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D3 Receptor Ligand
Dopamine D3 receptor ligand-2 is a selective antagonist targeting the D3 dopamine receptor, exhibiting a Ki of 11.4 nM. This compound demonstrates high selectivity, showing minimal affinity for the D2 receptor with a Ki of 1228 nM. It is valuable for studies related to neurological disorders, addiction research, and the exploration of dopaminergic pathways. -
Dopamine Receptor Inhibitor
Opromazine hydrochloride is a dopamine receptor inhibitor known for its sedative and antiemetic effects. It primarily reduces dopaminergic activity by blocking dopamine receptors in the brain, making it useful in the treatment of psychiatric disorders such as schizophrenia and psychosis. Additionally, studies have investigated its metabolites through various microsomal enzymes, highlighting differences in formation rates and the variability of drug-metabolizing enzymes in human liver and placenta microsomes, which is essential for understanding its pharmacokinetic profile. -
D3/D2 Receptor Antagonist
PF-4363467 is a selective antagonist of the dopamine D3 and D2 receptors, demonstrating a Ki value of 3.1 nM for D3R and 692 nM for D2R. This compound effectively reduces opioid drug-seeking behavior while minimizing the associated side effects typically linked to D2 receptor antagonism. PF-4363467 is valuable for research applications focused on addiction and neuropharmacology, providing insights into dopaminergic modulation in therapeutic contexts. -
D2R/SSTR2 Agonist
Onzigolide is a chimeric compound that acts as a potent agonist at dopamine type 2 (D2R) and somatostatin type 2 (SSTR2) receptors. This dual receptor activation may play a crucial role in modulating neuroendocrine and neurological functions. It is particularly relevant in research focused on neuropsychiatric disorders and endocrine-related conditions, contributing to the understanding of receptor interactions and their implications in therapeutic contexts. -
D4R Antagonist
D4R antagonist-2 is a selective antagonist of the D4 dopamine receptor, exhibiting an IC50 of 6.52 µM. This compound demonstrates favorable in vitro pharmacokinetic properties and effective brain penetration. D4R antagonist-2 is suitable for research applications related to Parkinson's disease and other neurological disorders. -
Antipsychotic Agent
Pipotiazine palmitate is a dopamine receptor antagonist primarily used as an antipsychotic agent. As a long-acting phenothiazine derivative, it is suitable for intramuscular administration, providing sustained therapeutic effects. This compound is valuable in research applications focused on mental illnesses, particularly schizophrenia, facilitating studies into its neuropharmacological effects and treatment strategies. -
Dopamine D2 Receptor Agonist
(-)-IHCH7041 is a selective and orally active agonist of the dopamine D2 receptor, exhibiting a Ki value of 22.44 nM. It effectively activates the Gαi1 protein and β-arrestin2 signaling pathways with EC50 values of 1.38 nM and 2.75 nM, respectively. This compound has demonstrated potential in enhancing cognitive function and memory capacity, making it valuable for research into neurological disorders, including Alzheimer's disease. -
D-2 Dopamine Receptor Agonist
RU-24213 hydrochloride is a selective agonist for the D-2 dopamine receptor, known to modulate dopaminergic signaling. Additionally, it acts as an antagonist at the kappa-opioid receptor, contributing to its pharmacological profile. This compound has been observed to induce stereotyped behaviors, making it valuable for research in neuropharmacology and the exploration of dopamine-related conditions. -
α1-adrenergic Receptor Antagonist
Butanserin is a selective antagonist of the α1-adrenergic receptor, primarily utilized in cardiovascular research. This compound modulates adrenergic signaling pathways, making it valuable for investigating the role of α1-adrenoceptors in various cardiovascular conditions. Its potency and specificity support its application in studies aimed at understanding hypertension and heart failure mechanisms. -
α2 Receptor Antagonist
Napitane mesylate is a selective antagonist of presynaptic α2 adrenergic receptors, impacting norepinephrine reuptake inhibition. This compound demonstrates significant antidepressant activity, making it relevant for research in mood disorders and neuropharmacology. It is utilized to explore the modulation of noradrenergic neurotransmission and its effects on depressive states. -
α2-adrenergic Agonist
