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Drugs of Abuse Affecting 5-HT2B Receptors

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5-HT2B Receptors

Part of the book series: The Receptors ((REC,volume 35))

Abstract

Stimulant and psychedelic drugs of abuse exert their effects through interactions with monoaminergic systems. Compared to other monoaminergic receptors and transporters, the 5-hydroxytryptamine 2B (5-HT2B) receptor represents a relatively little studied target of serotonergic drugs of abuse. However, studies suggest the involvement of 5-HT2B receptors in the mechanism of action of serotonergic stimulants and receptor activation may additionally lead to specific adverse effects such as cardiac valvulopathy in users. 5-HT2B receptor activation has been demonstrated for stimulant-type new psychoactive substances of the benzofuran class and for substituted amphetamines with a distinct serotonergic vs. dopaminergic profile. Besides stimulants, many psychedelic drugs activate the 5-HT2B receptor but the consequence thereof remains unclear. Cardiac valvulopathy is likely not an adverse effect to consider when psychedelics are used occasionally but this may be different for “microdosing” which involves low doses of psychedelics taken daily or multiple times per week.

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Abbreviations

MDA:

3,4-methylenedioxyamphetamine

MDMA:

3,4-methylenedioxymethamphetamine

CYP:

Cytochrome P450

LSD:

Lysergic acid diethylamide

NPS:

New psychoactive substances

SERT:

Serotonin transporter

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Authors and Affiliations

  1. Division of Clinical Pharmacology and Toxicology, University Hospital Basel and University of Basel, Basel, Switzerland

    Dino Luethi & Matthias E. Liechti

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  1. Dino Luethi
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  2. Matthias E. Liechti
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Correspondence to Dino Luethi .

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Editors and Affiliations

  1. Inserm, U1270, Institut du Fer a Moulin, Paris, France

    Luc Maroteaux

  2. Pharmacology, Strasbourg Medical school, Strasbourg, France

    Laurent Monassier

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Luethi, D., Liechti, M.E. (2021). Drugs of Abuse Affecting 5-HT2B Receptors. In: Maroteaux, L., Monassier, L. (eds) 5-HT2B Receptors. The Receptors, vol 35. Springer, Cham. https://doi.org/10.1007/978-3-030-55920-5_16

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