Search Result

Results for "

Adrenergic ��2 Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (42) 5-HT Receptor (14) AAK1 (2) Adenosine Receptor (1) Apoptosis (4) Arrestin (1) Autophagy (6) Bacterial (2) Calcium Channel (2) Cytochrome P450 (1) Dopamine Receptor (3) Histamine Receptor (7) Isotope-Labeled Compounds (2) mAChR (8) P2X Receptor (1) PROTACs (1) Serotonin Transporter (5) Sigma Receptor (1) Sodium Channel (5) Trk Receptor (4)
By Research Areas:	Cancer (15) Cardiovascular Disease (14) Endocrinology (21) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (26)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Adrenergic Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0194A

Tizanidine hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology Cancer
Tizanidine hydrochloride is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.

HY-B0194

Tizanidine	Adrenergic Receptor	Neurological Disease Endocrinology Cancer
Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.

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-B0194S

Tizanidine-d4	Adrenergic Receptor	Neurological Disease Endocrinology Cancer
Tizanidine-d₄ is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons[1][2].

HY-100543

Zenidolol ICI-118551
Zenidolol (ICI-118551) is a selective β2 adrenergic receptor antagonist. Zenidolol inhibits β2-, β1- and β3-adrenergic receptor with K_i values of 0.7, 49.5 and 611 nM, respectively. Zenidolol can be used as an ocular hypotensive agent used for ophthalmic disease research .

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 ^[2] .

HY-123059

(Rac)-ICI-118551 hydrochloride	Adrenergic Receptor	Neurological Disease
(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-112658

p-Iodoclonidine hydrochloride	Adrenergic Receptor Adenosine Receptor	Endocrinology
p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC₅₀ of 1.5 μM .

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-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 ^[2] .

HY-108302

Nifenalol	Adrenergic Receptor	Others
Nifenalol is a β-adrenergic receptor blocker. Nifenalol inhibits β-adrenoceptor differentiation in right atrium, diaphragm and adipose tissue in a rat model ^[2].

HY-32329S

Setiptiline-d3	Isotope-Labeled Compounds 5-HT Receptor Adrenergic Receptor	Neurological Disease
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[1][2].

HY-B0203BS1

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

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-P1376A

G-Protein antagonist peptide TFA	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 .

HY-100634

4-Hydroxypropranolol hydrochloride (±)-4-hydroxy Propranolol 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 ^[2] .

HY-B0193A

Prazosin hydrochloride 5+ 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 ^[2].Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively .

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 ^[2].

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-12709

ARC 239	Adrenergic Receptor 5-HT Receptor	Neurological Disease
ARC 239 is an α2B/C-adrenergic receptor antagonist with pK_i of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a K_i of 63.1 nM ^[2].

HY-119706

Barbadin 5+ 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 ^[2].

HY-100634S

4-Hydroxypropranolol-d7 hydrochloride (±)-4-Hydroxy Propranolol-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[1][2][3].

HY-B0193AR

Prazosin hydrochloride (Standard)	Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology Cancer
Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. 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 ^[2].Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively .

HY-A0077

Perphenazine 1 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 .

HY-A0077A

Perphenazine dihydrochloride	Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy	Neurological Disease Inflammation/Immunology Endocrinology Cancer
Perphenazine dihydrochloride 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 dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation .

HY-100634SA

4-Hydroxypropranolol-d7 (±)-4-Hydroxy Propranolol-d₇	Isotope-Labeled Compounds Adrenergic Receptor	Neurological Disease
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[1][2][3].

HY-14794

Dextromilnacipran (1R,2S)-milnacipran; F2696	Serotonin Transporter	Metabolic Disease
Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC₅₀ of 3.4 μM. (patent WO2013014263A1).

HY-153091

BMY 14802	Adrenergic Receptor 5-HT Receptor Sigma Receptor	Neurological Disease
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and **adrenergic alpha-1 receptors*. BMY 14802 inhibits* abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM ^[2].

HY-14560A

(R,R)-Reboxetine mesylate (R,R)-FCE20124 mesylate; (R,R)-PNU155950E mesylate	Adrenergic Receptor mAChR	Neurological Disease
(R,R)-Reboxetine mesylate is an antidepressant agent with great bioavailability. (R,R)-Reboxetine is the enantiomer of Reboxetine, which is a selective noradrenaline reuptake inhibitor. Reboxetine consists of (R,R) and (S,S) enantiomer, has low affinity for *alpha-adrenergic* and muscarinic receptors and low toxicity in animals ^[2].

HY-B0527A

Amitriptyline hydrochloride 3 Publications Verification	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease Cancer
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 ^[2] .

HY-122537A

Arotinolol	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
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 ^[2]. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

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-13338

Mabuterol	Adrenergic Receptor	Cardiovascular Disease
Mabuterol is a selective and orally active **beta-2 adrenergic receptor (ADRB2)** agonist. Mabuterol inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB ^[2].

HY-W755295

Mabuterol hydrochloride	Adrenergic Receptor	Cardiovascular Disease
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 ^[2].

HY-B0527AS

Amitriptyline-d6 hydrochloride	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease
Amitriptyline-d₆ (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis 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 Ki 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[1][2][3].

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 ^[2] .

HY-14299

Indacaterol 4 Publications Verification	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a *β-arrestin2*-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research ^[2].

HY-U00244A

Benzquinamide hydrochloride P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride	Adrenergic Receptor	Cancer
Benzquinamide (P2647) is an antiemetic which can bind to the *α_2A, α_2B, and α_2C* **adrenergic receptors** (α2-AR) with K_i values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells ^[2].

HY-14299A

Indacaterol maleate 4 Publications Verification QAB149	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a *β-arrestin2*-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research ^[2].

HY-B0527AR

Amitriptyline hydrochloride (Standard)	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease Cancer
Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. 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 ^[2] .

HY-120179

LP-922761	AAK1	Neurological Disease
LP-922761 is a potent, selective and orally active *adapter protein-2 associated kinase 1 (AAK1) inhibitor* with IC₅₀s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC₅₀ of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .

HY-120179A

LP-922761 hydrate	AAK1	Neurological Disease
LP-922761 hydrate is a potent, selective and orally active *adapter protein-2 associated kinase 1 (AAK1) inhibitor* with IC₅₀s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC₅₀ of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .

HY-112461A

NF449 octasodium 1 Publications Verification	P2X Receptor	Cardiovascular Disease
NF449 octasodium is a highly potent **P2X₁ receptor antagonist, with IC₅₀*s 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 ^[2].

HY-B0573

Propranolol hydrochloride 15+ Cited Publications	Adrenergic Receptor Bacterial	Neurological Disease Endocrinology Cancer
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 ^[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573B

Propranolol 15+ Cited Publications	Adrenergic Receptor Bacterial	Cardiovascular Disease Neurological Disease Endocrinology Cancer
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 ^[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-A0016S

Dronedarone D6 hydrochloride	mAChR Sodium Channel Calcium Channel Adrenergic Receptor Cytochrome P450 Autophagy	Cardiovascular Disease
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[1][2][3][4].

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 Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. 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 Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[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 Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. 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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0573

Propranolol hydrochloride 15+ Cited Publications	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Endocrinology	Adrenergic Receptor Bacterial
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 ^[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573B

Propranolol 15+ Cited Publications	Cardiovascular Disease Alkaloids Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	Adrenergic Receptor Bacterial
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 ^[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

Cat. No.	Product Name	Chemical Structure

HY-B0194S

Tizanidine-d4
Tizanidine-d₄ is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons[1][2].

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 ^[2] .

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[1][2].

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-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[1][2][3].

HY-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis 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 Ki 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[1][2][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[1][2][3][4].

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 Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].

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 Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[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
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks