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. 2018 Oct 1;21(10):926-931.
doi: 10.1093/ijnp/pyy047.

Monoamine Transporter and Receptor Interaction Profiles in Vitro Predict Reported Human Doses of Novel Psychoactive Stimulants and Psychedelics

Dino Luethi  1 , Matthias E Liechti  1
Affiliations

Monoamine Transporter and Receptor Interaction Profiles in Vitro Predict Reported Human Doses of Novel Psychoactive Stimulants and Psychedelics

Dino Luethi et al. Int J Neuropsychopharmacol. .

Abstract

Background: Pharmacological profiles of new psychoactive substances can be established rapidly in vitro and provide information on potential psychoactive effects in humans. The present study investigated whether specific in vitro monoamine transporter and receptor interactions can predict effective psychoactive doses in humans.

Methods: We correlated previously assessed in vitro data of stimulants and psychedelics with human doses that are reported on the Internet and in books.

Results: For stimulants, dopamine and norepinephrine transporter inhibition potency was positively correlated with human doses, whereas serotonin transporter inhibition potency was inversely correlated with human doses. Serotonin 5-hydroxytryptamine-2A (5-HT2A) and 5-HT2C receptor affinity was significantly correlated with psychedelic doses, but 5-HT1A receptor affinity and 5-HT2A and 5-HT2B receptor activation potency were not.

Conclusions: The rapid assessment of in vitro pharmacological profiles of new psychoactive substances can help to predict psychoactive doses and effects in humans and facilitate the appropriate scheduling of new psychoactive substances.

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Figures

Figure 1.
Figure 1.
Correlations between dose estimates of stimulants and their transporter inhibition potencies (mean IC50 values).
Figure 2.
Figure 2.
Correlations between dose estimates of psychedelics and their serotonin 5-HT receptor affinities (mean Ki values).
See this image and copyright information in PMC

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