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| Other names | 2′-Amino-MPTP |
| Drug class | Serotonergic and noradrenergic neurotoxin |
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| Formula | C12H16N2 |
| Molar mass | 188.274 g·mol−1 |
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2′-NH2-MPTP, also known as2′-amino-MPTP, is amonoaminergic neurotoxin that wasderived fromMPTP and is used inscientific research tolesionbrainmonoaminergic systems in animals.[1][2] Whereas MPTP is a selectivedopaminergic neurotoxin, 2′-NH2-MPTP is a specificserotonergic andnoradrenergic neurotoxin that does not affectdopaminergicneurons.[1][2] 2′-NH2-MPTP istransported by theserotonin transporter (SERT) intoserotonergic neurons and by thenorepinephrine transporter (NET) intonoradrenergic neurons, and its serotonergic and noradrenergic neurotoxicity is dependent on this transport by the SERT and NET, respectively.[3][4][5] 2′-NH2-MPTP was first described in thescientific literature by 1993.[1][6]
Selective neurotransmitter depletion was observed with the MPTP analog 1-methyl-4-(2'-aminophenyl)-1-(2'-NH2-MPTP) leading to marked reductions (60-70%) in levels of 5-HT, 5-HIAA and NA in frontal cortex and hippocampus while not affecting striatal DA. In contrast, 1-methyl-4-(2'- methylphenyl)-1,2,3,6-tetrahydropyridine (2'-Me-MPTP) minimally affected 5-HT, 5-HIAA and NA, while markedly reducing (90%) striatal DA content [128].
SERT has some ability to transport other endogenous amines such as dopamine, and also is a drug transporter for agents that include fenfluramine, nonfenfluramine, substituted amphetamines (i.e., MDMA, and parachloroamphetamine), methcathinone, and the serotonin (but not dopamine) neurotoxin amino-MPTP [1-methyl-4-(2′-aminophenyl)-1,2,3,6-tetrahydropyridine], which enters neurons via SERT to induce persistent (months-long) reductions of serotonin accompanied by neurodegenerative changes (11–14).
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