norepinephrine transporter (net)

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Atomoxetine (HSDB 7352) is a selective norepinephrine inhibitor that may cause an increase in blood pressure by increasing norepinephrine concentrations in peripheral sympathetic neurons .Atomoxetine is a highly selective antagonist of presynaptic norepinephrine transporters with little or no affinity for other norepinephrine receptors or other neurotransmitter transporters or receptors, but has little or no affinity for 5- hydroxytryptamine transporter. Atomoxetine selectively inhibits reuptake of norepinephrine and can be used to treat adolescents with ADHD and chronic tics.

Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.

SPD-473 citrate (BTS 74398 citrate) is a dopamine reuptake inhibitor, a norepinephrine transporter protein (NET) inhibitor, and a 5-hydroxytryptamine reuptake inhibitor, and is used in the study of neurological disorders and endocrine and metabolic diseases.

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Atomoxetine hydrochloride (LY 139603) is the hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft. The effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.

Adrenalone hydrochloride (Adrenalone HCl) is a dopamine β-oxidase inhibitor with a similar structure to the norepinephrine transporter (NET) ligand, with an IC50 of 36.9 μM. It is an adrenergic agonist that acts as a local vasoconstrictor and hemostatic agent.

Milnacipran hydrochloride (Savella) is a serotonin and norepinephrine reuptake inhibitor used to treat major depressive disorders. Milnacipran hydrochloride is an enantiomer of milnacipran, which is used to treat fibromyalgia. Milnacipran hydrochloride and milnacipran have been associated with a low rate of transient elevations in serum aminotransferase levels during treatment and with rare instances of clinically apparent acute liver injury with jaundice.

Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) is an inhibitor of Rho-related protein kinase (ROCK) and norepinephrine transporter (NET) and is effective in reducing intraocular pressure (IOP).

3,4-Dihydroxypyrovalerone HCl is an analog of Pyrovalerone. Pyrovalerone inhibits the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET).

Nisoxetine hydrochloride is a noradrenaline transporter (NET) inhibitor

JNJ-7925476 HCl is a triple monoamine uptake inhibitor. JNJ-7925476 Salt blocks the dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter (SERT) in the central nervous system. The ED(50) values for JNJ-7925476 occupancy of

4'-hydroxy Atomoxetine glucuronide is a metabolite of the norepinephrine transporter (NET) inhibitor atomoxetine .1It is formed from atomoxetine by glucuronidation of the intermediate metabolite 4-hydroxy atomoxetine.2 1.Todor, I., Popa, A., Neag, M., et al.Evaluation of a potential metabolism-mediated drug-drug interaction between atomoxetine and bupropion in healthy volunteersJ. Pharm. Pharm. Sci.19(2)198-207(2016) 2.Sauer, J.-M., Ring, B.J., and Witcher, J.W.Clinical pharmacokinetics of atomoxetineClin. Pharmacokinet.44(6)571-590(2005)

TAS-303 is a selective norepinephrine reuptake inhibitor which displays significant norepinephrine transporter (NET) inhibitory activity toward serotonin or dopamine transporters. Radioligand-binding studies showed that TAS-303 selectively and potently inhibited [3H]norepinephrine binding to the human NET.

Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in rat brain and peripheral tissues. It reduces isolation-induced aggressive behavior and inhibits electrical foot-shock stimulation-induced belligerence in mice when administered at doses ranging from 3 to 10 mg kg. Maprotiline also reduces aggressive behavior in rhesus monkeys housed in groups. Formulations containing maprotiline have been used in the treatment of depression and anxiety.

(S)-5-hydroxy-6-methoxy Duloxetine, an active metabolite of the (S)-duloxetine, functions as a serotonin (5-HT) and norepinephrine reuptake inhibitor. Its formation occurs through the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6 via a 5- or 6-hydroxy duloxetine intermediate, followed by a catechol duloxetine intermediate. This compound effectively inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) across lipid membranes, with inhibition constants (Kis) of 266, 920, and 2,814 nM, respectively, for human transporters.

SRI-29574 acts as an allosteric modulator of the dopamine transporter (DAT), partially inhibiting its uptake (IC50=2.3 nM) while also moderately inhibiting the uptake of serotonin transporter (SERT) and norepinephrine transporter (NET). This compound serves as a valuable probe for researching the function and regulatory mechanisms of DAT.