Detomidine is a potent α2-adrenergic agonist characterized by its imidazole structure. Its primary mechanism involves the activation of α2-adrenergic receptors, leading to significant analgesic effects in a dose-dependent manner. This compound is commonly utilized in veterinary medicine for sedation and analgesia, as well as in research applications focused on examining α2-adrenergic signaling pathways. -
ADRB2 Agonist
Indacaterol xinafoate is a potent β2-adrenergic receptor agonist known for its long-acting bronchodilatory effects. By inhibiting NF-κB activity in a β-arrestin2-dependent manner, it not only improves lung function but also mitigates further lung damage, making it relevant in the context of chronic obstructive pulmonary disease (COPD). This compound serves as a valuable tool for research into asthma and related respiratory disorders. -
Stable Isotope
Tetrahydrozoline-d4 hydrochloride is a deuterium-labeled form of Tetrahydrozoline hydrochloride, an α-adrenergic agonist that targets α-adrenergic receptors to induce vasoconstriction. This stable isotope is utilized in research applications focusing on nasal and conjunctival congestion. Its unique isotopic labeling allows for enhanced tracking and quantification in various biochemical studies. -
β-adrenergic Blocker
Bunitrolol hydrochloride is a β-adrenergic blocker known for its high affinity for β-adrenergic receptors and its significant antagonist activity. It also exhibits weak α1-blocking effects. This compound is primarily utilized in research related to cardiovascular diseases, including hypertension and angina pectoris, and is applicable in studies of placental transport. -
Silodosin Racemate
(Rac)-Silodosin is a racemic mixture that targets the α1A-adrenergic receptor (α1A-AR) as a potent and selective antagonist. This compound is primarily utilized in research related to urology and the treatment of benign prostatic hyperplasia (BPH), contributing to the understanding of adrenergic signaling pathways. Its oral bioavailability makes it a significant candidate for pharmacological studies focusing on α1-adrenergic receptor modulation. -
Adrenergic Receptor
2-(4-(2-Hydroxy-3-(isopropyl(nitroso)amino)propoxy)phenyl)acetamide targets adrenergic receptors and is recognized as a genotoxic derivative of Atenolol. This compound has been shown to induce DNA fragmentation in rat hepatocytes at concentrations between 0.1 and 1 mM, making it a valuable tool for studying genotoxic mechanisms and the effects of adrenergic signaling in cellular contexts. Its applications extend to research involving DNA damage and repair pathways. -
Adrenergic Receptor Agonist
Octopamine is a biogenic monoamine that functions as an adrenergic receptor agonist, primarily targeting alpha2-adrenoceptors. It serves as a neurohormone, neuromodulator, and neurotransmitter in invertebrates. In vitro studies demonstrate that Octopamine enhances glycogenolysis, glycolysis, oxygen uptake, and gluconeogenesis, along with increasing portal perfusion pressure. This compound is valuable for research in neurobiology, metabolism, and cardiovascular studies. -
Adrenergic Receptor Inhibitor
Cetamolol hydrochloride acts as a potent β1-adrenergic receptor inhibitor, exhibiting intrinsic sympathomimetic activity and cardioselectivity. It demonstrates a prolonged inhibitory effect on heart rate and myocardial contractility at low to moderate doses, making it a valuable reagent for cardiovascular research. Its unique profile allows for exploration in studies evaluating hypertension, arrhythmias, and other cardiac conditions. -
α2 Agonist
Apraclonidine dihydrochloride is a selective α2 adrenergic receptor agonist with weak activity at α1 receptors. This compound is primarily used to reduce intraocular pressure (IOP) in various ophthalmic conditions. Its effectiveness in lowering IOP makes it a valuable tool in the study of glaucoma and other eye disorders. -
β2-adrenergic Receptor Agonist
Trantinterol hydrochloride is a potent agonist of the β2-adrenergic receptor, demonstrating significant efficacy in bronchial relaxation. It serves as a valuable tool in the investigation of asthma and other respiratory conditions. This compound may aid in understanding the mechanisms of bronchial hyperreactivity and support the development of therapeutic strategies targeting β2-adrenergic pathways. -
Adrenergic Receptor Agonist
BFE-55 is a derivative of befunolol that acts as a β-adrenergic receptor partial agonist. This compound exhibits significant biological activity by modulating adrenergic signaling pathways. BFE-55 can be utilized in research focused on cardiovascular dynamics and therapeutic interventions targeting adrenergic receptors. -
Adrenoreceptor Agonist
