Drugs of Abuse Affecting 5-HT_2B Receptors
Dino Luethi, Matthias E. Liechti
5-HT2B Receptors January 1, 2021 Peer reviewed DOI: 10.1007/978-3-030-55920-5_16 via Springer Nature
Summary
The 5-hydroxytryptamine 2B (5-HT_2B) receptor is less studied compared to other monoaminergic receptors but plays a role in the effects of serotonergic stimulants and psychedelics. Activation of this receptor can lead to adverse effects, such as cardiac valvulopathy, particularly associated with certain stimulant-type substances. While occasional psychedelic use may not raise significant concerns for valvulopathy, daily or frequent low-dose use, known as 'microdosing,' may present different risks.
Study at a glance
| Key finding | Activation of the 5-HT_2B receptor by serotonergic drugs may lead to adverse effects like cardiac valvulopathy, especially in the context of microdosing. |
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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.