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β2-AR agonist
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries.- Ana Rubio, .et al. , Drug Test Anal, 2023, Jul 31 PMID: 37525530
- Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
- Antonia Donat, .et al. , iScience, 2023, Aug 29;26(10):107761 PMID: 37720081
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Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
- Nebivolol hydrochloride is t a highly selective antagonist of the β1-adrenoceptor (Ki = 0.88 nM, β2-adrenoceptor Ki = 48 nM).
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14 PMID: 33330842
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β3 adrenergic receptor activator
Mirabegron is a potent bladder relaxant and reagent for diabetes remedy.- Havard Fjelltveit, .et al. , Auton Neurosci, 2025, Apr:258:103253 PMID: 39977963
- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
- Bhavik Patel, .et al. , Pharmacol Res Perspect, 2020, 8 (1), e00564 PMID: 32030913
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β-adrenergic blocker
S(-)-Propranolol Hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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β adrenoceptor agonist
Isoprenaline or isoproterenol is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
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β1-selective adrenergic receptor agonist
Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
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α1-adrenergic receptor agonist
Phenylephrine is a selective α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure.- Johanna Stenqvist, .et al. , Auton Neurosci, 2024, Jun 11:254:103194 PMID: 38875740
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α2C antagonist
JP 1302 2HCl is a potent and selective α2C antagonist.- Junya Maruoka, .et al. , Int J Neuropsychopharmacol, 2026, Apr 6;29(4):pyag007 PMID: 41717785
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H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150 PMID: 34334499
- Doxazosin mesylate, a quinazoline compound, is an α1-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).
- L Klem, .et al. , Psychopharmacology (Berl), 2023, Aug;240(8):1629-1650 PMID: 37329343
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β2 adrenergic receptor antagonist
ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.- Moon Jain, .et al. , Tropical Journal of Pharmaceutical Research, 2020, Vol. 19 No. 4
- Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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alpha1/beta adrenergic receptors antagonist
Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Clenbuterol Hydrochloride is a sympathomimetic β2-adrenoceptor agonist that has been used as a bronchodilator in the treatment of pulmonary diseases such as asthma. At higher doses, clenbuterol acts as an anabolic steroid, favoring skeletal muscle protein synthesis at the expense of fat deposition.
- Younian Xu, .et al. , J Inflamm Res, 2022, Jan 14;15:295-309 PMID: 35058704
- Alfuzosin (provided as the hydrochloride salt) is an α1 receptor antagonist used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
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β1 adrenergic receptor blocker
Bisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type β1 adrenergic receptor blocker. -
Alpha adrenergic agonist
Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist. -
Adrenergic Receptor agonist
Detomidine is a sedative with analgesic properties. α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters. -
Adrenoceptors agonist
Dobutamine is a direct-acting agent whose primary activity results from stimulation of the β1-adrenoceptors of the heart, increasing contractility and cardiac output. -
noradrenalin re-uptake inhibitor
Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor. - Naftopidil (Flivas) is a selective α1-adrenergic receptor antagonist or alpha blocker with a Ki of 58.3 nM.
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5-HT1A and α1-adrenergic receptor antagonist
Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. -
alpha-1 adrenergic agonist
Oxymetazoline is a selective alpha-1 agonist and partial alpha-2 agonist topical decongestant, used in the form of Oxymetazoline hydrochloride. -
α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
α2 adrenergic agonist
Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist. -
Adrenergic Receptor agonist
Salbutamol sulfate (Albuterol) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. -
α1-adrenoceptor antagonist
Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers). -
Adrenergic Receptor agonist
Synephrine (Oxedrine) is an amine compound commonly used for weight loss. -
alpha2-Adrenergic receptor agonist
Flutonidine is an alpha2-Adrenergic receptor agonist. -
beta-adrenoceptor antagonist
DL 071-IT is a potent non-selective beta-adrenoceptor antagonist. . -
Adrenergic Receptor Antagonist
Propranolol hydrochloride is a nonselective β-adrenergic receptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1AR and β2AR receptors, with Ki values of 1.8 nM and 0.8 nM, respectively, and inhibits [3H]-DHA binding in rat brain membranes with an IC50 of 12 nM. This reagent is widely used in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
Antihypertensive Agent
Indoramin is an orally active antihypertensive agent targeting the α1A-adrenoceptor. This compound works by selectively blocking α1-adrenoceptors, leading to vasodilation and a reduction in blood pressure. Indoramin is utilized in cardiovascular research to study blood pressure regulation and the mechanisms of hypertension. -
β2-Adrenergic Receptor Agonist
Levalbuterol hydrochloride is a potent β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. It exhibits enhanced bronchodilator activity, making it a valuable reagent in respiratory research. Primarily, it is utilized in studies focusing on the treatment of chronic obstructive pulmonary disease (COPD) and other airway obstruction disorders. -
