noradrenergic

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

Guanfacine hydrochloride (Intuniv) is a centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.

1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effects, seems to be dependent on its interaction with the dopaminergic system, but not with the serotonergic and noradrenergic systems.

Tizanidine, an α2-adrenergic receptor agonist, suppresses the release of neurotransmitters from central nervous system (CNS) noradrenergic neurons.

Brexpiprazole HCl (OPC 34712 dihydrochloride) is a new antipsychotic drug.

Tizanidine hydrochloride (Tizanidine HCl), an α2-adrenergic receptor agonist, inhibits neurotransmitter release from CNS noradrenergic neurons.

DSP-4 hydrochloride (Neurotoxin DSP 4 (hydrochloride)) (Neurotoxin DSP 4 hydrochloride) can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons, mainly those from the locus coeruleus (LC). is a highly selective neurotoxin and readily passes the blood-brain barrier with neurotoxic effects on noradrenergic neurons of adult and developing rats,

RGH-5526 is a novel antihypertensive drug. It causes an increase in hypothalamic norepinephrine (NA) turnover (utilization), and the increase in hypothalamic noradrenergic neuron activity may lead to a decrease in peripheral sympathetic nerve activity, resulting in a significant reduction in blood pressure.

ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels, and enzymes. ONO-2952 is a potent and selective translocator protein 18 kDa (TSPO) antagonist (Ki: 0.33-9.30 nM for rat and human TSPO). ONO-2952 has the potential for i

Pardoprunox (SLV-308) is a partial dopamine D2 agonist and noradrenergic agonist with serotonin 5-HT1A agonist properties, used in trials for treating Early Stage Parkinson's Disease and Advanced Stage Parkinson's Disease.

BE 2254 is an antagonist of central noradrenergic receptor.

R-84760 is a κ-opioid receptor agonist. R-84760 produces an extremely potent antinociceptive effect against tonic pain through the kappa-opioid receptors; the sites of action of subcutaneously administered R-84760 are the supraspinal and spinal loci in th

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

PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg/kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neuronal input transformations by tunable dendritic inhibition. Nat.Neurosci. 15 423 PMID:22246433 |Satoh et al (2016) Context-dependent gait choice elicited by EphA4 mutation in Lbx1 spinal interneurons. Neuron 89 1046 PMID:26924434 |Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Nature 488 172 PMID:22801496 |Hirschberg et al (2017) Functional dichotomy in spinal- vs prefrontal-projecting locus coeruleus modules splits descending noradrenergic analgesia from ascending aversion and anxiety in rats. Elife 6 e29808 PMID:29027903

Moxonidine Hydrochloride serves as a selective agonist for the imidazoline receptor subtype 1 and functions as an antihypertensive agent. It primarily acts within the central nervous system and demonstrates a significant preference for I1 imidazoline receptors over α2-adrenoceptors, with a 40-fold higher affinity. This compound effectively reduces stimulated norepinephrine overflow, indicating its potent efficacy. Despite similar agents like AGN192403 targeting the same receptor, moxonidine's dose-response efficacy remains unaffected. Its ability to lower blood pressure and reduce heart rate is distinctly mediated through imidazoline receptors, reliant on well-preserved noradrenergic pathways within the rostral ventrolateral medulla (RVLM). This interaction is potentially linked to a specific 42 kDa imidazoline receptor protein, emphasizing its unique mechanism of action compared to other drugs like clonidine.

FFN 270 is a fluorescent false neurotransmitter (FFN). Fluorescent substrate for NET and VMAT2. Labels noradrenergic neurons and their synaptic vesicles, and enables imaging of synaptic vesicle content release from specific axonal sitesin vivo. Selectively labels NA neurons over other monoamine and CNS targets. Exhibits two resolved absorption/excitation maxima depending on solvent pH (excitation maxima: 320 nm or 365 nm, emission maxima: 475 nm).

CART(62-76)(human,rat) TFA, a neuropeptide encompassing residues 62-76 of the CART peptide, exhibits neurotransmitter-like properties and modulates the striatal noradrenergic system, as well as the corticostriatal and hypothalamic serotoninergic (5-HT) systems in the rat brain [1].

Dothiepin (Dosulepin; Dothep), an antidepressant with sedative anxiolytic properties, preferentially inhibits noradrenaline over serotonin uptake, enhancing noradrenergic neurotransmission by blocking neuronal reuptake. Additionally, it acts as a histamine H1-receptor antagonist and lacks cardiotoxicity. Its analgesic efficacy is noted in conditions such as psychogenic facial pain, idiopathic fibromyalgia syndrome, and rheumatoid arthritis [1].

3-Methoxy-4-hydroxyphenylglycol (HMPG), a metabolite of norepinephrine degradation in the brain, serves as an indicator of central nervous system noradrenergic activity and is useful for research on depression, chronic schizophrenia, and other conditions [1].

Non-competitive nicotinic cholinergic antagonist; selectively inhibits nicotinic-stimulated catecholamine secretion from chromaffin cells and noradrenergic neurons (IC50 ~ 200 nM). Blocks nicotinic-induced cationic signaling (IC50 ~ 200 - 250 nM) and inhi