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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 monoamine reuptake inhibitor (MRI) [1] is a drug that acts as a reuptake inhibitor of one or more of the three major monoamine neurotransmitters serotonin, norepinephrine, and dopamine by blocking the action of one or more of the respective monoamine transporters (MATs), which include the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT).
Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine.Guanethidine is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself (NET, uptake 1), and uptake is essential for the drug's action.
Monoamine transporters are members of the group of Na + /Cl −-dependent substrate-specific neuronal membrane transporters belonging to the SLC6 gene family. [5] MATs are large integral membrane proteins composed of 12 transmembrane domains connected by intracellular and extracellular loops.
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]
Specific transporter proteins called monoamine transporters that transport monoamines in or out of a cell exist. These are the dopamine transporter (DAT), serotonin transporter (SERT), and the norepinephrine transporter (NET) in the outer cell membrane and the vesicular monoamine transporter (VMAT1 and VMAT2) in the membrane of intracellular ...
The first commercially available selective norepinephrine reuptake inhibitor (sNRI) was reboxetine (Edronax) and was developed as a first-line therapy for major depressive disorder. [29] The selectivity of reboxetine for the norepinephrine transporter (NET) results in benign side effect profile because the drug is well tolerated. [11]
It does this by concomitantly inhibiting the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT), respectively. Inhibition of the reuptake of these neurotransmitters increases their extracellular concentrations and, therefore, results in an increase in serotonergic , adrenergic , and dopaminergic ...