noradrenaline

Norepinephrine bitartrate acts directly on the α- and β-adrenergic receptors. Norepinephrine Bitartrate is a bitartrate salt of norepinephrine, a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine. Clinically, norepinephrine is used as a peripheral vasoconstrictor that causes constriction of arterial and venous beds via its alpha-adrenergic action. It is also used as a potent inotropic and chronotropic stimulator of the heart mediated through its beta-1 adrenergic action.

Norepinephrine bitartrate is a precursor of epinephrine. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

Norepinephrine bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.

It is an isomer of cresotinic acid (2-hydroxy-3-methylbenzoic acid) and oxymethylbenzoic acid (2-methoxybenzoic acid). Derivatives of mandelic acid are formed as a result of metabolism of adrenaline and noradrenaline by monoamine oxidase and catechol-o-methyl transferase. It is also present in certain skin care products, is an intermediate molecule in the production of other biochemicals, may be used as an analytical reagent and is a precursor in the manufacture of dyes. Mandelic acid (acidomandelico) is found to be associated with phenylketonuria, which is an inborn error of metabolism.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

Octopamine hydrochloride ((±)-p-Octopamine hydrochlorid) is a biogenic monoamine structurally associated with noradrenaline. It can serve as a neurohormone, a neurotransmitter, and a neuromodulator in invertebrates.

Octodrine (2-Amino-6-methylheptane) is primarily used as a pharmaceutical intermediate for Octamylamine; it also functions as a local anesthetic and vasoconstrictor.

Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.

D-Phenylalanine, a necessary aromatic amino acid, is a precursor of thyroxine, dopamine, melanin, and noradrenaline (norepinephrine).

Pancuronium dibromide (Pavulon), a competitive AChR antagonist (IC50 = 5.5 nM), acts as a skeletal muscle relaxant. Pancuronium dibromide(Pancuronium bromide) blocking neuromuscular transmission is achieved by competing with acetylcholine for receptor sites on the motor end-plate.

Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a thiophene derivative and selective neurotransmitter uptake inhibitor for serotonin and noradrenaline (SNRI). It is an antidepressant agent and anxiolytic, also used for treating pain in patients with diabetes mellitus and fibromyalgia.

Urantide acetate is a selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-ind

Guanoclor (VATENSOL) (INN), also known as guanochlor, is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.

S 18986 is a selective, orally active, brain-penetrant positive allosteric modulator of AMPA-type receptors that enhances cognition in rodents by inducing the release of noradrenaline and acetylcholine in the rat hippocampus, subsequently improving object-recognition memory.

Iprindole, a tricyclic indole antidepressant, is a dual weak inhibitor of noradrenaline and 5-HT uptake [1].

Venlafaxine hydrochloride (Wy 45030 hydrochloride) is a cyclohexanol and phenylethylamine derivative functioning as a serotonin and noradrenaline reuptake inhibitor (SNRI) used as an antidepressive agent.

Lurasidone hydrochloride (Lurasidone HCl) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.

Selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. Behav

Amezinium methylsulfate (Lu-1631) has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition of noradrenaline and tyramine uptake.

Desvenlafaxine (O-Desmethylvenlafaxine) is a cyclohexanol and phenol derivative and metabolite of venlafaxine that functions as a serotonin and noradrenaline reuptake inhibitor (SNRI) and is used as an antidepressive agent.

D-Amphetamine sulfate, a central nervous system (CNS) stimulant, acts on monoamine transporters to increase noradrenaline, dopamine, and serotonin levels in synapses. Additionally, it serves as an antagonist to the α7 nicotinic acetylcholine receptor (nAChR).

Etozolin HCl is a safe and effective diuretic agent in the treatment of acute cardiac failure. In isolated rings of guinea-pig aorta not responding to acetylcholine, the diuretic dexetozoline did not influence basal vascular tone but inhibited noradrenaline- and histamine-induced contractions. Dexetozoline has a very high bioavailability after oral administration and is fairly lipohilic. The half-life of etozolin is 2.5 h. Dexetozoline accumulates in cirrhosis.

Secoverine is a selective muscarinic receptor antagonist that was studied as a neurotropic spasmolytic agent. It was shown that the drug had no nicotinolytic or antihistaminic activity, a moderate antisterotonic activity, an inhibiting effect on the noradrenaline uptake mechanism of the vas deferens and marked local anesthetic activity.

Bicifadine, also known as DOV-220075, CL 220,075, is a SNDR inhibitor potentially for the treatment of lower back pain. Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs. While the drug is purported to be a serotonin (SERT) and noradrenaline transporter (NET) inhibitor, it also has effects at the dopamine transporter (DAT), effectively making it a broad-spectrum monoamine transporter inhibitor or triple reuptake inhibitor.

Resveratrol is a potent phenolic antioxidant found in grapes, red wine, and various berries that also has antiproliferative and anti-inflammatory activity. cis-Resveratrol is the double bond isomer of trans-resveratrol, the more often studied and naturally abundant of the two resveratrol isomers. cis-Resveratrol exhibits antioxidant activity in the µM range similar to that observed with trans-resveratrol. It blocks production of reactive oxygen species (ROS) by inhibition of NAD(P)H oxidase and also inhibits production of nitric oxide. At a concentration of 100 µM, cis-resveratrol significantly inhibits the expression of genes related to the Rel/NF-κB/IκB family, adhesion molecules, and acute-phase proteins in LPS and INF-γ-stimulated murine peritoneal macrophages. cis-Resveratrol inhibits uptake of noradrenaline and 5-HT by synaptosomes from rat brain with IC50 values of 79 and 51 µM, respectively. It also inhibits human monoamine oxidase-A (MOA-A) and MOA-B with IC50 values of 25 and 61 µM, respectively, which is similar to, but slightly less effective than, values obtained with trans-resveratrol.

(R,R)-Reboxetine mesylate, an antidepressant agent, exhibits high bioavailability and is the (R,R) enantiomer of Reboxetine, a selective noradrenaline reuptake inhibitor. Contrasting its counterpart, the (S,S) enantiomer, this compound demonstrates low affinity for alpha-adrenergic and muscarinic receptors, alongside low toxicity in animals.

Trimipramine N-oxide, an active metabolite of the tricyclic antidepressant trimipramine, effectively inhibits human monoamine transporters for noradrenaline (hNAT), serotonin (hSERT), dopamine (hDAT), and the human organic cation transporters (hOCT1 and hOCT2), with IC50 values of 11.7, 3.59, 9.4, 9.35, and 27.4 nM, respectively. It is utilized in the research of depression and anxiety [1].

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

(±)-Mandelic-2,3,4,5,6-d5 Acid is a deuterated compound of (±)-Mandelic Acid. (±)-Mandelic Acid has a CAS number of 90-64-2. It is an isomer of cresotinic acid (2-hydroxy-3-methylbenzoic acid) and oxymethylbenzoic acid (2-methoxybenzoic acid). Derivatives of mandelic acid are formed as a result of metabolism of adrenaline and noradrenaline by monoamine oxidase and catechol-o-methyl transferase. It is also present in certain skin care products, is an intermediate molecule in the production of other biochemicals, may be used as an analytical reagent and is a precursor in the manufacture of dyes. Mandelic acid is found to be associated with phenylketonuria, which is an inborn error of metabolism.

Dexnafenodone Free Base is a potent inhibitor of noradrenaline, and to a lesser degree of serotonin reuptake, induced changes in the pattern of sleep which are comparable to those of non‐sedating tricyclic antidepressants.

SCH-12650 maleate is a noradrenaline uptake and gastric secretion inhibitor.

