Catalog No.
Product Name
Application
Product Information
Citations
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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
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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
- 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
- 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. - Piribedil D8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
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vasopressor/antihypotensive agent
Midodrine D6 hydrochloride is deuterium labeled Midodrine, which is a vasopressor/antihypotensive agent. - Indoramin D5 is deuterium labeled Indoramin, which is a piperidine antiadrenergic agent.
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β1-selective adrenergic receptor agonist
Norepinephrine hydrochloride (Levarterenol hydrochloride; L-Noradrenaline hydrochloride) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. - Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
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β-adrenoceptor antagonist
(+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. -
beta-adrenoceptor agonist
Bambuterol ((??)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline. -
β-adrenergic receptor (βAR) antagonist
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol 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.
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β3-adrenergic receptor agonist
Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. -
β2-adrenergic receptor agonist
Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol. -
A2AR/ENT1 agonist
A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1. -
dual NE/DA transporter inhibitor
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively. -
α2-adrenoceptor antagonist
Atipamezole is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM. -
muscarinic receptor antagonist and β2-adrenoceptor agonist
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