Colterol hydrochloride is an agonist of the adrenergic receptors, demonstrating significant affinity for the β1-adrenoreceptor and β2-adrenoreceptor, with respective IC50 values of 645 nM and 147 nM. It exhibits potent bronchodilator activity, making it valuable for research applications related to respiratory conditions. This compound can be utilized in studies investigating cardiovascular responses and airway reactivity, contributing to the understanding of adrenergic signaling pathways. -
Adrenergic Receptor Agonist
Amibegron is a selective β3-adrenergic receptor agonist, demonstrating an EC50 of 3.5 nM for activation of β-adrenoceptors in rat colon tissues. This compound exhibits notable anxiolytic and antidepressant properties, making it a valuable tool for research in neuropharmacology and the study of mood disorders. Its specificity for β3-adrenergic receptors lends it potential applications in exploring metabolic and cardiovascular responses. -
β3-adrenergic Receptor Agonist
SB251023 is a selective β3-adrenergic receptor agonist, exhibiting pEC50 values of 7.14 for the β3a and 6.91 for the β3b receptor subtypes. This compound effectively modulates intracellular cyclic AMP levels and influences extracellular acidification rates (EAR) in cellular systems. SB251023 is relevant for research into cardiovascular diseases and metabolic disorders, providing insights into the therapeutic potential of β3-adrenergic signaling in related pathologies. -
Drug Metabolite
Deacetylmoxisylyte is an orally active drug metabolite derived from the prodrug Moxisylyte, primarily targeting alpha-1 and alpha-2 adrenoceptors. It demonstrates significant affinity and selectivity in rabbit corpus cavernosum and urethra tissues, with IC50 values of 400 nM and 1200 nM, respectively. This compound is valuable in pharmacological research focused on understanding adrenergic receptor interactions and their physiological effects. -
Adrenergic Receptor Antagonist
Phenoprolamine hydrochloride is an adrenergic α1 receptor antagonist known for its potent antihypertensive properties. In addition to lowering blood pressure, it exhibits neuroprotective and cardioprotective activities. This compound also inhibits the enzymatic activity of CYP2D and CYP3A, resulting in the down-regulation of their mRNA transcription, which may have implications in drug metabolism studies and cardiovascular research. -
Metabolite
4-Hydroxy xylazine O-glucuronide lithium is a metabolite derived from the α2-adrenergic receptor agonist xylazine. This compound serves as an important biochemical marker, aiding in the study of xylazine metabolism and its physiological effects. It can be synthesized from xylazine through the intermediate metabolite 4-hydroxy xylazine and is valuable in pharmacokinetic and toxicological research applications. -
β1/β2 Adrenergic Receptor Antagonist
4-Hydroxypropranolol-d7 hydrochloride is a deuterated derivative of 4-Hydroxypropranolol, functioning as a potent β1/β2 adrenergic receptor antagonist. It exhibits equivalent potency to its parent compound Propranolol, with pA2 values of 8.24 and 8.26 for β1 and β2 receptors, respectively. This compound is characterized by its intrinsic sympathomimetic activity, membrane stabilizing effects, and significant antioxidant properties, making it valuable for various biochemical and pharmacological research applications. -
α-Adrenoreceptor Antagonist
Taprizosin is an α-adrenoreceptor antagonist that selectively inhibits the activity of α1-adrenergic receptors. It has demonstrated efficacy in modulating vascular smooth muscle contraction and influencing blood pressure regulation. This compound is primarily utilized in cardiovascular research, particularly in studies focused on hypertension and related disorders. -
α-2B adrenergic receptor Agonist
AGN-201781 is an orally active agonist of the α-2B adrenergic receptor. This compound exhibits significant biological activity in modulating adrenergic signaling pathways, making it a valuable tool for research into neuropathic pain mechanisms and potential therapeutic interventions. Its specificity for the α-2B receptor supports investigations into pain management and related neurological studies. -
α1-Adrenoceptor Ligand
CHIR-2279 is a high-affinity ligand for the α1-adrenergic receptor, exhibiting a binding affinity characterized by a Ki value of 5 nM. This compound serves as a valuable tool for investigating the α1-adrenoceptor signaling pathways and has potential applications in drug development aimed at cardiovascular and other relevant disorders. -
β-Adrenergic Receptor Agonist
