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Results for "

2 Adrenergic Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (187) Serpin (1) 5-HT Receptor (39) AAK1 (2) Adenosine Receptor (1) Adenylate Cyclase (1) Akt (8) Aldose Reductase (2) Amyloid-β (1) Androgen Receptor (1) AP-1 (1) Apoptosis (23) Arrestin (1) Autophagy (19) Bacterial (5) Bcl-2 Family (4) Beta-secretase (2) Calcium Channel (16) CaMK (5) Casein Kinase (2) Caspase (4) Cholinesterase (ChE) (1) Cytochrome P450 (8) Dopamine Receptor (20) Dopamine Transporter (5) Drug Derivative (1) Drug Metabolite (2) Endogenous Metabolite (9) Environmental Pollutants (1) ERK (2) GABA Receptor (5) Glucocorticoid Receptor (1) GnRH Receptor (2) GPR109A (1) GSK-3 (1) HIF/HIF Prolyl-Hydroxylase (2) Histamine Receptor (14) Histone Methyltransferase (1) iGluR (9) Imidazoline Receptor (3) Influenza Virus (8) Integrin (1) Isotope-Labeled Compounds (22) LXR (2) mAChR (12) MAP3K (2) MDM-2/p53 (2) MetAP (2) mGluR (1) Mitophagy (2) MMP (6) Molecular Glues (1) Monoamine Oxidase (5) Monoamine Transporter (1) mTOR (2) N-myristoyltransferase (1) nAChR (3) NADPH Oxidase (1) Neurokinin Receptor (2) NF-κB (9) NO Synthase (1) Nuclear Hormone Receptor 4A/NR4A (1) Opioid Receptor (8) P-glycoprotein (5) P2X Receptor (2) p38 MAPK (2) Parasite (2) Phosphatase (2) Phosphodiesterase (PDE) (5) PI3K (8) PKC (2) Potassium Channel (11) Prostaglandin Receptor (1) PROTACs (1) Proteasome (1) Reactive Oxygen Species (ROS) (5) Reference Standards (37) ROS Kinase (2) Serotonin Transporter (9) Sigma Receptor (2) Sodium Channel (9) Taste Receptor (1) Tau Protein (1) Trk Receptor (5) Vasopressin Receptor (1)
By Research Areas:	Cancer (40) Cardiovascular Disease (88) Endocrinology (61) Infection (11) Inflammation/Immunology (47) Metabolic Disease (24) Neurological Disease (100)

By Targets:

Adrenergic Receptor (187)

Serpin (1)

5-HT Receptor (39)

AAK1 (2)

Adenosine Receptor (1)

Adenylate Cyclase (1)

Akt (8)

Aldose Reductase (2)

Amyloid-β (1)

Androgen Receptor (1)

AP-1 (1)

Apoptosis (23)

Arrestin (1)

Autophagy (19)

Bacterial (5)

Bcl-2 Family (4)

Beta-secretase (2)

Calcium Channel (16)

CaMK (5)

Casein Kinase (2)

Caspase (4)

Cholinesterase (ChE) (1)

Cytochrome P450 (8)

Dopamine Receptor (20)

Dopamine Transporter (5)

Drug Derivative (1)

Drug Metabolite (2)

Endogenous Metabolite (9)

Environmental Pollutants (1)

ERK (2)

GABA Receptor (5)

Glucocorticoid Receptor (1)

GnRH Receptor (2)

GPR109A (1)

GSK-3 (1)

HIF/HIF Prolyl-Hydroxylase (2)

Histamine Receptor (14)

Histone Methyltransferase (1)

iGluR (9)

Imidazoline Receptor (3)

Influenza Virus (8)

Integrin (1)

Isotope-Labeled Compounds (22)

LXR (2)

mAChR (12)

MAP3K (2)

MDM-2/p53 (2)

MetAP (2)

mGluR (1)

Mitophagy (2)

MMP (6)

Molecular Glues (1)

Monoamine Oxidase (5)

Monoamine Transporter (1)

mTOR (2)

N-myristoyltransferase (1)

nAChR (3)

NADPH Oxidase (1)

Neurokinin Receptor (2)

NF-κB (9)

NO Synthase (1)

Nuclear Hormone Receptor 4A/NR4A (1)

Opioid Receptor (8)

P-glycoprotein (5)

P2X Receptor (2)

p38 MAPK (2)

Parasite (2)

Phosphatase (2)

Phosphodiesterase (PDE) (5)

PI3K (8)

PKC (2)

Potassium Channel (11)

Prostaglandin Receptor (1)

PROTACs (1)

Proteasome (1)

Reactive Oxygen Species (ROS) (5)

Reference Standards (37)

ROS Kinase (2)

Serotonin Transporter (9)

Sigma Receptor (2)

Sodium Channel (9)

Taste Receptor (1)

Tau Protein (1)

Trk Receptor (5)

Vasopressin Receptor (1)

By Research Areas:

Cancer (40)

Cardiovascular Disease (88)

Endocrinology (61)

Infection (11)

Inflammation/Immunology (47)

Metabolic Disease (24)

Neurological Disease (100)

231

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Adrenergic Receptor Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0193A

Prazosin hydrochloride 15+ Cited Publications	Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology Cancer
Prazosin hydrochloride is a well-tolerated, CNS-active *α1-adrenergic* receptor** antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC₅₀ of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively .

HY-100543

Zenidolol Maximum Cited Publications 45 Publications Verification ICI-118551	Adrenergic Receptor Apoptosis Caspase Bcl-2 Family HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Zenidolol (ICI-118551) is a selective *β2-adrenergic* receptor antagonist with K_i** values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research .

HY-B0661

Tamsulosin 2 Publications Verification (R)-(-)-YM12617 free base; LY253351 free base	Adrenergic Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .

HY-119706

Barbadin 15+ Cited Publications	Apoptosis Arrestin	Others
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC₅₀ values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis .

HY-B0478A

Trazodone 5+ Cited Publications AF-1161 free base	5-HT Receptor Serotonin Transporter Histamine Receptor Adrenergic Receptor	Neurological Disease
Trazodone (AF-1161 free base) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and *a2-adrenergic* receptors and histamine H1 receptors**, with minimal anticholinergic effects .

HY-B0532

Trifluoperazine 5+ Cited Publications	Dopamine Receptor Adrenergic Receptor P-glycoprotein CaMK Influenza Virus Autophagy	Neurological Disease
Trifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent *α1-adrenergic* receptor antagonist. Trifluoperazine is a potent NUPR1** inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis .

HY-B0661A

Tamsulosin hydrochloride 2 Publications Verification (R)-(-)-YM12617; LY253351	Adrenergic Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .

HY-B1392

Esmolol hydrochloride 3 Publications Verification	Adrenergic Receptor Caspase Apoptosis Aldose Reductase Neurokinin Receptor	Cardiovascular Disease Endocrinology Cancer
Esmolol hydrochloride is an ultra-short-acting cardioselective *β1-adrenergic* blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol hydrochloride attenuates post resuscitation myocardial dysfunction. Esmolol hydrochloride improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers .

HY-32329

Setiptiline Org-8282	5-HT Receptor Adrenergic Receptor	Neurological Disease
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

HY-111022

Icerguastat 3 Publications Verification Sephin1; IFB-088	Phosphatase	Infection Inflammation/Immunology
Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect .

HY-B0532A

Trifluoperazine dihydrochloride 5+ Cited Publications	Dopamine Receptor Adrenergic Receptor CaMK P-glycoprotein Influenza Virus Autophagy	Neurological Disease Cancer
Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent *α1-adrenergic* receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1** inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .

HY-B0478

Trazodone hydrochloride 5+ Cited Publications AF-1161	5-HT Receptor Serotonin Transporter Histamine Receptor Adrenergic Receptor	Neurological Disease
Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and *a2-adrenergic* receptors and histamine H1 receptors**, with minimal anticholinergic effects .

HY-A0066A

Tolazoline hydrochloride Imidaline hydrochloride; NSC35110 hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Tolazoline hydrochloride (Imidaline hydrochloride) is an *α-adrenergic* receptor** antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α₂-adrenergic receptor agonist-related poisoning, and skin vascular disease research .

HY-B2169

Melperone	5-HT Receptor Dopamine Receptor Adrenergic Receptor Cytochrome P450	Neurological Disease
Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, *α1-adrenergic, and α2-adrenergic* receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6** inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly .

HY-B1111

Amitraz BTS-27419	Environmental Pollutants Adrenergic Receptor Parasite Monoamine Oxidase	Infection Endocrinology
Amitraz is a non-systemic acaricide and insecticide with alpha-adrenergic agonist activity that interacts with octopamine receptors in the central nervous system and inhibits monoamine oxidase and prostaglandin synthesis .

HY-113248

3-Nitro-L-tyrosine	Endogenous Metabolite Adrenergic Receptor Reactive Oxygen Species (ROS)	Cardiovascular Disease Inflammation/Immunology
3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α₁-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis .

HY-148804

Vemtoberant APD418	Adrenergic Receptor	Cardiovascular Disease
Vemtoberant is a β₃-adrenergic receptor inhibitor with a human K_i of 8.2 nM, and exhibits 400- to 600-fold selectivity over human β₁-AR and β₂-AR. Vemtoberant attenuates β₃-AR-mediated cardiac inhibition. Vemtoberant can be used for the research of systolic heart failure .

