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

Luethi, Dino; Liechti, Matthias E.

doi:10.1093/ijnp/pyy047

The International Journal of Neuropsychopharmacology

2018

DOI: 10.1093/ijnp/pyy047

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

Dino Luethi

¹

,

Matthias E. Liechti

²

Abstract: BackgroundPharmacological 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.MethodsWe correlated previously assessed in vitro data of stimulants and psychedelics with human doses that are reported on the Internet and in books.ResultsFor stimulants, dopamine and no… Show more

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Cited by 64 publications

(60 citation statements)

References 48 publications

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“…The rank order of affinity observed in our study for all the 2C-O and amphetamine-based derivatives at TAAR1 (rat > mouse > human TAAR1) was consistent with previous studies that investigated substituted phenethylamines with various bulky modifications (Lewin et al, 2008; Luethi et al, 2018; Luethi et al, 2019).…”

Section: Discussionsupporting

confidence: 92%

Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines

Kolaczynska

¹

,

Luethi

²

,

Trachsel³

et al. 2019

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Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.

“…The rank order of affinity observed in our study for all the 2C-O and amphetamine-based derivatives at TAAR1 (rat > mouse > human TAAR1) was consistent with previous studies that investigated substituted phenethylamines with various bulky modifications (Lewin et al, 2008; Luethi et al, 2018; Luethi et al, 2019).…”

Section: Discussionsupporting

confidence: 92%

Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines

Kolaczynska

¹

,

Luethi

²

,

Trachsel³

et al. 2019

Self Cite

Get access via publisher Add to collection Cite

Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.

“…In the current study, methylone was a potent inhibitor of norepinephrine uptake and to a lesser extent an inhibitor of dopamine and 5-HT uptake. The N -demethylated metabolite MDC exerted similar 5-HT uptake inhibition potency to methylone but much weaker potency at norepinephrine and dopamine uptake inhibition, suggesting weaker psychotropic effects compared to the parent compound (Luethi and Liechti, 2018), which is in accordance with animal studies (Elmore et al, 2017). The partial dopamine inhibition by HHMC at sub-micromolar concentrations may not be sufficient to produce discernable dopaminergic effects over the course of time after methylone intake.…”

Section: Discussionsupporting

confidence: 81%

Metabolites of the ring-substituted stimulants MDMA, methylone and MDPV differentially affect human monoaminergic systems

Luethi

¹

,

Kolaczynska

²

,

Walter

³

et al. 2019

Self Cite

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Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.

“…Studies investigating the association of 5-HT 1A receptor activation and immune modulation showed that the potent and selective 5-HT 1A receptor agonist DPAT induces lymphocyte proliferation probably by increased translocation of NF-κB into the nucleus (20, 21). However, none of these studies observed immunomodulatory effects of psychedelics, although several psychedelics potently activate the 5-HT 1A receptor (48). We, therefore, assume that the in the current study tested psychedelics are, in contrast to DPAT, not potent or selective enough 5-HT 1A receptor agonists to induce immune modulation.…”

Section: Discussionmentioning

confidence: 73%

Classic psychedelics do not affect T cell and monocyte immune responses

Rudin

¹

,

Areesanan

²

,

Liechti

³

et al. 2023

Get access via publisher Add to collection Cite

Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.

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