Adrenergic Receptor

Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline can be used for non-bacterial conjunctivitis research.

Detomidine hydrochloride, an imidazole derivative, is a potent α2-adrenergic agonist. Detomidine hydrochloride produces dose-dependent analgesic effects.

Imiloxan (RS 21361) hydrochloride is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan hydrochloride produces a dose-related reversal of Guanoxabenz (HY-U00123)-induced maximal mydriasis in male rats. Imiloxan hydrochloride has the potential for acute kidney injury research.

3-Hydroxy xylazine is a metabolite of the α2-adrenergic receptor agonist Xylazine.

Desipramine-d₄ is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.

Sophoramine ((-)-Sophoramine) is a prejunctional α₂-adrenoceptor inhibitor that can be found in the seeds of Sophora alopecuroides. Sophoramine inhibits prejunctional α2-adrenoceptors to facilitate norepinephrine release from adrenergic nerves. Sophoramine shows cytotoxic activity against human cancer cells, positive inotropic activity, and activity in rodent arrhythmia models. Sophoramine can be used for the research of arrhythmias.

Olodaterol (hydrochloride) (Standard) is the analytical standard of Olodaterol (hydrochloride). This product is intended for research and analytical applications. Olodaterol (BI1744) hydrochloride is a selective, long acting β₂-adrenoceptor (β₂-AR) agonist (EC₅₀=0.1 nM and pK_i= 9.14 for human β₂-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.

Amitraz-d₃ is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.

3,4-Dihydro-6,7-isoquinolinediol (compound 7) is a β2-AR agonist with an EC50 of 106.9 μM in CH-K1/GA1S cells. 3,4-Dihydro-6,7-isoquinolinediol can also inhibit the production of NO in mouse macrophage RAW 264.7 cells induced by lipopolysaccharide, showing anti-inflammatory activity.

Dextromilnacipran ((1R,2S)-Milnacipran; F2696) is an orally active Serotonin (HY-B1473A)/Noradrenaline (HY-13715) transporter inhibitor. Dextromilnacipran inhibits Serotonin and Noradrenaline reuptake. Dextromilnacipran can be used for the research of depression, fibromyalgia.

(R)-Octopamine is a Gs-coupled receptor agonist. (R)-Octopamine binds to the orthosteric site of BmOAR2 and interacts with the Asp115, Ser202 and Tyr300 residues to activate the receptor, which couples to Gs protein and thereby stimulates adenylate cyclase activity.

Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine hydrochloride inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

Dexmedetomidine (Standard) is the analytical standard of Dexmedetomidine. This product is intended for research and analytical applications. Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a K_i of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects.

MT-1207 is an orally active, selective adrenergic α1 and 5-HT2A receptor antagonist. The IC₅₀ values of MT-1207 for α1A, α1B, α1D, and 5-HT2A are <0.1 nM, 0.15 nM, 1.40 nM, and 0.27 nM, respectively. MT-1207 induces vasodilation, improves baroreflex sensitivity, and reduces heart rate in isolated hearts. MT-1207 lowers blood pressure, protects the heart, brain, and kidneys, improves cognition, delays stroke, reduces mortality, and lowers uric acid without impairing renal function in SHR/2K1C/2K2C models. MT-1207 exhibits high plasma protein binding, resistance to plasma esterases, and NADPH-dependent hepatic metabolism. MT-1207 can be used for research related to hypertension.

Bisoprolol-d₅ is the deuterium labeled Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.

Olodaterol-d₃ hydrochloride (BI1744-d₃ hydrochloride) is the deuterium labeled Olodaterol hydrochloride (HY-14301A). Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC₅₀=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.

Clozapine-d₈ is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.

Hordenine-d₆ (Ordenina-d₆; Peyocactine-d₆) is the deuterated-labeled Hordenine (HY-N0113). Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

Acebutolol-d₅ is the deuterium labeled Acebutolol.

Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.