacology. Its mechanism of action positions it as a valuable tool in studies related to mood disorders and anxiety. -
Piperazine
1-(3-Fluorophenyl)piperazine (hydrochloride) is a selective blocker of the 5-HT receptor 1A and an adrenergic receptor antagonist. This compound exhibits significant biological activity relevant to research in neuropharmacology, particularly in the study of serotonergic and adrenergic signaling pathways. It can be utilized in various applications, including the investigation of anxiety, depression, and other mood disorders. -
5-HT6 Receptor Agonist
ST1936 oxalate is a selective agonist of the 5-HT6 receptor, demonstrating high nanomolar affinity with a Ki value of 13 nM for the human receptor. It exhibits additional binding affinity for 5-HT7 and 5-HT2B receptors with Ki values of 168 nM and 245 nM, respectively, as well as moderate binding to α2 adrenergic receptors in both human and rat models (Ki of 300 nM). This compound is valuable for research applications focused on serotonergic signaling and its implications in neuropharmacology. -
Antipsychotic Agent
Mazapertine is an orally active antipsychotic agent primarily targeting dopamine D2, D3, and D4 receptors with high affinity (Ki values < 3 nM). Additionally, it exhibits significant binding to serotonin 5-HT1A receptors (Ki = 1.7 nM) and α1-adrenergic receptors (Ki = 1.3 nM). This compound is valuable for research into neurological diseases, particularly in the context of antipsychotic drug development and neuropharmacology studies. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole is a potent α2-adrenoceptor antagonist and 5-HT receptor reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is primarily utilized in research related to depression, facilitating studies on the modulation of serotonergic and adrenergic signaling pathways. Its unique pharmacological profile makes it a valuable tool for investigating potential therapeutic approaches in mood disorders. -
5-HT2C Receptor Positive Allosteric Modulator
CYD-1-79 is a selective positive allosteric modulator of the 5-HT2C receptor. This compound enhances 5-HT-induced intracellular calcium release through a distinct allosteric site, demonstrating significant inhibition at dopamine D3 receptors, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 has been shown to modulate spontaneous ambulation in rodents and can synergize with low doses of 5-HT2C receptor agonists. Additionally, it reduces relapse vulnerability in models of psychoactive substance self-administration, highlighting its potential applications in neurological disease research. -
Stable Isotope
Arotinolol-d5 hydrochloride is a deuterated analog of Arotinolol, a nonselective α/β-adrenergic receptor blocker with vasodilatory properties. This compound exhibits notable activity in inhibiting the binding of the radioligand 125I-ICYP to 5HT1B serotonergic receptor sites. Arotinolol serves as an effective antihypertensive agent and is utilized in research related to various cardiovascular and non-cardiovascular diseases. -
5-HT1AR Agonist/α1-Adrenergic Receptor Antagonist
Enciprazine dihydrochloride is an orally active non-benzodiazepine anxiolytic that functions as a 5-HT1A receptor agonist and α1-adrenergic receptor antagonist. This compound demonstrates key biological activity by inducing electroencephalogram changes, characterized by a reduction in δ and θ wave power and an increase in α and fast β wave power. Enciprazine dihydrochloride exhibits anti-aggressive properties, alongside minimal sedative and ataxic effects. It also modulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis, making it a valuable reagent for research into anxiety disorders, generalized anxiety syndrome, and psychosis. -
5-HT1A Receptor Inhibitor
LY 178210 is a selective partial agonist of the 5-HT1A receptor, exhibiting Ki values of 0.67 nM for 5-HT1A and 380 nM for 5-HT1D receptors, thereby demonstrating its specificity. Its minimal activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors makes it a valuable tool in neuropharmacology. Additionally, LY 178210 effectively inhibits forskolin-stimulated cyclase activity, though with lower potency compared to full agonists like 8-OH-DPAT. This compound is significant for studies on serotonergic modulation, as it markedly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the hypothalamus while increasing serum corticosterone concentrations. -
β-adrenoceptor Blocker
Tiprenolol is a selective β-adrenoceptor blocker that primarily targets β-adrenergic receptors. It has demonstrated efficacy in abolishing adrenaline-induced ventricular arrhythmias in canine models exposed to halothane anesthesia. This compound is valuable in pharmacological research related to cardiac function and the study of arrhythmias. -
Antihypertensive Agent
Pelanserin is an orally active antihypertensive agent that primarily functions as a potent 5-HT2 receptor antagonist. It effectively inhibits α-adrenergic receptor activity, showcasing an ED50 value of 0.03 μg/mL. Additionally, Pelanserin demonstrates vasodilatory properties with an ED100 of 5 μg. This compound is valuable for research applications focused on hypertension, proving effective in hypertensive rodent models and renal hypertensive dog breeds. -
Antipsychotic Agent
Melperone hydrochloride is a butyrophenone that functions primarily as an atypical antipsychotic agent. It acts as a multireceptor antagonist, demonstrating binding affinities with Kd values of 102 nM for 5-HT2A, 180 nM for dopamine D2, 180 nM for α1-adrenergic, and 150 nM for α2-adrenergic receptors. While exhibiting weaker interactions with additional receptors, Melperone hydrochloride shows potential as a CYP2D6 inhibitor. This compound is utilized in research for investigating schizophrenia and managing agitation in elderly populations. -
5-HT Receptor
LEK 8841 methanesulfonate is a selective antagonist of the 5-HT2 receptor, demonstrating notable gastrointestinal calming properties. It exhibits strong competitive antagonism towards 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. LEK 8841's superior selectivity compared to other antagonists makes it a valuable reference compound in receptor research. Additionally, studies on structural modifications indicate that LEK 8841 possesses a high affinity for 5-HT2 receptors while exhibiting minimal activity at alpha-adrenergic receptors, enhancing its potential for therapeutic applications in psychopharmacology. -
Mixed Agonist/Antagonist
2-(2-Methoxyphenoxy)ethylamine hydrochloride acts as a mixed agonist and antagonist, primarily targeting the 5-HT1A receptor as a partial agonist and the α1-adrenergic receptor as an antagonist. This reagent exhibits significant potential in studying neurological disorders, particularly in relation to anxiety, depression, and psychosis. Its dual mechanism of action makes it valuable for exploring therapeutic avenues in mental health research. -
D2 Receptor Agonist
(Rac)-Rotigotine serves as a dopamine D2 receptor agonist, exhibiting a multifaceted mechanism of action. It is recognized as a full agonist at dopamine receptors and a partial agonist at the 5-HT1A receptor, while also functioning as an antagonist of the α2B-adrenergic receptor, demonstrating Ki values of 0.71 nM for dopamine D3 and 4-15 nM for D2, D5, D4, and dopamine D1 receptors. This compound is primarily utilized in research focused on neurological disorders, particularly in the context of Parkinson's disease and other dopamine-related pathologies. -
Stable Isotope
(Rac)-Rotigotine-d3 hydrochloride is a deuterium-labeled analog of (Rac)-Rotigotine, primarily acting as a full agonist at dopamine receptors. It also serves as a partial agonist of the 5-HT1A receptor and acts as an antagonist at the α2B-adrenergic receptor, showcasing Ki values of 0.71 nM, 4-15 nM, and 83 nM for the respective targets. This stable isotope is vital for pharmacokinetic studies, isotope labeling experiments, and research related to neuropharmacology. -
5-HT1A Receptor Modulator
Ipsapirone hydrochloride is a selective modulator of the 5-HT1A receptor, functioning primarily as a partial agonist. This compound demonstrates anxiolytic properties, making it relevant for research in anxiety disorders. At elevated concentrations, ipsapirone hydrochloride can also exhibit antagonistic effects on the 5-HT1A receptor and inhibit 5-HT2 and α1-adrenergic receptor activities, expanding its applicability in pharmacological studies of serotonergic and adrenergic signaling pathways. -
Antidepressant Agent
Etoperidone hydrochloride is an orally active antagonist of serotonin and norepinephrine reuptake, primarily functioning as an antidepressant agent. It exhibits Kd values of 36 nM for the 5-HT2 receptor, 38 nM for the α1-adrenergic receptor, 85 nM for the 5-HT1A receptor, and 570 nM for the α2-adrenergic receptor. This compound is utilized in research focused on mood disorders and the neurochemical pathways related to depression. -
α/β-Adrenergic Receptor Blocker
Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker that also functions as a vasodilating β-blocker. This compound exhibits significant potency in inhibiting the binding of the radioligand 125I-ICYP to 5HT1B serotonergic receptor sites. Arotinolol hydrochloride is primarily utilized as an antihypertensive agent in the management of various cardiovascular conditions, in addition to being studied for potential applications in non-cardiovascular diseases. -
Stable Isotope
Paliperidone-d4 is the deuterated form of Paliperidone, a major active metabolite of Risperidone, acting as a dopamine D2 antagonist and 5-HT2A antagonist. This compound also exhibits antagonistic properties at alpha-1 and alpha-2 adrenergic receptors as well as H1-histaminergic receptors. Paliperidone's primary application is in the treatment of schizophrenia, making it valuable for pharmacological research and development of antipsychotic therapies. -
5-HT6 Receptor Agonist
ST1936 is a selective agonist of the 5-HT6 receptor, exhibiting nanomolar affinity with a Ki value of 13 nM for human 5-HT6 receptors. It also demonstrates notable selectivity across related serotonin receptors, with Ki values of 168 nM for 5-HT7 and 245 nM for 5-HT2B. Additionally, ST1936 has moderate affinity for human and rat α2 adrenergic receptors, with a Ki of 300 nM. This compound is valuable for neuroscience research, particularly in studies related to cognitive function and mood disorders. -
Dopamine Receptor Antagonist
Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes. -
Stable Isotope
(R)-Propranolol-d7 is a deuterated derivative of (R)-Propranolol, serving as a stable isotope-labeled compound. This reagent is invaluable for pharmacokinetic studies and metabolic pathway analysis, enabling the tracking of drug metabolism and distribution in biological systems. Researchers can utilize (R)-Propranolol-d7 in studies focused on cardiovascular research, anxiety treatments, and the mechanisms of action associated with beta-adrenergic receptors. -
β1-adrenoceptor Antagonist
Landiolol is a highly selective, ultra-short-acting antagonist of β1-adrenergic receptors. By competitively inhibiting these receptors, Landiolol effectively reduces heart rate and myocardial oxygen demand while minimally affecting cardiac ion channels and exhibiting a weak negative inotropic effect. Its ability to inhibit TNF-α-induced mitochondrial hyperactivity and reactive oxygen species production makes it valuable in models of sepsis, where it can mitigate renal injury. Landiolol is applicable in research involving perioperative tachycardia management and investigations into sepsis-related acute kidney injury. -
Dopamine Receptors Blocker
Trifluoperazine is an antipsychotic agent primarily acting as a blocker of central dopamine receptors. It exhibits significant activity as a potent α1-adrenergic receptor antagonist and a NUPR1 inhibitor, demonstrating anticancer properties. Additionally, Trifluoperazine functions as a calmodulin inhibitor and inhibits P-glycoprotein, contributing to its diverse biological effects. This compound is utilized in research on schizophrenia and shows potential as a reversible inhibitor of influenza virus morphogenesis. -
β-Adrenoceptor Blocker
Propranolol is a non-selective β-adrenoceptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1 and β2 adrenergic receptors, with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol has demonstrated inhibitory activity against [3H]-DHA binding in rat brain membrane preparations, with an IC50 of 12 nM. This compound is commonly employed in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
Fluorescent α1-Adrenergic Antagonist
