Mechanism of Action of Selective Monoaminergic Reuptake Inhibitors

During neurotransmission, monoamine neurotransmitters such as serotonin, dopamine or norepinephrine, are released into the synaptic cleft from storage vesicles present in the pre-synaptic neuron (Figure A). The neurotransmitters then bind to their respective receptors on the post-synaptic neuron, thereby transferring the signal. The actions of the neurotransmitters are terminated via their reuptake into the pre-synaptic neuron via specific transporter proteins following which the neurotransmitter is taken up into the vesicles for re-release. When a monoaminergic reuptake inhibitor is present (Figure B), it binds to the monoamine transporter and blocks the reuptake of the neurotransmitter whose levels increase in the synaptic cleft thereby enhancing neurotransmission.

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