Search results
Results from the WOW.Com Content Network
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).
They work by competitively and/or noncompetitively inhibiting the norepinephrine transporter (NET) and dopamine transporter (DAT). [1] NDRIs are used clinically in the treatment of conditions including attention deficit hyperactivity disorder (ADHD), narcolepsy, and depression. Examples of well-known NDRIs include methylphenidate and bupropion.
The pharmacology of antidepressants is not entirely clear.. The earliest and probably most widely accepted scientific theory of antidepressant action is the monoamine hypothesis (which can be traced back to the 1950s), which states that depression is due to an imbalance (most often a deficiency) of the monoamine neurotransmitters (namely serotonin, norepinephrine and dopamine). [1]
Below are examples of drugs that act directly by inhibiting two or more MATs simultaneously. Serotonin-norepinephrine re-uptake inhibitors act by blocking both SERTs and NETs. Triple re-uptake inhibitors act by blocking DATs, NETs, and SERTs simultaneously. Most modern antidepressant drugs work on the principle of blocking re-uptake transporters.
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 ...
Serotonin–norepinephrine reuptake inhibitors (SNRIs) such as venlafaxine (Effexor), its active metabolite desvenlafaxine (Pristiq), and duloxetine (Cymbalta) prevent the reuptake of both serotonin and norepinephrine, however their efficacy appears to be only marginally greater than the SSRIs.
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]