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist, exhibiting Ki values of 14.5 nM and 43.3 nM for the α1a and α1b adrenergic receptors, respectively. This compound acts as a fluorescent ligand, with excitation and emission wavelengths at 485 nm and 535 nm. BODIPY FL prazosin is valuable for elucidating the subcellular localization and distribution of different α1-adrenoceptor subtypes in various biological contexts. -
β₂-adrenergic receptor Agonist/PDE4 Inhibitor
GS-5759 is a dual-action compound functioning as a β₂-adrenergic receptor agonist and a phosphodiesterase 4 (PDE4) inhibitor. By activating the β₂ receptor, GS-5759 elevates intracellular cAMP levels, resulting in bronchial dilation. Additionally, its inhibition of PDE4 activity decreases cAMP degradation, thereby enhancing anti-inflammatory responses. This compound is relevant for research into respiratory disorders, particularly chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilatory and anti-inflammatory effects in preclinical models. -
Cardiac
UK-1745 is a cardiotonic agent that targets phosphodiesterase III, leading to increased intracellular levels of cyclic adenosine monophosphate (cAMP) in cardiomyocytes. This elevation enhances myocardial contractility while also exhibiting β-adrenergic receptor antagonism, which decreases cardiac oxygen consumption and mitigates calcium overload. Due to these properties, UK-1745 is a valuable tool for research applications focused on congestive heart failure and cardiac function modulation. -
α/β Adrenergic Receptor Blocker
Primidolol is an orally active α/β Adrenergic Receptor blocker that exhibits antihypertensive properties. This compound demonstrates significant antibacterial and antioxidant activities, making it relevant in studies focused on both cardiovascular diseases and infectious processes. Its dual mechanism of action positions Primidolol as a valuable tool for research aimed at understanding the interplay between adrenergic signaling and microbial resistance. -
β2-Drenergic Receptor Agonist
Terbutaline is an orally active β2-adrenergic receptor agonist that effectively stimulates the β2-adrenergic receptors. Its primary biological activity includes bronchodilation, making it relevant for research on asthma symptoms and respiratory disorders. Terbutaline is commonly used in studies investigating the therapeutic effects of β2-agonists in pulmonary conditions. -
β2-Drenergic Receptor Agonist
Terbutaline sulfate is an orally active β2-adrenergic receptor agonist, primarily utilized in the treatment of asthma and other bronchospastic conditions. As an active metabolite of bambuterol, it promotes bronchodilation by relaxing smooth muscle in the airways. This compound is essential for research applications focused on respiratory pharmacology and the therapeutic evaluation of β2-adrenergic systems in asthma symptom management. -
NMDA Receptor Antagonist
Ifenprodil is a noncompetitive antagonist of the NMDA receptor, with a strong affinity for the NR1A/NR2B subunit (IC50 = 0.34 μM) compared to NR1A/NR2A (IC50 = 146 μM). This compound also acts as an α1 adrenergic receptor antagonist and inhibits GIRK channels, reducing basal inward currents. Additionally, Ifenprodil demonstrates antiviral activity against A/H1N1 strains (EC50 = 6.6 µM) and possesses neuroprotective, anticonvulsant, and antinociceptive properties. It is suitable for research in cerebrovascular diseases and peripheral arterial obliterative disease. -
α/β-Adrenergic Receptor Blocker
Arotinolol is a nonselective α/β-adrenergic receptor blocker that also acts as a vasodilating β-blocker. It exhibits significant inhibitory activity against the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is primarily utilized as an antihypertensive agent in the management of various cardiovascular conditions, as well as for certain non-cardiovascular diseases, facilitating research in cardiovascular pharmacology and receptor interaction studies. -
Antipsychotic Agent
Melperone is a butyrophenone class compound that functions primarily as an atypical antipsychotic agent. It acts as a multireceptor antagonist, with binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for the 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. With lower binding affinity for histamine H1 and various serotonin receptors, Melperone also exhibits inhibitory effects on CYP2D6. This compound is valuable for research into schizophrenia and behavioral disturbances in elderly populations.
