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Amphetamine


Mechanism of action:

When amphetamine reaches the presynaptic nerve terminal, it enters neurons through transporters such as the norepinephrine transporter (NET) and dopamine transporter (DAT). It is then transported into synaptic vesicles via VMAT2 (vesicular monoamine transporter 2), where it disrupts the vesicular proton gradient, causing norepinephrine and dopamine to leak from the vesicles into the cytoplasm. These neurotransmitters are subsequently released into the synaptic cleft through reverse transport via NET and DAT, thereby increasing norepinephrine and dopamine activity in the central nervous system.

Reference(s):

1. Wu X et al. (1998). cDNA sequence, transport function, and genomic organization of human OCTN2, a new member of the organic cation transporter family. Biochem Biophys Res Commun. 


2. Wu X et al. (1999). Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. J Pharmacol Exp Ther. 


3. Rytting E et al. (2005). Novel organic cation transporter 2-mediated carnitine uptake in placental choriocarcinoma (BeWo) cells. J Pharmacol Exp Ther.

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