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Norepinephrine Epinephrine. A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline) by blocking the action of the norepinephrine transporter (NET).
The norepinephrine transporter (NET) serves as the fundamental mechanism for the inactivation of noradrenergic signaling because of the NET termination in the reuptake of norepinephrine (NE). The selectivity and mechanism of action for the NRI drugs remain mostly unresolved and, to date, only a limited number of NRI-selective inhibitors are ...
The norepinephrine transporter (NET), also known as noradrenaline transporter (NAT), is a protein that in humans is encoded by the solute carrier family 6 member 2 (SLC6A2) gene. [ 5 ] NET is a monoamine transporter and is responsible for the sodium-chloride (Na + /Cl − )-dependent reuptake of extracellular norepinephrine (NE), which is also ...
A norepinephrine–dopamine reuptake inhibitor (NDRI) is a type of drug that inhibits the reuptake of the monoamine neurotransmitters norepinephrine and dopamine and thereby increases extracellular levels of these neurotransmitters and noradrenergic and dopaminergic neurotransmission. [1]
3 H-nisoxetine (3 H-NIS), on the other hand, is a potent and selective inhibitor for the uptake of norepinephrine [13] and is now used as a selective marker of the norepinephrine transporter. [14] Most studies using 3 H-NIS are conducted in the rat model, and not many have been performed in humans.
It shows high affinity for both the norepinephrine transporter (NET) and the serotonin transporter (SERT), with 4-fold selectivity for the NET over the SERT, and is thought to act as a dual serotonin–norepinephrine reuptake inhibitor (SNRI) at higher doses. [4] [1] As of November 2023, ampreloxetine is in phase 3 clinical trials for NOH. [2]
Serotonin-norepinephrine reuptake inhibitors Bicifadine Desvenlafaxine Duloxetine Eclanamine Levomilnacipran Milnacipran Sibutramine Venlafaxine Serotonin-norepinephrine-dopamine reuptake inhibitors Brasofensine Diclofensine DOV-102,677 DOV-21,947 DOV-216,303 JNJ-7925476 JZ-IV-10 Methylnaphthidate Naphyrone NS-2359 PRC200-SS SEP-225,289 SEP ...
In 1993, a new drug was introduced to the US market called venlafaxine, a serotonin–norepinephrine reuptake inhibitor. [20] Venlafaxine was the first compound described in a new class of antidepressant substances called phenylethylamines .