HY-B1238

Pronethalol 2 Publications Verification (±)-Pronethalo	Adrenergic Receptor	Cardiovascular Disease Neurological Disease
Pronethalol ((±)-Pronethalo) is a non-selective *β-adrenergic* antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs) .

HY-118470

Butaxamine hydrochloride Butoxamin hydrochloride	Adrenergic Receptor	Endocrinology
Butaxamine (Butoxamin) hydrochloride is a specific β2-adrenergic receptor blocker. Butaxamine hydrochloride inhibits the decreases in urine volume in ethanol-anesthetized, water-diuretic rats .

HY-A0066

Tolazoline Imidaline; NSC35110	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Tolazoline (Imidaline) is an *α-adrenergic* receptor** antagonist. Tolazoline inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline can be used to study erectile dysfunction, α₂-adrenergic receptor agonist-related poisoning, and skin vascular disease research .

HY-W376701

Guanadrel	Adrenergic Receptor	Cardiovascular Disease
Guanadrel is an orally active postganglionic adrenergic inhibitor of spiroketal. Guanadre can be used in anti-hypertensive studies .

HY-12463A

Carmoterol	Adrenergic Receptor	Inflammation/Immunology
Carmoterol is a highly potent and selective long-acting *β2-adrenergic* receptor agonist with a pEC₅₀** of 10.19. Carmoterol shows 53-fold higher affinity for β2-adrenergic receptors than for β1-adrenergic receptors. Carmoterol stimulates cyclic adenosine monophosphate accumulation, induces airway smooth muscle relaxation, inhibits bronchoconstriction, reduces thromboxane B₂ release, and prolongs survival time. Carmoterol can be used in research related to asthma and chronic obstructive pulmonary disease (COPD) .

HY-17457

Levalbuterol hemitartrate Levosalbutamol hemitartrate	Adrenergic Receptor PI3K	Inflammation/Immunology
Levalbuterol (Levosalbutamol) hemitartrate is a β₂-adrenergic receptor agonist and PI3K inhibitor. Levalbuterol hemitartrate inhibits PI3K activity, reduces NF-κB and Rb protein expression, activates the cAMP/PKA pathway, and stimulates cAMP release. Levalbuterol hemitartrate relaxes airway smooth muscle, reduces intracellular calcium levels, and inhibits spasmogen-induced contractions. Levalbuterol hemitartrate can be used for the research of moderate-to-severe asthma .

HY-P10336

Serpinin	Serpin	Neurological Disease Endocrinology
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function . Serpinin is a selective agonist for *β-adrenergic* receptors*. Serpinin interacts with β1-adrenergic* receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .

HY-118944

L-748328	Adrenergic Receptor	Endocrinology
L-748328 is a potent and selective human *β3-adrenergic* receptor antagonist. L-748328 has a K_i of 3.7 nM against human cloned β3-AR** expressed in Chinese hamster ovary (CHO) cells. In addition, L-748328 inhibits the lipolytic response induced by the β3-AR agonist L-742791 in isolated non-human primate adipocytes .

HY-32329A

Setiptiline maleate MO-8282	5-HT Receptor	Neurological Disease
Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT_2A, 5-HT_2C, and/or 5-HT₃ subtypes, as well as an H1 receptor inverse agonist/antihistamine .

HY-121082

(-)-Dihydroalprenolol L-Dihydroalprenolol	Adrenergic Receptor	Endocrinology
(-)-Dihydroalprenolol (L-Dihydroalprenolol) is a β-adrenergic antagonist that inhibits the activity of β-adrenergic receptors. (-)-Dihydroalprenolol can cause desensitization of approximately 60% of β-adrenergic receptor binding sites. (-)-Dihydroalprenolol has also been shown to reduce the binding capacity of specific β-adrenergic ligands. (-)-Dihydroalprenolol may affect the ability to stimulate membrane-bound adenylate acylase .

HY-B0381B

Levobetaxolol hydrochloride (S)-Betaxolol hydrochloride; AL-1577A	Adrenergic Receptor	Cardiovascular Disease Neurological Disease Endocrinology
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker) that can lower the pressure in the eye.

HY-123059

(Rac)-Zenidolol hydrochloride (Rac)-ICI-118551 hydrochloride	Adrenergic Receptor	Neurological Disease
(Rac)-ICI-118551 ((Rac)-ICI-118551) hydrochloride is a selective *β2-adrenergic* receptor** antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease .

HY-B1615R

Clenbuterol (Standard) NAB-365 (Standard)	Reference Standards Adrenergic Receptor	Inflammation/Immunology
Clenbuterol (Standard) is the analytical standard of Clenbuterol. This product is intended for research and analytical applications. Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM . Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator .

HY-151198

CHF-6366	mAChR Adrenergic Receptor Calcium Channel	Inflammation/Immunology Endocrinology
CHF-6366 is a potent M3 muscarinic antagonist and *β2-adrenergic* receptors agonist with pK_i values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel** inhibitor (IC₅₀~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD) .

HY-106523

Nipradolol KT 210; K 351; Hypadil	Adrenergic Receptor	Cardiovascular Disease
Nipradolol (KT-210; K-351) is a potent blocker of alpha-1-adrenergic receptors. Nipradolol inhibits the increase of intraocular pressure (IOP) in an albino rabbit model induced by Phenylephrine (HY-B0769). Nipradolo suppresses the noradrenaline (NA)-induced muscles contraction, also exhibits vasodilator activity on the dog coronary artery .

HY-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

HY-179226

AP-7-168	Molecular Glues Adrenergic Receptor	Inflammation/Immunology
AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the *β2-adrenergic* receptor (β2AR*). AP-7-168 can promote β2AR homodimerization and inhibit* GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma .

HY-B1111R

Amitraz (Standard) BTS-27419 (Standard)	Reference Standards Adrenergic Receptor Monoamine Oxidase Parasite	Infection Endocrinology
Amitraz (Standard) is the analytical standard of Amitraz. This product is intended for research and analytical applications. Amitraz is a non-systemic acaricide and insecticide with alpha-adrenergic agonist activity that interacts with octopamine receptors in the central nervous system and inhibits monoamine oxidase and prostaglandin synthesis.

HY-W982195

Napamezole hydrochloride	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Napamezole hydrochloride is an orally active *α-2 adrenergic* receptor antagonist and serotonin (5-HT Receptor*) reuptake inhibitor, with K_i* values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole hydrochloride can be used for the research of depression .

HY-P5158

Conopeptide rho-TIA	Adrenergic Receptor	Others
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α_1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α_1A-Adrenergic Receptor and α_1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α₁-Adrenergic Receptor subtype-selective drugs .

HY-W752055

(Rac)-Nebivolol-d4 hydrochloride (Rac)-R 065824-d4 hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
(Rac)-Nebivolol-d4 hydrochloride is a labelled racemic Nebivolol. Nebivolol selectively inhibits *β1-adrenergic* receptor with an IC₅₀** of 0.8 nM .

HY-B1615

Clenbuterol NAB-365	Adrenergic Receptor	Inflammation/Immunology
Clenbuterol (NAB-365) is a *β2-adrenergic* receptor agonist with an EC₅₀** of 31.9 nM . Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator .

HY-B0661AS1

Tamsulosin-d4 hydrochloride (R)-(-)-YM12617-d₄; LY253351-d₄	Isotope-Labeled Compounds Adrenergic Receptor Endogenous Metabolite	Neurological Disease Endocrinology
Tamsulosin-d₄ (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .

HY-103109

Melperone hydrochloride	5-HT Receptor Dopamine Receptor Adrenergic Receptor Cytochrome P450	Neurological Disease
Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, *α1-adrenergic, and α2-adrenergic* receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6** inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .

HY-16525

XEN-2174	Monoamine Transporter Adrenergic Receptor	Neurological Disease
XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating *α2-adrenergic* receptor** at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research .

HY-B2169S2

Melperone-d4 hydrochloride	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor Adrenergic Receptor Cytochrome P450	Neurological Disease
Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, *α1-adrenergic, and α2-adrenergic* receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6** inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .

HY-B1392A

Esmolol	Adrenergic Receptor Caspase Apoptosis Aldose Reductase Neurokinin Receptor	Cardiovascular Disease Endocrinology Cancer
Esmolol is an ultra-short-acting cardioselective *β1-adrenergic* blocker. Esmolol exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol attenuates post resuscitation myocardial dysfunction. Esmolol improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers .

HY-B1308

Adrenalone hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Adrenalone hydrochloride is an *adrenergic* agonist used as a topical vasoconstrictor and hemostatic. Adrenalone hydrochloride is an inhibitor of dopamine β oxidase. Adrenalone hydrochloride is chemically similar to known norepinephrine transporter (NET) ligands with an IC₅₀ of 36.9 μM .

HY-B1308A

Adrenalone	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Adrenalone is an *adrenergic* agonist used as a topical vasoconstrictor and hemostatic. Adrenalone is an inhibitor of dopamine β oxidase. Adrenalone is chemically similar to known norepinephrine transporter (NET) ligands with an IC₅₀ of 36.9 μM .