α-adrenergic Receptor Agonist
Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research. -
β1-Adrenergic Blocker
Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker, primarily targeting the β1-adrenergic receptors. This compound demonstrates significant antiarrhythmic properties and is effective in mitigating post-resuscitation myocardial dysfunction. Additionally, esmolol hydrochloride inhibits aldose reductase activity, reducing advanced glycation end products and enhancing fibroblast migration, which contributes to improved diabetic wound healing. It serves as a valuable tool for research into cardiac diseases, including arrhythmias and diabetic foot ulcers. -
β2-adrenergic receptor Antagonist
Zenidolol is a selective β2-adrenergic receptor antagonist, exhibiting a Ki value of 0.7 nM for the β2 receptor, alongside higher Ki values for β1 and β3 receptors at 49.5 nM and 611 nM, respectively. This compound demonstrates significant antitumor activity by inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway in tumor cells. Additionally, Zenidolol has a unique vasodilatory effect specific to pulmonary vessels in mouse models and can serve as an intraocular pressure-lowering agent in ophthalmic research applications. -
Stable Isotope
N-(Phenylacetyl-d5)glycine is a deuterated form of phenylacetylglycine, functioning as a stable isotope. This compound serves as a gut microbial metabolite that can activate the beta-2 adrenergic receptor (β2AR). Its biological activity includes providing protective effects against cardiac injury induced by ischemia and reperfusion, making it valuable for research in cardiac health and metabolic studies. -
Stable Isotope
D-Mannitol-13C6 is a stable isotope-labeled form of D-Mannitol, targeting metabolic pathways through its role as an osmotic agent. This compound is utilized in various research applications, including studies on calcium and magnesium absorption, cecal fermentation, and the modulation of insulin sensitivity. D-Mannitol has been shown to promote the browning of white adipose tissue by activating the β3-adrenergic receptor, which can lead to enhanced thermogenesis and potential reductions in blood glucose levels. Additionally, it is employed in plant cell culture to maintain osmotic balance and protect cellular integrity. -
Stable Isotope
D-Mannitol-13C is a stable isotope-labeled derivative of D-Mannitol. This compound serves as a valuable osmotic diuretic and is utilized in various research applications, including the study of calcium and magnesium absorption and retention through cecal fermentation. D-Mannitol is known to promote brown adipose tissue formation, enhance insulin sensitivity, and lower blood glucose levels by activating the β3-adrenergic receptor, leading to the conversion of white fat cells into brown fat cells. Additionally, it is employed to maintain osmotic pressure in plant cell cultures, aiding in cellular protection during physiological manipulation. -
Stable Isotope
Perphenazine-d4 is a deuterated derivative of Perphenazine, a typical antipsychotic agent primarily inhibiting the 5-HT2A receptor, alpha-1A adrenergic receptor, dopamine receptor D2/D3, D2L receptor, and histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, allowing for the precise tracking of Perphenazine metabolism and distribution in biological systems. Perphenazine-d4 is essential for researchers focusing on neuropharmacology and drug interaction studies involving antipsychotic medications. -
Stable Isotope
D-Mannitol-2-13C is a stable isotope-labeled derivative of D-Mannitol. This 13C-labeled compound plays a critical role in metabolic studies, particularly in understanding carbohydrate metabolism and energy homeostasis. D-Mannitol serves as an osmotic diuretic, promotes the absorption of minerals, enhances brown adipose tissue formation, and demonstrates potential for reducing blood glucose levels through β3-adrenergic receptor activation. It is frequently employed in cell culture applications to maintain osmotic pressure and protect cells, particularly when cell walls are compromised. -
β2AR Activator
Phenylacetylglycine is a gut microbial metabolite that acts as a β2-adrenergic receptor (β2AR) activator. It has demonstrated protective effects against cardiac injury resulting from ischemia/reperfusion. This compound is significant for research into cardiovascular health and the role of microbiota in modulating cardiac responses. -
Adrenergic Receptor Agonist
Tizanidine hydrochloride is a selective α2-adrenoceptor agonist that serves as an effective skeletal muscle relaxant. It primarily promotes muscle relaxation by reducing the presynaptic release of excitatory amino acids, such as glutamate and aspartate, within spinal cord interneurons. In addition to its central effects, Tizanidine hydrochloride demonstrates potential anti-cancer properties by inhibiting lung cancer cell proliferation, migration, and invasion, while promoting apoptosis via the modulation of the AKT and Wnt3a/β-catenin signaling pathways. This compound is clinically relevant for the management of spasticity associated with conditions like multiple sclerosis, stroke, and spinal cord injury. -
Adrenergic Receptor Agonist
Tizanidine is a selective α2-adrenoceptor agonist that functions primarily as a skeletal muscle relaxant. It exerts muscle relaxation effects by inhibiting the release of excitatory amino acids, thereby modulating synaptic activity in the spinal cord. Additionally, Tizanidine demonstrates anti-cancer properties by inhibiting proliferation, migration, and invasion of lung cancer cells, as well as inducing apoptosis through the upregulation of Nischarin and suppression of the AKT and Wnt3a/β-catenin pathways. This compound is utilized clinically for the management of spasticity associated with conditions such as multiple sclerosis, stroke, and spinal cord injury.

