Search Result

Pathways Recommended:	PI3K/Akt/mTOR

Results for "

Adrenergic ��3 Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (95) 5-HT Receptor (23) Akt (7) Aldose Reductase (2) Amyloid-β (1) Androgen Receptor (1) AP-1 (1) Apoptosis (22) Autophagy (18) Bacterial (4) Bcl-2 Family (4) Beta-secretase (2) Calcium Channel (14) CaMK (5) Casein Kinase (2) Caspase (4) Cholinesterase (ChE) (1) COX (1) Cytochrome P450 (7) Dopamine Receptor (14) Dopamine Transporter (4) Drug Derivative (1) Drug Metabolite (2) Endogenous Metabolite (4) Fungal (1) GABA Receptor (5) Glucocorticoid Receptor (1) GnRH Receptor (2) GSK-3 (1) HIF/HIF Prolyl-Hydroxylase (2) Histamine Receptor (11) Histone Methyltransferase (1) iGluR (7) Imidazoline Receptor (3) Influenza Virus (7) Isotope-Labeled Compounds (16) mAChR (11) MAP3K (2) MDM-2/p53 (2) Mitophagy (2) MMP (6) Monoamine Oxidase (3) mTOR (2) nAChR (3) Neurokinin Receptor (2) NF-κB (7) Opioid Receptor (8) P-glycoprotein (5) P2X Receptor (2) Phosphodiesterase (PDE) (2) PI3K (8) Potassium Channel (10) PROTACs (1) Proteasome (1) Reactive Oxygen Species (ROS) (5) Reference Standards (22) ROS Kinase (2) Serotonin Transporter (5) Sodium Channel (9) Taste Receptor (1) Tau Protein (1) Trk Receptor (5)
By Research Areas:	Cancer (29) Cardiovascular Disease (44) Endocrinology (37) Infection (7) Inflammation/Immunology (36) Metabolic Disease (9) Neurological Disease (61)

By Targets:

Adrenergic Receptor (95)

5-HT Receptor (23)

Akt (7)

Aldose Reductase (2)

Amyloid-β (1)

Androgen Receptor (1)

AP-1 (1)

Apoptosis (22)

Autophagy (18)

Bacterial (4)

Bcl-2 Family (4)

Beta-secretase (2)

Calcium Channel (14)

CaMK (5)

Casein Kinase (2)

Caspase (4)

Cholinesterase (ChE) (1)

COX (1)

Cytochrome P450 (7)

Dopamine Receptor (14)

Dopamine Transporter (4)

Drug Derivative (1)

Drug Metabolite (2)

Endogenous Metabolite (4)

Fungal (1)

GABA Receptor (5)

Glucocorticoid Receptor (1)

GnRH Receptor (2)

GSK-3 (1)

HIF/HIF Prolyl-Hydroxylase (2)

Histamine Receptor (11)

Histone Methyltransferase (1)

iGluR (7)

Imidazoline Receptor (3)

Influenza Virus (7)

Isotope-Labeled Compounds (16)

mAChR (11)

MAP3K (2)

MDM-2/p53 (2)

Mitophagy (2)

MMP (6)

Monoamine Oxidase (3)

mTOR (2)

nAChR (3)

Neurokinin Receptor (2)

NF-κB (7)

Opioid Receptor (8)

P-glycoprotein (5)

P2X Receptor (2)

Phosphodiesterase (PDE) (2)

PI3K (8)

Potassium Channel (10)

PROTACs (1)

Proteasome (1)

Reactive Oxygen Species (ROS) (5)

Reference Standards (22)

ROS Kinase (2)

Serotonin Transporter (5)

Sodium Channel (9)

Taste Receptor (1)

Tau Protein (1)

Trk Receptor (5)

By Research Areas:

Cancer (29)

Cardiovascular Disease (44)

Endocrinology (37)

Infection (7)

Inflammation/Immunology (36)

Metabolic Disease (9)

Neurological Disease (61)

113

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-B0573

Propranolol hydrochloride Maximum Cited Publications 44 Publications Verification	Adrenergic Receptor Bacterial	Cardiovascular Disease Infection Neurological Disease Metabolic Disease Cancer
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 ^[3] .

HY-B0573B

Propranolol Maximum Cited Publications 44 Publications Verification	Adrenergic Receptor Bacterial	Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
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 ^[3].

