Drugs of Abuse Affecting 5-HT_2B Receptors
Dino Luethi, Matthias E. Liechti
5-HT2B Receptors 2021 DOI: 10.1007/978-3-030-55920-5_16 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | MDMA Serotonin |
| Keywords | Stimulants Psychedelics Receptor Valvulopathy Benzofuran Fenfluramine |
| Citations | 3 |
| Key findings | Activation of the 5-HT_2B receptor by serotonergic stimulants and psychedelics may lead to cardiac valvulopathy, especially with frequent microdosing, though occasional psychedelic use likely poses less risk. |
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-HT_2B) receptor represents a relatively little studied target of serotonergic drugs of abuse. However, studies suggest the involvement of 5-HT_2B 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-HT_2B 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-HT_2B 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.
Comparable studies
Other narrative reviews on serotonin, most cited first.
Citations in the library
Cited by 2
- (2-Aminopropyl)benzo[β]thiophenes (APBTs) are novel monoamine transporter ligands that lack stimulant effects but display psychedelic-like activity in mice. Neuropsychopharmacology March 1, 2022
- Pharmacological characterization of 3,4-methylenedioxyamphetamine (MDA) analogs and two amphetamine-based compounds: ,α-DEPEA and DPIA European Neuropsychopharmacology April 1, 2022
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