Hexoprenaline sulfate is a selective β-adrenergic receptor agonist that promotes bronchodilation. This compound enhances adenylate cyclase activity, leading to an increased uptake of 14C-Aminopyrine. Additionally, Hexoprenaline sulfate exhibits anti-inflammatory and anti-infective properties, while also demonstrating effects on placental weight and blood flow. It is applicable in research areas including inflammation, immunology, infection, endocrinology, and the study of neurological diseases, such as asthma, chronic bronchitis, sepsis, and organophosphorus compound intoxication. -
Adrenergic Receptor Antagonist
RU 52583 is an oral bioactive antagonist of the alpha-2 adrenergic receptor. This compound has been shown to enhance cognitive function in rodent models with septohippocampal system damage, indicating its potential utility in studying cognitive disorders. Its pharmacological profile may provide insights into the modulation of adrenergic signaling in various neurological research applications. -
Stable Isotope
Solabegron-d8 is a deuterium-labeled derivative of Solabegron, a selective β3-adrenergic receptor agonist. It effectively stimulates cAMP accumulation in Chinese hamster ovary cells expressing human β3-adrenergic receptors, exhibiting an EC50 value of 22 nM. This compound is primarily utilized in research focused on the treatment of overactive bladder and irritable bowel syndrome, allowing for the investigation of β3-adrenergic signaling pathways in various biological contexts. -
Stable Isotope
Lofexidine-d4 is a deuterium-labeled derivative of Lofexidine (hydrochloride), a selective α2-adrenergic receptor agonist. This compound is primarily employed in research related to opioid withdrawal by mimicking the activity of Lofexidine in biological assays. The stable isotope labeling enables precise tracking in pharmacokinetic studies and helps in elucidating the pharmacological properties of opioid withdrawal treatments. -
β3-adrenergic Receptor Agonist
N-5984 hydrochloride is a potent and selective agonist of the β3-adrenergic receptor. This compound exhibits significant biological activity in promoting lipolysis and thermogenesis, making it a valuable tool for research on obesity and diabetes mellitus. Its specificity for the β3-adrenergic receptor allows for targeted investigations into metabolic regulation and potential therapeutic applications in metabolic disorders. -
β-Adrenergic Receptor Antagonist
Falintolol is a selective β-adrenergic receptor antagonist that exhibits potential therapeutic effects in ocular conditions, particularly in the management of glaucoma. By inhibiting β-adrenergic receptor activity, it effectively reduces intraocular pressure, thereby facilitating research into novel treatment strategies for this prevalent eye disease. This compound is valuable for exploring the role of adrenergic signaling in ocular health and disease. -
β-Adrenergic Receptor Inhibitor
Bufetolol is a selective β-adrenergic receptor inhibitor that modulates cardiac activity by decreasing the maximum rate of depolarization during action potentials. Its antiarrhythmic properties make it a valuable tool for research into the mechanisms of cardiac rhythm disorders. Bufetolol is utilized in studies aimed at exploring therapeutic strategies for arrhythmias and related cardiovascular conditions. -
α2 Adrenergic Receptor Antagonist
Org 6906 is an α2 Adrenergic Receptor antagonist that promotes monoaminergic neurotransmission by inhibiting the reuptake of noradrenaline, dopamine, and serotonin. With a pKi value of 6.3, Org 6906 demonstrates significant antidepressant activity, making it a valuable tool for research into neurological disorders. This compound's mechanisms provide insight into the modulation of neurotransmitter systems and their implications for mental health therapies. -
Adrenergic Receptor
Bremazocine is a potent agonist of the kappa opioid receptor, demonstrating significant analgesic activity. It exerts its effects by enhancing the release of endogenous norepinephrine, leading to peripheral analgesia. Additionally, Bremazocine interacts with adenosine receptors, further contributing to its analgesic properties. Its peripheral analgesic effects are dose-dependent and may be influenced by nonselective α(2) adrenergic receptor antagonists, indicating a mechanism involving norepinephrine pathways. This compound is suitable for research applications focused on pain modulation and neuropharmacology. -
β2-adrenergic Receptor Agonist
