Hallucinogen-Like Action of the Novel Designer Drug 25I-NBOMe and Its Effect on Cortical Neurotransmitters in Rats
Monika Herian, Adam Wojtas, Katarzyna Kamińska, Paweł Świt, Anna Wach, Krystyna Gołembiowska
Neurotoxicity Research April 15, 2019 DOI: 10.1007/s12640-019-00033-x (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Rats |
| Intervention | 25I-NBOMe |
| Dose | 1, 3, and 10 mg/kg |
| Topics | LSD Serotonin |
| Keywords | Hallucinogen Neurochemical Microdialysis Homovanillic acid Pharmacology Monoamine neurotransmitter Dopamine Extracellular 5-HT Receptor |
| Citations | 44 |
| Key findings | 25I-NBOMe increases extracellular dopamine, serotonin, and glutamate in the rat frontal cortex and induces head-twitch response, with dose-response patterns suggesting hallucinogenic activity mediated by glutamate release via 5-HT2A receptors. |
Abstract
NBOMes are N-benzylmethoxy derivatives of the 2C family hallucinogens. 4-Iodo-2,5-dimethoxy-N-(2-methoxybenzyl)phenethylamine (25I-NBOMe) is one of the commonly used illicit drugs. It exhibits high binding affinity for 5-HT 2A/C and 5-HT 1A serotonin receptors. Activation of 5-HT 2A receptor induces head-twitch response (HTR) in rodents, a behavioral marker of hallucinogen effect in humans. There is not much data on neurochemical properties of NBOMes. Therefore, we aimed to investigate the effect of 25I-NBOMe on extracellular level of dopamine (DA), serotonin (5-HT), and glutamate (GLU) in the rat frontal cortex, tissue contents of monoamines, and hallucinogenic activity in rats. The extracellular levels of DA, 5-HT, and GLU were studied using microdialysis in freely moving animals. The tissue contents of DA, 5-HT and their metabolites 3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), and 5-hydroxyindoleacetic acid (5-HIAA) were determined in the rat frontal cortex. We also tested a drug-elicited HTR. 25I-NBOMe at doses 1, 3, and 10 mg/kg (sc) increased extracellular DA, 5-HT, and GLU levels, enhanced tissue content of 5-HT and 5-HIAA, but did not affect tissue level of DA and its metabolites. The compound exhibited an inverted U -shaped dose-response curve with respect to the effect on extracellular DA and 5-HT levels, but a U -shaped dose-response curve was observed for its effect on GLU release and HTR. The data from our study suggest that hallucinogenic activity of 25I-NBOMe seems to be related with the increase in extracellular GLU level-mediated via cortical 5-HT 2A receptors. The influence of 25I-NBOMe on 5-HT 2C and 5-HT 1A receptors may modulate its effect on neurotransmitters and HTR.
Comparable studies
Other preclinical and animal studies on LSD, most cited first.
Citations in the library
Cited by 30
- Designer drugs: mechanism of action and adverse effects Archives of Toxicology April 1, 2020
- Effect of Psilocybin and Ketamine on Brain Neurotransmitters, Glutamate Receptors, DNA and Rat Behavior International Journal of Molecular Sciences June 16, 2022
- NBOMes–Highly Potent and Toxic Alternatives of LSD Frontiers in Neuroscience February 26, 2020
- Sex and Gender Differences in the Effects of Novel Psychoactive Substances. Brain Sciences September 3, 2020
- Neurochemical and Behavioral Effects of a New Hallucinogenic Compound 25B-NBOMe in Rats Neurotoxicity Research December 18, 2020
and 25 more in the library
Cites 32
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and 27 more in the library