HY-120473

TAK-259	Adrenergic Receptor	Metabolic Disease
TAK-259 is an orally active α1D-adrenergic receptor antagonist with a K_i value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 can inhibit the contraction of isolated bladder strips in rats with bladder outlet obstruction, reduce non-voiding bladder contractions, and improve urinary frequency symptoms. TAK-259 can be used in research related to overactive bladder .

HY-W722796

Tuaminoheptane sulfate	Adrenergic Receptor	Others
Tuaminoheptane sulfate is an alpha-adrenergic receptor agonist. Tuaminoheptane sulfate exerts its decongestant and irritant effects by inhibiting norepinephrine reuptake and promoting its release. Tuaminoheptane sulfate can be used in research on nasal diseases such as decongestion .

HY-W103960

Mirabegron impurity-1	Adrenergic Receptor	Metabolic Disease
Mirabegron impurity-1 is a potent and selective β3- adrenergic receptor agonist. Mirabegron impurity-1 has the activity of inhibiting metabolism. Mirabegron impurity-1 can be used in the study of the study of bladder impurity .

HY-122221

KUM 32	Adrenergic Receptor Adenylate Cyclase	Cardiovascular Disease
KUM 32 is a potent antagonist of epinephrine-induced platelet aggregation. KUM 32 is an adenylate cyclase activity inhibitor. KUM 32 binds to the *alpha 2 adrenergic* receptor** of human platelets .

Cat. No.	Product Name

HY-L062

Neurotransmitter Receptor Compound Library

2,495 compounds

Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.

In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.

MCE designs a unique collection of 2,495 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.

HY-L013

Neuronal Signaling Compound Library

3,802 compounds

Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

MCE designs a unique collection of 3,802 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Cat. No.	Product Name	Target	Research Area

HY-P10336

Serpinin	Serpin	Neurological Disease Endocrinology
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function . Serpinin is a selective agonist for *β-adrenergic* receptors*. Serpinin interacts with β1-adrenergic* receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .

HY-P3641A

Kisspeptin 13 TFA	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

HY-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

HY-P5158

Conopeptide rho-TIA	Adrenergic Receptor	Others
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α_1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α_1A-Adrenergic Receptor and α_1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α₁-Adrenergic Receptor subtype-selective drugs .

HY-16525

XEN-2174	Monoamine Transporter Adrenergic Receptor	Neurological Disease
XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating *α2-adrenergic* receptor** at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research .

HY-P1376A

G-Protein antagonist peptide TFA 1 Publications Verification	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0573

Propranolol hydrochloride Maximum Cited Publications 44 Publications Verification	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor Bacterial
Propranolol hydrochloride is a nonselective and BBB-permeableβ-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i 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. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573B

Propranolol Maximum Cited Publications 44 Publications Verification	Cardiovascular Disease Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Adrenergic Receptor Bacterial
Propranolol is a nonselective and BBB-permeable *β-adrenergic* receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i** values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0661

Tamsulosin 2 Publications Verification (R)-(-)-YM12617 free base; LY253351 free base	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Endocrinology Source Classification Cancer	Adrenergic Receptor Apoptosis
Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .

HY-101392

Harmane 1 Publications Verification	Alkaloids other families Pyridine Alkaloids Plants Indole Alkaloids Source Classification	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor
Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and *α2-adrenergic* receptor** of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .

HY-N2037

Higenamine 5+ Cited Publications Norcoclaurine; Demethyl-Coclaurine	Alkaloids Structural Classification Classification of Application Fields Ranunculaceae Phenols Polyphenols Aconitum carmichaeli Debx. Plants Isoquinoline Alkaloids Disease Research Fields Endocrinology Source Classification	MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a *α1-adrenergic* receptor antagonist with hypotensive effect. is a selective LSD1** inhibitor (IC₅₀=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .

HY-B0661A

Tamsulosin hydrochloride 2 Publications Verification (R)-(-)-YM12617; LY253351	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor Apoptosis
Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .

HY-12882A

Ifenprodil tartrate 5+ Cited Publications NP-120 tartrate; RC-61-91 tartrate	Alkaloids Piperidine Alkaloids Neurological Disease Classification of Application Fields Crassulaceae Sedum sarmentosum Bunge Plants Disease Research Fields Source Classification	iGluR Adrenergic Receptor Potassium Channel Calcium Channel Influenza Virus
Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC₅₀=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC₅₀=146 μM) . Ifenprodil tartrate is an *α1 adrenergic* receptor** antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC₅₀ of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .

HY-N1255

Scoulerine (-)-Scoulerine; Discretamine	Alkaloids Structural Classification other families Classification of Application Fields Phenols Polyphenols Plants Isoquinoline Alkaloids Disease Research Fields Source Classification Cancer	Bcl-2 Family Apoptosis mTOR GABA Receptor PI3K Adrenergic Receptor Beta-secretase Akt
Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine mainly targets the PI3K/Akt/mTOR signaling axis and *α1D-*adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine is applicable to research related to leukemia, ovarian cancer, and colorectal cancer .

HY-A0066A

Tolazoline hydrochloride Imidaline hydrochloride; NSC35110 hydrochloride	Alkaloids Classification of Application Fields Other Alkaloids Alpinia officinarum Hance Plants Disease Research Fields Endocrinology Source Classification Zingiberaceae	Adrenergic Receptor
Tolazoline hydrochloride (Imidaline hydrochloride) is an *α-adrenergic* receptor** antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α₂-adrenergic receptor agonist-related poisoning, and skin vascular disease research .

HY-113248

3-Nitro-L-tyrosine	Structural Classification Monophenols Classification of Application Fields Ketones, Aldehydes, Acids Disease markers Phenols Metabolic Disease Nervous System Disorder Endogenous metabolite Disease Research Fields Cardiovascular System Disorder Source Classification	Endogenous Metabolite Adrenergic Receptor Reactive Oxygen Species (ROS)
3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α₁-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis .

HY-N2374

Eupatorin 2 Publications Verification	Structural Classification Flavonoids Classification of Application Fields Flavones Cruciferae Phenols Polyphenols Isatis tinctoria L. Plants Disease Research Fields Source Classification Cancer	Apoptosis NF-κB MMP Adrenergic Receptor
Eupatorin is an orally active flavonoid with antiproliferative and vasodilatory properties. Eupatorin downregulates the expression levels of NF-κB, MMP9, IL-1β and TNF-α. Eupatorin induces apoptosis, G2/M phase cell cycle arrest, and reactive oxygen species (ROS) production. Eupatorin modulates the activities of muscarinic receptors and *β-adrenergic* receptors*; inhibits* sarcoplasmic reticulum calcium release and calcium channels; and activates the NO/sGC/cGMP pathway, indomethacin-sensitive pathway, and potassium channel pathway. Eupatorin exerts cytotoxic effects on cancer cell lines, and is metabolized by CYP1A1 and CYP1 family enzymes to form metabolites with antiproliferative activity. Eupatorin can be used in research related to breast cancer, hypertension, and leukemia .

HY-N4225

Aaptamine 2 Publications Verification	Alkaloids Animals Classification of Application Fields Marine natural products Quinoline Alkaloids Sponge Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor Proteasome Cholinesterase (ChE) Bacterial Apoptosis AP-1 NF-κB
Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the *α-adrenergic* receptor*, as well as an inhibitor* of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects .

HY-101392A

Harmane hydrochloride 1 Publications Verification	Apocynaceae Alkaloids Other Alkaloids Plants Rauwolfia canescens Source Classification	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and *α2-adrenergic* receptor** of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .

HY-B0573R

Propranolol hydrochloride (Standard)	Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Adrenergic Receptor Bacterial
Propranolol (hydrochloride) (Standard) is the analytical standard of Propranolol (hydrochloride). This product is intended for research and analytical applications. Propranolol hydrochloride is a nonselective *β-adrenergic* receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i** 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 . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-135525

Agroclavine	Infection Structural Classification Alkaloids Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Endogenous metabolite Disease Research Fields Indole Alkaloids Source Classification Cancer	Dopamine Receptor Adrenergic Receptor
Agroclavine acts as an agonist of the D1-dopamine receptor and α₁-adrenergic receptor. Agroclavine enhances the sensitivity of the brain to magnetic fields; it impairs spatial memory without affecting hippocampal long-term potentiation (LTP). Agroclavine exerts bidirectional regulatory effects on immune activity: it enhances NK cell activity with low toxicity under normal conditions, while it inhibits NK cell activity and exhibits significant cardiac and hepatic toxicity under stress conditions. Agroclavine can be used for research on neuroelectrophysiology, learning and memory, and immunoregulation .

HY-N3198A

Sophoramine 1 Publications Verification (-)-Sophoramine	Alkaloids Structural Classification Classification of Application Fields Leguminosae Other Diseases Pyridine Alkaloids Sophora flavescens Aiton Plants Disease Research Fields Source Classification	Adrenergic Receptor
Sophoramine ((-)-Sophoramine) is a prejunctional α₂-adrenoceptor inhibitor that can be found in the seeds of Sophora alopecuroides. Sophoramine inhibits prejunctional α2-adrenoceptors to facilitate norepinephrine release from adrenergic nerves. Sophoramine shows cytotoxic activity against human cancer cells, positive inotropic activity, and activity in rodent arrhythmia models. Sophoramine can be used for the research of arrhythmias .

HY-113248R

3-Nitro-L-tyrosine (Standard)	Structural Classification Monophenols Ketones, Aldehydes, Acids Disease markers Phenols Nervous System Disorder Endogenous metabolite Cardiovascular System Disorder Source Classification	Endogenous Metabolite Reference Standards
3-Nitro-L-tyrosine (Standard) is the analytical standard of 3-Nitro-L-tyrosine (HY-113248). This product is intended for research and analytical applications. 3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α₁-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis .

HY-120408

(±)-Scopolamine Atroscine	Alkaloids other families Other Alkaloids Plants Source Classification	Adrenergic Receptor
(±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits *α-adrenergic* receptor activity. (±)-Scopolamine has K_i** values of 33 μM and 7.25 nM for α₁-adrenerg receptor and muscarinic cholinergic receptor, respectively .

HY-N2037R

Higenamine (Standard) Norcoclaurine (Standard); Demethyl-Coclaurine (Standard)	Alkaloids Structural Classification Ranunculaceae Phenols Polyphenols Aconitum carmichaeli Debx. Plants Isoquinoline Alkaloids Source Classification	Reference Standards MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .

HY-B0661R

Tamsulosin (Standard) (R)-(-)-YM12617 free base (Standard); LY253351 free base (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Adrenergic Receptor Endogenous Metabolite
Tamsulosin (Standard) is the analytical standard of Tamsulosin. This product is intended for research and analytical applications. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α₁-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .

HY-W015546R

β-N-methylamino-L-alanine hydrochloride (Standard) BMAA hydrochloride (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Source Classification	Bacterial Reference Standards mGluR PKC
Clenbuterol (Standard) is the analytical standard of Clenbuterol. This product is intended for research and analytical applications. Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM . Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator .

HY-A0066AR

Tolazoline hydrochloride (Standard) Imidaline hydrochloride (Standard); NSC35110 hydrochloride (Standard)	Alkaloids Other Alkaloids Alpinia officinarum Hance Plants Source Classification Zingiberaceae	Reference Standards Adrenergic Receptor
Tolazoline (hydrochloride) (Standard) is the analytical standard of Tolazoline hydrochloride (HY-A0066A). This product is intended for research and analytical applications. Tolazoline hydrochloride (Imidaline hydrochloride) is an *α-adrenergic* receptor** antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α₂-adrenergic receptor agonist-related poisoning, and skin vascular disease research .

HY-B0661AR

Tamsulosin hydrochloride (Standard) (R)-(-)-YM12617 (Standard); LY253351 (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Adrenergic Receptor Apoptosis
Tamsulosin (hydrochloride) (Standard) is the analytical standard of Tamsulosin hydrochloride (HY-B0661A). Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .

HY-N18279

Bulbocapnine	Structural Classification Alkaloids Corydalis yanhusuo W. T. Wang Quinoline Alkaloids Plants Papaveraceae Source Classification	Dopamine Receptor Adrenergic Receptor
Bulbocapnine is an aporphine isoquinoline alkaloid that exerts antagonistic effects on dopamine Receptor) and α-adrenergic receptors, as well as anti-peroxidative effects. The K_i value of bulbocapnine for tyrosine hydroxylase (TH) is 0.20 mM. Bulbocapnine reduces intracellular dopamine content, inhibits TH activity, and decreases Ca ²⁺ concentration. Bulbocapnine antagonizes the dose-dependent inhibitory effect of dopamine on the heart rate acceleration induced by stimulating the postganglionic fibers of the right cardiac accelerator nerve .

HY-N1255A

Scoulerine hydrochloride (-)-Scoulerine hydrochloride; Discretamine hydrochloride	Structural Classification Alkaloids Phenols Polyphenols Umbelliferae Plants Isoquinoline Alkaloids Carphephorus corymbosus (Nutt.) Torr. & A.Gray Source Classification	Apoptosis PI3K Akt mTOR Adrenergic Receptor GABA Receptor Beta-secretase Bcl-2 Family
Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and *α1D-*adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer .

Cat. No.	Product Name	Chemical Structure

HY-B0573S1

Propranolol-d7 (ring-d7)

Propranolol-d₇ (ring-d₇) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i 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 . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-113248S

3-Nitro-L-tyrosine-d3

3-Nitro-L-tyrosine-d₃ is the deuterium labeled 3-Nitro-L-tyrosine (HY-113248). 3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α₁-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis .

HY-B0573BS

Propranolol-d7

Propranolol-d₇ is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573S

Propranolol-d7 hydrochloride

Propranolol-d₇ (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i 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 . Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-A0077S1

Perphenazine-d4
Perphenazine-d₄ is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, 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.

HY-W752055

(Rac)-Nebivolol-d4 hydrochloride
(Rac)-Nebivolol-d4 hydrochloride is a labelled racemic Nebivolol. Nebivolol selectively inhibits *β1-adrenergic* receptor with an IC₅₀** of 0.8 nM .

HY-B0661AS1

Tamsulosin-d4 hydrochloride
Tamsulosin-d₄ (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .

HY-B2169S2

Melperone-d4 hydrochloride

Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .

HY-A0016S

Dronedarone-d6 hydrochloride

Dronedarone-d₆ (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4 .

HY-90003S

Tianeptine-d12

Tianeptine-d₁₂ is a deuterated analog of Tianeptine (HY-90003).Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

HY-B0532S

Trifluoperazine-d8
Trifluoperazine-d₈ is a deuterium labeled Trifluoperazine. Trifluoperazine is an antipsychotic phenothiazine agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine is also a potent dopamine D2 receptor inhibitor .

HY-B0661AS

Tamsulosin-d5 hydrochloride
Tamsulosin-d₅ (hydrochloride) is the deuterium labeled Tamsulosin hydrochloride. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .

HY-B0532AS

Trifluoperazine-d3 dihydrochloride

Trifluoperazine-d₃ (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .

HY-B0661S

Tamsulosin-d4
Tamsulosin-d₄ ((R)-(-)-YM12617 (free base)-d₄) is deuterium labeled Tamsulosin. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α₁-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .

HY-B0203BS1

(rac)-Nebivolol-d4
(rac)-Nebivolol-d₄ is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM[1][2].

HY-100634S

4-Hydroxypropranolol-d7 hydrochloride

4-Hydroxypropranolol-d₇ (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

HY-100634SA

4-Hydroxypropranolol-d7

4-Hydroxypropranolol-d₇ is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .

HY-113248S1

3-Nitro-L-tyrosine-13C6

3-Nitro-L-tyrosine- ¹³C₆ is the ¹³C labeled 3-Nitro-L-tyrosine (HY-113248). 3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α₁-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis .

HY-B1392S

Esmolol-d7 hydrochloride

Esmolol-d₇ hydrochloride is the deuterium labeled Esmolol hydrochloride (HY-B1392). Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptorinhibiting (aldose reductase) and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers .

HY-32329S

Setiptiline-d3

Setiptiline-d₃ is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .

HY-W777360

Harman-13C2,15N

Harman- ¹³C₂, ¹⁵N is ¹³C and ¹⁵N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC₅₀ values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .

HY-152051S

Mabuterol-d9 hydrochloride

Mabuterol-d₉ (hydrochloride) is deuterium labeled Mabuterol (hydrochloride). Mabuterol hydrochloride is a selective and orally active beta-2 adrenergic receptor (ADRB2) agonist. Mabuterol hydrochloride inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol hydrochloride suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB .

HY-W653969

Arotinolol-d5 hydrochloride

Arotinolol-d₅ (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-A0016S3

Dronedarone-d6

Dronedarone-d₆ (SR 33589-d₆) is deuterium labeled Dronedarone. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4 .

HY-A0077S2

Perphenazine-d6 fumarate

Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine . Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .

HY-144224S

Tianeptine-d6 hydrochloride

Tianeptine-d₆ hydrochloride is the deuterium labeled Tianeptine hydrochloride. Tianeptine hydrochloride is an atypical antidepressant. Tianeptine hydrochloride is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine hydrochloride is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine hydrochloride increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine hydrochloride exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine hydrochloride inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine hydrochloride can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

HY-166478S

O-Desmethyl carvedilol-d5

O-Desmethyl carvedilol-d₅ (Desmethylcarvedilol-d₅) is deuterium labeled O-Desmethylcarvedilol. O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol (HY-B0006). O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2 ^R4496C) mutation (IC₅₀ = 7.62 μM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol (HY-B0468) in conscious rabbits (ED₅₀s = 32 and 5 μg/kg, respectively) .

HY-W700834

Harman-d3

Harman-d₃ is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC₅₀ values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .

HY-100607S

Landiolol-d8

Landiolol-d₈ (ONO1101-d₈) is the deuterium labeled Landiolol (HY-100607). Landiolol (ONO1101) is a highly selective, ultra-short-acting competitive inhibitor of β₁ adrenergic receptors. Landiolol specifically blocks cardiac β₁ receptors, reducing heart rate and myocardial oxygen consumption. Landiolol inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol has little effect on cardiac ion channels (such as L-type calcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury .

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