Mechanism

Dopamine/norepinephrine transporter

Assets acting on this target.

Class
Dopamine/norepinephrine reuptake inhibitor

The dopamine transporter (DAT) and norepinephrine transporter (NET) are membrane proteins that recapture the neurotransmitters dopamine and norepinephrine from the synaptic space after they have been released, ending their signaling and recycling them for reuse. Both transporters belong to a family of sodium-dependent transport proteins found on the surface of nerve terminals. Molecules that inhibit DAT and NET block this reuptake process, leaving more dopamine and norepinephrine available in the synapse to act on their receptors. Because these two catecholamines are central to circuits governing arousal, attention, motivation, and mood, dual DAT/NET inhibition is a mechanism used to promote wakefulness and alertness, and related pathways are also targeted in conditions such as attention-deficit disorders and certain mood disorders. Combining inhibition of both transporters, rather than acting on only one, is thought to produce broader effects on arousal circuits that depend on the interplay of both neurotransmitter systems, compared with a more narrowly selective agent. This class of mechanism is broadly relevant to sleep-wake disorders and to neuropsychiatric conditions in which catecholamine signaling is disrupted.

Research

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