What does VMAT2 do?
The vesicular monoamine transporter 2 (VMAT2) is an integral presynaptic protein that regulates the packaging and subsequent release of dopamine and other monoamines from neuronal vesicles into the synapse.
How does dopamine enter vesicles?
DAT transports dopamine from the extracellular space into the cytosol of the presynaptic terminal. VMAT2 then packages this cytosolic dopamine into vesicular compartments for subsequent release upon neurotransmission. Thus, DAT and VMAT2 act in concert to move transmitter efficiently throughout the neuron.
Which neurotransmitters are monoamines?
Monoamines refer to the particular neurotransmitters dopamine, noradrenaline and serotonin. Dopamine and noradrenaline are sometimes also referred to as catecholamines.
What drug binds with dopamine transporters?
The dopamine transporter (DAT) has been implicated as a primary binding site for several drugs of abuse, including cocaine and methamphetamine (Amara and Kuhar, 1993) as well as for therapeutic drugs such as methylphenidate, mazindol, and bupropion, which are used to treat attention deficit disorder, as an anorexiant …
Where is VMAT2 located?
VMAT2 is primarily expressed in multiple monoaminergic cells in the brain, sympathetic nervous system, mast cells, and histamine containing cells in the gut19–20. VMAT1 and VMAT2 are co-expressed in chromaffin cells of the adrenal medulla.
What blocks VMAT?
VMAT inhibitors include: Reserpine (RES), bietaserpine, and ketanserin (KET) (potent inhibitors of VMAT2 mediated serotonin transport) Tetrabenazine (TBZ) (specific to VMAT2) Phenylethylamine.
What type of transporter is dat?
The dopamine transporter (DAT) is a presynaptic monoamine transporter that mediates dopamine reuptake from the synapse. Cocaine intoxication and addiction are mediated primarily through dopaminergic pathways, with acute effects due to inhibition of dopamine uptake by binding to the DAT.
Is 5ht a monoamine?
Monoamine neurotransmitters, such as 5-HT, norepinephrine (NE), and dopamine (DA), are the important bioactive substances in central nervous system (CNS), which participate in many physiological activities of the body, including emotion, learning, and memory (Wu, Yan, et al., 2016).
How are monoamines inactivated?
All monoamines are derived from aromatic amino acids like phenylalanine, tyrosine, and tryptophan by the action of aromatic amino acid decarboxylase enzymes. They are deactivated in the body by the enzymes known as monoamine oxidases which clip off the amine group.
Which drug mimics serotonin and is taken up by serotonin transporters?
Opiates are natural painkillers. Mimics Serotonin and is more readily taken up by serotonin transporters. It alters the serotonin transporters so they do their jobs in reverse and transport serotonin out of the cell instead of taking them back up.