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 ^[3].

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 ^[3] .

HY-B0527A

Amitriptyline hydrochloride 5+ Cited Publications	Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
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 ^[3] .

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 ^[3] .

HY-A0016

Dronedarone 4 Publications Verification SR 33589	mAChR Sodium Channel Calcium Channel Adrenergic Receptor Cytochrome P450 Autophagy	Cardiovascular Disease
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-B0527

Amitriptyline 5+ Cited Publications	Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline 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 is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline 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 can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity ^[3] .

HY-112461A

NF449 octasodium 4 Publications Verification	P2X Receptor	Cardiovascular Disease
NF449 octasodium is a highly potent P2X₁ receptor antagonist, with IC₅₀s of 0.28, 0.69, and 120 nM for rP2X₁, rP2X₁₊₅, P2X₂₊₃, respectively. NF449 octasodium is a G_sα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to G_sα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to G_s .

HY-101392

Harmane 1 Publications Verification	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor	Neurological Disease Inflammation/Immunology
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) ^[3] .

HY-N2037

Higenamine 5+ Cited Publications Norcoclaurine; Demethyl-Coclaurine	MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis	Cardiovascular Disease Endocrinology
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 ^[3] .

HY-A0077

Perphenazine 3 Publications Verification	Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy	Neurological Disease Inflammation/Immunology Endocrinology Cancer
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 ^[3] .

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 ^[3] .

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-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 ^[3] .

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 ^[3].

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 ^[3] .

HY-90003

Tianeptine 1 Publications Verification	Opioid Receptor iGluR MMP PI3K Akt NF-κB	Neurological Disease Inflammation/Immunology
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 ^[3] .

HY-N1255

Scoulerine (-)-Scoulerine; Discretamine	Bcl-2 Family Apoptosis mTOR GABA Receptor PI3K Adrenergic Receptor Beta-secretase Akt	Cancer
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 ^[3].

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 ^[3] .

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-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 ^[3] .

HY-100607A

Landiolol hydrochloride ONO1101 hydrochloride	Adrenergic Receptor Calcium Channel Potassium Channel Reactive Oxygen Species (ROS)	Cardiovascular Disease Inflammation/Immunology Endocrinology
Landiolol (ONO1101) hydrochloride is a highly selective, ultra-short-acting competitive inhibitor of β₁ adrenergic receptors. Landiolol hydrochloride specifically blocks cardiac β₁ receptors, reducing heart rate and myocardial oxygen consumption. Landiolol hydrochloride inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol hydrochloride 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 hydrochloride can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury ^[3].

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 ^[3] .

HY-90003A

Tianeptine sodium salt 1 Publications Verification	Opioid Receptor iGluR MMP PI3K Akt NF-κB	Neurological Disease Inflammation/Immunology
Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt 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 sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the *PI3K/Akt*-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects ^[3] .

HY-B0573S1

Propranolol-d7 (ring-d7)	Adrenergic Receptor	Neurological Disease Endocrinology
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 ^[3].

HY-N4225

Aaptamine 2 Publications Verification	Adrenergic Receptor Proteasome Cholinesterase (ChE) Bacterial Apoptosis AP-1 NF-κB	Infection Neurological Disease Inflammation/Immunology Endocrinology Cancer
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 ^[3] .

HY-112461

NF449	P2X Receptor	Cardiovascular Disease
NF449 is a highly potent P2X₁ receptor antagonist, with IC₅₀s of 0.28, 0.69, and 120 nM for rP2X₁, rP2X₁₊₅, P2X₂₊₃, respectively. NF449 is a G_sα-selective G Protein antagonist. NF449 suppresses the rate of GTP[γS] binding to G_sα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to G_s .

HY-101392A

Harmane hydrochloride 1 Publications Verification	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor	Neurological Disease Inflammation/Immunology
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) ^[3] .

HY-113248S

3-Nitro-L-tyrosine-d3	Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology
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	Adrenergic Receptor	Cardiovascular Disease Neurological Disease Endocrinology
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 ^[3].

HY-B0573S

Propranolol-d7 hydrochloride	Adrenergic Receptor	Cardiovascular Disease Neurological Disease Endocrinology
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 ^[3].

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) ^[3].

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 ^[3].

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 ^[3] .

