Adrenergic Receptor Inhibitor

Todralazine hydrochloride (Ecarazine hydrochloride) is an anti-hypertensive agent, acts as a β₂AR blocker, with antioxidant and free radical scavenging activity.

Isoferulic acid (Standard) (3-Hydroxy-4-methoxycinnamic acid (Standard)) is the analytical standard of Isoferulic acid (HY-N0761). This product is intended for research and analytical applications. Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is an orally active cinnamic acid derivative. Isoferulic acid exhibits hypoglycemic, antiviral, and antioxidant activities. Isoferulic acid can also inhibit fructose- and glucose-mediated protein glycation. Isoferulic acid can be used in the research of diseases such as diabetes.

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

DL 071IT is a potent non-selective beta-adrenergic receptor blocker. DL 071IT exhibits intrinsic sympathomimetic activity and weak membrane stabilizing activity. DL 071IT reduces exercise heart rate and systolic blood pressure, and even significantly lowers resting heart rate.

(+)-Sotalol ((S)-Sotalol) is the S-isomer of Sotalol (HY-103196). Sotalol is an orally active, non-selective β-adrenergic receptor blocker. (+)-Sotalol is an antiarrhythmic agent. (+)-Sotalol can prolong action potential duration in isolated cardiac muscle.

Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone shows K_d values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively.

Ampreloxetine (TD-9855) TFA is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine TFA has the potential for the research of neurogenic orthostatic hypotension.

MK-761 free base is an orally effective β2-adrenergic receptor antagonist. MK-761 free base attenuates positive inotropic effects, reduces arterial pressure, enhances the contractility of papillary muscles in cat hearts, and exerts effects mediated by catecholamine release. MK-761 free base can be used in the research of hypertension.

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.

2-Aminoheptane (Tuaminoheptane) is a norepinephrine transporter inhibitor. 2-Aminoheptane binds to norepinephrine transporter via ionic and hydrophobic interactions to block norepinephrine uptake. 2-Aminoheptane deactivates ω-TAmla enzyme, reduces recombinant whole cell stability, and acts as an amino group donor substrate for ω-TA and ω-TAmla enzymes. 2-Aminoheptane can be used in research on depression and Alzheimer's disease.

Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC₅₀=30 nM) over α2-adrenoceptor (IC₅₀=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC₅₀s=0.5 and 5 μM for human MAO A/B, respectively).

AD109 is a combination of the selective norepinephrine reuptake inhibitor Atomoxetine (HY-107370) and the antimuscarinic agent Aroxybutynin (HY-B0267C). AD109 shows orally active significantly and reduces the apnea-hypopnea index.

Carvedilol-d₃ is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC₅₀ of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.

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.

LY 78335 (DCMB) is a brain-penetrant phenylethanolamine-N-methyltransferase (PNMT) inhibitor with a K_i of 0.09 μM. LY 78335 acts as an α₂-adrenoceptor inhibitor with an IC₅₀ of 10 μM. LY 78335 increases spontaneous locomotor activity in rats. LY 78335 increases extracellular concentration of 3-methoxy-4-hydroxyphenylglycol (MHPG) in rat hypothalamus. LY 78335 prevents growth hormone (GH) secretion in rats. LY 78335 can be used for the research of depression.

Prazobind (SZL 49), a prazosin analog, is an irreversible α1-adrenoceptor antagonist. Prazobind competes for alpha 1-adrenoceptor binding sites with a similar potency (IC₅₀ of 1 nM) in tissues enriched in both the alpha 1A (hippocampus) and alpha 1B (liver) subtypes. Prazobind partially inhibits the contractions of circular muscles, longitudinal muscles and smooth muscles of the spleen. Prazobind can be used for the study of blood pressure.

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).

Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC₅₀s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.

Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR).

4-Hydroxy nebivolol (4-OH nebivolol) hydrochloride is an active β-blocking hydroxylated metabolite of Nebivolol (HY-B0203).