Naphthylisopropylamine
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Oral |
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| Synonyms | 1-(2-naphthyl)-2-aminopropane; alpha-methylnapthylethylamine |
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| Formula | C13H15N |
| Molar mass | 185.27 g/mol |
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Naphthylisopropylamine (PAL-287) is an experimental drug currently under investigation for the treatment of alcohol and stimulant addiction.
Naphthylisopropylamine acts as a non-neurotoxicreleasing agent of serotonin, norepinephrine, and dopamine, with EC50 values of 3.4 nM, 11.1 nM, and 12.6 nM, respectively. It also has affinity for the 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50 values = 466 nM, 40 nM, and 2.3 nM, respectively), and acts as a full agonist at 5-HT2B and as a partial agonist at 5-HT2C, while its affinity for 5-HT2A is probably too low to be significant.
In animal studies, naphthylisopropylamine was shown to reduce cocaine self-administration, yet produced relatively weak stimulant effects when administered alone, being a (much) lesser stimulant than d-amphetamine for comparison. Further research is now being conducted in primates to see if it will be a useful substitute for treating drug addiction in humans as well.
An important observation is that in behavioral studies, rodents would consistently self-administer selective norepinephrine and dopamine releasing agents such as d-amphetamine, yet compounds that also release serotonin like naphthylisopropylamine would not be self-administered. In addition to the drugs (acute) effects on self-administration, all of the available evidence suggests that the locomotor activation caused by the majority of dopamine releasers is also dampened when the drugs also cause serotonergic release. In fact, PAL-287 causes no locomotor activation at all (although admittedly the tests were only after acute dosing).
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