Carbuterol hydrochloride is a selective β2-adrenergic receptor agonist that primarily targets bronchial smooth muscle, demonstrating significant bronchodilatory and anti-allergic properties. This compound effectively inhibits the immunologically induced release of histamine and slow-reacting substance of anaphylaxis, thereby mitigating allergic responses. Additionally, it exhibits mild β1-mediated cardiac stimulation and is pertinent for research involving respiratory and immune-related conditions, such as asthma and allergic disorders. -
Adrenergic Receptor Antagonist
Pargolol is a selective β-adrenergic receptor antagonist. It effectively inhibits β-receptor-mediated signaling pathways, thereby regulating cardiovascular responses. Pargolol is utilized in research focused on cardiovascular pharmacology, hypertension, and the role of adrenergic signaling in various physiological processes. Its mechanism is valuable for studying the therapeutic effects of β-blockade in preclinical models. -
Stable Isotope
(rac)-Dobutamine-d4 hydrochloride is a stable isotope-labeled form of the synthetic catecholamine Dobutamine hydrochloride, which primarily targets β1-adrenergic receptors (β1-AR) with lower affinity for α1-adrenergic (α1-AR) and β2-adrenergic receptors (β2-AR). This compound is known for its ability to enhance cardiac output and ameliorate conditions of hypoperfusion. It serves as a valuable tool in pharmacological research, particularly in studies focused on cardiovascular function and receptor activity. -
Adrenergic Receptor Agonist
Methylhexanamine hydrochloride is an adrenergic receptor agonist that functions as a potent vasoconstrictor. This compound primarily acts to alleviate nasal congestion by inducing vasoconstriction in the nasal mucosa when administered via inhalation. Its properties make it a valuable tool for research into respiratory therapies and the modulation of vascular responses. -
Adrenergic Receptor Agonist
A-61603 (free base) is a potent agonist of adrenergic receptors, specifically targeting α1 and α2 subtypes. This compound significantly reduces carotid artery conductance in anesthetized pig models, demonstrating a pEC50 of 7.25. A-61603 (free base) serves as an effective tool for investigating adrenergic signaling pathways and their physiological implications in cardiovascular research. -
β2-adrenergic Receptor Agonist
Clorprenaline-d7 is a deuterium-labeled derivative of Clorprenaline, which functions as a selective agonist for the β2-adrenergic receptor. This compound facilitates bronchial expansion and is significant in the investigation of asthma and respiratory disorders. It is valuable for research applications focusing on pulmonary function, receptor pharmacology, and the development of bronchodilator therapies. -
Indacaterol S-enantiomer
(S)-Indacaterol is the S-enantiomer of Indacaterol, functioning as an ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. This compound exhibits potent bronchodilatory activity, making it a valuable resource in respiratory research, particularly for conditions such as asthma and chronic obstructive pulmonary disease (COPD). Its prolonged duration of action supports studies aimed at understanding and developing new therapeutic strategies targeting β2 adrenergic pathways. -
α2-Adrenergic Receptor Antagonist
Fipamezole hydrochloride is a potent α2-adrenergic receptor antagonist, exhibiting Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C receptors, respectively. This compound functions as an anti-dyskinetic agent, making it valuable for research into Parkinson's disease. Its selective action on α2-adrenergic receptors offers insights into the modulation of dopaminergic activity and potential therapeutic strategies for movement disorders. -
Stable Isotope
Phentolamine-d4 hydrochloride is a deuterated form of Phentolamine hydrochloride, a reversible and non-selective inhibitor of α1 and α2 adrenergic receptors. This compound is utilized primarily for its vasodilatory effects, which reduce peripheral vascular resistance. Phentolamine-d4 hydrochloride is valuable in research applications related to pheochromocytoma-induced hypertension, heart failure, and erectile dysfunction, providing insights into adrenergic receptor modulation in these conditions. -
Stable Isotope
Mabuterol-d9 hydrochloride is a deuterium-labeled form of Mabuterol hydrochloride, targeting the beta-2 adrenergic receptor (ADRB2) as a selective agonist. This compound exhibits the ability to inhibit cellular proliferation and reduce PDGF-BB-induced increases in intracellular calcium levels. Additionally, Mabuterol hydrochloride downregulates the expression of key proteins such as Drp-1, cyclin D1, and PCNA, while promoting the expression of Mfn-2. This reagent is valuable for research involving cellular signaling, proliferation, and metabolic regulation.

