Adrenergic Receptor Inhibitor

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.

Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.

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.

2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC₅₀ of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart.

Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.

Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β₁/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer.

Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC₅₀ value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .

(S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).

Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC₅₀ values of 6.6 nM, 48 nM and 830 nM, and K_i values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine has antidepressant and analgesic effects. Nomifensine is used in neurodegenerative diseases, compound addiction, and pain research.

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

Betaxolol is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.

Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC₅₀ values of 6.6 nM, 48 nM and 830 nM, and K_i values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research.

Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABA_A receptor associated Cl^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABA_A receptor associated Cl^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.

Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.

Centanafadine (hydrochloride) 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.

Carvedilol (Standard) is the analytical standard of Carvedilol. This product is intended for research and analytical applications. 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.

Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

Clozapine-d₄ is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.

Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC₅₀s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. .

Diclofensine (Ro 8-46500) hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC₅₀ values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.