S-8510 is a GABA-A receptor inverse agonist. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. S-8510 ameliorated memory impairment induced

Carmoxirole (free base) is a dopamine D2 receptor agonist with limited central activity that modulates sympathetic activation and subsequently reduces pre-load and afterload in animals. It was shown, that carmoxirole induced beneficial effects on hemodynamic and neurohumoral parameters in heart failure. In addition, experimental evidence showed that carmoxirole lowered blood pressure in various models of hypertension mainly or exclusively through inhibition of noradrenaline release from sympathetic nerve endings. That effect of carmoxirole was mediated by presynaptic dopamine receptors with the characteristic that release inhibition was restricted to low rates of sympathetic nerve discharge.

Amezinium is a sympathomimetic drug used for the treatment of low blood pressure. It has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition of noradrenaline and tyramine uptake.

4-Hydroxyatomoxetine D3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.

Tesofensine, a serotonin–noradrenaline–dopamine reuptake inhibitor, is used potentially for the treatment of obesity.

Daurinoline is a non-competitive antagonist, it exerts marked relaxation effect on basilar artery of rabbits through non-competitive antagonism, it would have a protective function on microcirculation of cerebral pia mater, which may be beneficial to relieve cerebral ischemic injury. Daurinoline could significantly reverse noradrenaline induced constriction of pial arterioles and venules, and increase the number of blood vessels which were decreased by noradrenaline.

LY-104119 is a thermogenic weight loss compound that rapidly reduces noradrenaline concentrations in brown adipose tissue between the scapulas, the heart, and the liver.

DSP 4 is a selective neurotoxin selective for noradrenergic neurons in the locus coeruleus noradrenergic system and capable of crossing the blood–brain barrier and cyclizes to a reactive aziridinium derivative that is accumulated into the noradrenergic ne

Lurasidone D8 Hydrochloride is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C, and is the deuterium labeled Lurasidone.

Benzoctamine is an orally active and potent psychoactive agent with tranquillizing properties that increases the turnover rate of catecholamines, enhances the uptake of [3H]noradrenaline in the rat heart, and accelerates the disappearance of intracisternally injected [3H]noradrenaline [1].

Cavα2δ1&NET-IN-3 (example 216) is an inhibitor targeting both the α2δ subunit of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET), exhibiting inhibitory constants (Ki) ranging from 100 to 500 nM for the human α2δ-1 subunit of the Cav2.2 calcium channel and NET, respectively.

Lysyltyrosine TFA (H-Lys-Tyr-OH TFA) is a dipeptide consisting of lysine and tyrosine. It enhances brain function or mitigates neurological diseases by facilitating the release of noradrenaline and tyrosine into the brain [1].

Nisoxetine, a potent and selective noradrenaline transporter (NET) inhibitor with a dissociation constant (Kd) of 0.76 nM, serves as an antidepressant and exhibits local anesthetic properties by blocking voltage-gated sodium channels.

Desethylreboxetine is an desethylated metabolite of Reboxetine (R142000), a selective noradrenaline reuptake inhibitor and an antidepressant.

(+/-)-Venlafaxine-d6 HCl is a deuterated compound of (+/-)-Venlafaxine HCl. (+/-)-Venlafaxine HCl has a CAS number of 99300-78-4. Venlafaxine hydrochloride is a cyclohexanol and phenylethylamine derivative that functions as a SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR (SNRI) and is used as an ANTIDEPRESSIVE AGENT.

Ciclazindol (free base) is a noradrenaline uptake inhibitor.

Nipradolol (KT-210; K-351), an alpha-1-adrenergic receptor antagonist, effectively inhibits the elevation of intraocular pressure (IOP) induced by Phenylephrine in an albino rabbit model, suppresses noradrenaline (NA)-induced muscle contractions, and demonstrates vasodilatory effects on the coronary artery in dogs [1] [2].

Duloxetine-d3 HCl is a deuterated compound of Duloxetine HCl. Duloxetine HCl has a CAS number of 136434-34-9. Duloxetine hydrochloride is a thiophene derivative and selective neurotransmitter uptake inhibitor for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.