Transporter reversal

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Transporter reversal is the action of reversing a membrane transporter via a process known as phosphorylation. Neurotransmitter transporters normally function as part of the reuptake process, by carrying neurotransmitter chemicals from the extracellular space into the cytoplasm of a presynaptic neuron. When they operate in reverse, they instead carry the neurotransmitter from the cytoplasm into the extracellular space, where it may become capable of binding to postsynaptic receptors. Transporter reversal is utilized by all drugs that act as releasing agents, e.g., amphetamine.


Amphetamine and other similar substances colloquially termed "releasing agents" reverse the transport direction of monoamine transporters through the activation of a presynaptic intracellular receptor called trace amine-associated receptor 1 (TAAR1).[1] TAAR1 signals through protein kinase A and protein kinase C to phosphorylate monoamine transporters, which subsequently either reverse transport direction or withdrawal into the cytoplasm, resulting in non-competitive reuptake inhibition.[1]

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