HY-N1433

Phytolaccagenin	Fungal mAChR Adrenergic Receptor Calcium Channel	Cardiovascular Disease Infection Inflammation/Immunology
Phytolaccagenin is a triterpenoid saponin aglycone, Antifungal agent, vasodilator, antihypertensive agent, and anti-inflammatory agent. Phytolaccagenin activates vascular and cardiac Muscarinic receptors, blocks cardiac *β-adrenergic* receptors, and inhibits voltage-dependent calcium channels in blood vessels. Phytolaccagenin inhibits the growth of Candida albicans and Cryptococcus neoformans. Phytolaccagenin induces vasodilation, produces negative inotropic and negative chronotropic effects, reduces mean arterial pressure, and inhibits LPS-induced inflammation. Phytolaccagenin exhibits enhanced antihypertensive effects in high salt-induced hypertensive rats. Phytolaccagenin can be used in the research of candidiasis, cryptococcosis, hypertension, and inflammation-related diseases ^[3] .

HY-B0573R

Propranolol hydrochloride (Standard)	Reference Standards Adrenergic Receptor Bacterial	Neurological Disease Endocrinology Cancer
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 ^[3].

HY-106954

Upidosin Rec 15/2739; Recordati 15/2739; SB 216469	Adrenergic Receptor	Inflammation/Immunology
Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a K_b value of 2-3 nM higher than in ear artery and aorta with a K_b value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction .

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 ^[3] .

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-135096

Amitriptyline-d3 hydrochloride	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease
Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits *adrenergic, muscarinic, histamine* and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity ^[3].

HY-135525

Agroclavine	Dopamine Receptor Adrenergic Receptor	Neurological Disease Inflammation/Immunology
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 ^[3].

HY-B0527AS

Amitriptyline-d6 hydrochloride	Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
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-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 ^[3] .

HY-A0077S1

Perphenazine-d4	5-HT Receptor Adrenergic Receptor Apoptosis Autophagy Dopamine Receptor Histamine Receptor	Neurological Disease Endocrinology
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-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-113248R

3-Nitro-L-tyrosine (Standard)	Endogenous Metabolite Reference Standards	Cardiovascular Disease Inflammation/Immunology
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-101755

Tedatioxetine hydrobromide Lu AA24530 hydrobromide	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT_2A, 5-HT_2C, *5-HT₃* and **α_1A-adrenergic receptor** antagonist . ,

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 ^[3].

Cat. No.	Product Name

HY-L013

Neuronal Signaling Compound Library

3,854 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 3,854 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-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 ^[3] .

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 ^[3] .

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 ^[3] .

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 ^[3].

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 ^[3] .

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) ^[3] .

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 ^[3] .

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 ^[3] .

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 ^[3].

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 ^[3] .

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 ^[3] .

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 ^[3] .

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) ^[3] .

HY-N1433

Phytolaccagenin	Triterpenes Structural Classification Classification of Application Fields Terpenoids Phytolacca acinosa Roxb. Plants Inflammation/Immunology Disease Research Fields Phytolaccaceae Source Classification	Fungal mAChR Adrenergic Receptor Calcium Channel
Phytolaccagenin is a triterpenoid saponin aglycone, Antifungal agent, vasodilator, antihypertensive agent, and anti-inflammatory agent. Phytolaccagenin activates vascular and cardiac Muscarinic receptors, blocks cardiac *β-adrenergic* receptors, and inhibits voltage-dependent calcium channels in blood vessels. Phytolaccagenin inhibits the growth of Candida albicans and Cryptococcus neoformans. Phytolaccagenin induces vasodilation, produces negative inotropic and negative chronotropic effects, reduces mean arterial pressure, and inhibits LPS-induced inflammation. Phytolaccagenin exhibits enhanced antihypertensive effects in high salt-induced hypertensive rats. Phytolaccagenin can be used in the research of candidiasis, cryptococcosis, hypertension, and inflammation-related diseases ^[3] .

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 ^[3].

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 ^[3].

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-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 ^[3] .

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 ^[3] .

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 ^[3] .

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 ^[3].

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 ^[3].

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 ^[3].

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 ^[3].

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 ^[3].

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 ^[3] .

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 ^[3] .

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-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 ^[3] .

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-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-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 ^[3].

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) ^[3] .

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 ^[3].

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 ^[3]. 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 ^[3].

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-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 ^[3].

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-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-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) ^[3] .

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 ^[3].

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks