Pharmacokinetics, systemic toxicity, thermoregulation and acute behavioural effects of 25CN‐NBOMe

N‐(2‐methoxybenzyl)phenethylamines (NBOMes) are a family of potent 5‐HT2A agonists containing substances emerging on the illicit drug market as a replacement for N,N‐diethyllysergamide (LSD). Despite the increasing use of NBOMes for diagnostic, research and recreational purposes, only a limited numb...

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Published in:Addiction biology 2022-09, Vol.27 (5), p.e13216-n/a
Main Authors: Šíchová, Klára, Syrová, Kateřina, Kofroňová, Edita, Pinterova‐Leca, Nikola, Vejmola, Čestmír, Nykodemová, Jitka, Palivec, Petr, Olejníková, Lucie, Danda, Hynek, Jorratt, Pascal, Adam, Šafanda, Hiep, Bui Quang, Štefková‐Mazochová, Kristýna, Končická, Markéta, Kuchař, Martin, Páleníček, Tomáš
Format: Article
Language:English
Subjects:
25CN
Animals
Arrhythmia
behavioural study
Benzonitrile
Blood-brain barrier
Body temperature
Body Temperature Regulation
Dose-Response Relationship, Drug
Drug dosages
Hallucinogens - pharmacology
Lethal dose
Locomotor activity
Lysergide
NBOMe
novel psychoactive substances
Open-field behavior
Pharmacokinetics
Phenethylamines
Rats
Rats, Wistar
Sensorimotor gating
Startle response
Thermoregulation
Toxicity
Wistar rat
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Summary:N‐(2‐methoxybenzyl)phenethylamines (NBOMes) are a family of potent 5‐HT2A agonists containing substances emerging on the illicit drug market as a replacement for N,N‐diethyllysergamide (LSD). Despite the increasing use of NBOMes for diagnostic, research and recreational purposes, only a limited number of studies have focussed on their in vivo effect. Here, we investigated pharmacokinetics, systemic toxicity, thermoregulation in individually and group‐housed animals, and acute behavioural effects after subcutaneous administration of 2,5‐dimethoxy‐4‐(2‐((2‐methoxybenzyl)amino)ethyl)benzonitrile (25CN‐NBOMe; 0.2, 1, and 5 mg/kg) in Wistar rats. Drug concentration peaked 1 h after the administration of 5 mg/kg in both blood serum and brain tissue with a half‐life of 1.88 and 2.28 h, respectively. According to Organisation for Economic Co‐operation and Development 423 toxicity assay, the drug is classified into category 3 with a lethal dose of 300 mg/kg and an estimated LD50 value of 200 mg/kg. Histological examination of organs collected from rats injected with the lethal dose revealed subtle pathological changes, highly suggestive of acute cardiovascular arrest due to malignant arrhythmia. Altered thermoregulation after 5 mg/kg was demonstrated by reduced body temperature in individually housed rats (p 
ISSN:1355-6215
1369-1600
DOI:10.1111/adb.13216