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Positive Allosteric Modulation of the 5-HT1A Receptor by Indole-Based Synthetic Cannabinoids Abused by Humans.

Abstract：

:The nonmedical (i.e., recreational) misuse of synthetic cannabinoids (SCs) is a worldwide public health problem. When compared to cannabis, the misuse of SCs is associated with a higher incidence of serious adverse effects, suggesting the possible involvement of noncannabinoid sites of action. Here, we find that, unlike the phytocannabinoid Δ9-tetrahydrocannabinol, the indole-moiety containing SCs, AM2201 and JWH-018, act as positive allosteric modulators (PAMs) at the 5-HT1A receptor (5-HT1AR). This suggests that some biological effects of SCs might involve allosteric interactions with 5-HT1ARs. To test this hypothesis, we examined effects of AM2201 on 5-HT1AR agonist-activated G protein-coupled inwardly rectifying potassium channel currents in neurons in vitro and on the hypothermic response to 5-HT1AR stimulation in mice lacking the cannabinoid receptor 1. We found that both 5-HT1AR effects were potentiated by AM2201, suggesting that PAM activity at 5-HT1AR may represent a novel noncannabinoid receptor mechanism underlying the complex profile of effects for certain SCs.

journal_name

ACS Chem Neurosci

journal_title

ACS chemical neuroscience

authors

Yano H,Adhikari P,Naing S,Hoffman AF,Baumann MH,Lupica CR,Shi L

doi

10.1021/acschemneuro.0c00034

subject

Has Abstract

pub_date

2020-05-20 00:00:00

pages

1400-1405

issue

10

issn

1948-7193

journal_volume

11

pub_type

杂志文章

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