Abuse potential of 2-(4-iodo-2, 5-dimethoxyphenyl) N-(2-methoxybenzyl)ethanamine (25I NBOMe); in vivo and ex vivo approaches

Jeon, Seo Young; Kim, Young-Hoon; Kim, Sung Jin; Suh, Soo Jhi; Jin, Hongzhe

doi:10.1016/j.neuint.2019.02.007

Cited by 12 publications

(11 citation statements)

References 40 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Therefore, these results suggest that this compound has a common and alarming feature with them. These results are in line with previous studies showing an increased ex vivo striatal DA levels (Jeon et al, 2019) as well as an increased DA transmission in cortical areas of male rats (Herian et al, 2019). Moreover, 25I-NBOMe seems to act differently on DA and 5-HT levels in male and female rats, highlighting sex differences that might influence the frequency of ingestion, as well as the psychoactive effects and the long-term effects.…”

Section: I-nbome Affects the Dopaminergic Transmission In The Nac Ssupporting

confidence: 92%

“…(Jeon et al, 2019). Conversely, male Sprague-Dawley rats did not press the active lever to obtain an infusion of 25I-NBOMe (Jeon et al, 2019). Collectively, the results available so far suggest a putative abuse liability of this compound, but further investigations on the neurochemical and behavioral effects seem to be necessary.…”

Section: Introductionmentioning

confidence: 91%

“…Moreover, DA levels in mice synaptosomal striatal fractions were increased by in vitro administration of this substance, and male mice showed an increased conditioned place preference when injected with 25I-NBOMe (0.3 mg/kg, i.p.) (Jeon et al, 2019). Conversely, male Sprague-Dawley rats did not press the active lever to obtain an infusion of 25I-NBOMe (Jeon et al, 2019).…”

Section: Introductionmentioning

confidence: 97%

See 2 more Smart Citations

Neurochemical and Behavioral Profiling in Male and Female Rats of the Psychedelic Agent 25I-NBOMe

et al. 2019

View full text Add to dashboard Cite

4-Iodo-2,5-dimethoxy-N-(2-methoxybenzyl)phenethylamine (25I-NBOMe), commonly called "N-Bomb," is a synthetic phenethylamine with psychedelic and entactogenic effects; it was available on the Internet both as a legal alternative to lysergic acid diethylamide (LSD) and as a surrogate of 3,4-methylenedioxy-methamphetamine (MDMA), but now it has been scheduled among controlled substances. 25I-NBOMe acts as full agonist on serotonergic 5-HT2A receptors. Users are often unaware of ingesting fake LSD, and several cases of intoxication and fatalities have been reported. In humans, overdoses of "N-Bomb" can cause tachycardia, hypertension, seizures, and agitation. Preclinical studies have not yet widely investigated the rewarding properties and behavioral effects of this compound in both sexes. Therefore, by in vivo microdialysis, we evaluated the effects of 25I-NBOMe on dopaminergic (DA) and serotonergic (5-HT) transmissions in the nucleus accumbens (NAc) shell and core, and the medial prefrontal cortex (mPFC) of male and female rats. Moreover, we investigated the effect of 25I-NBOMe on sensorimotor modifications as well as body temperature, nociception, and startle/prepulse inhibition (PPI). We showed that administration of 25I-NBOMe affects DA transmission in the NAc shell in both sexes, although showing different patterns; moreover, this compound causes impaired visual responses in both sexes, whereas core temperature is heavily affected in females, and the highest dose tested exerts an analgesic effect prominent in male rats. Indeed, this drug is able to impair the startle amplitude with the same extent in both sexes and inhibits the PPI in male and female rats. Our study fills the gap of knowledge on the behavioral effects of 25I-NBOMe and the risks associated with its ingestion; it focuses the attention on sex differences that might be useful to understand the trend of consumption as well as to recognize and treat intoxication and overdose symptoms.Neuropharmacology of the Synthetic Hallucinogen 25I-NBOMe Miliano et al.

show abstract

Section: I-nbome Affects the Dopaminergic Transmission In The Nac Ssupporting

confidence: 92%

Section: Introductionmentioning

confidence: 91%

Section: Introductionmentioning

confidence: 97%

See 1 more Smart Citation

Neurochemical and Behavioral Profiling in Male and Female Rats of the Psychedelic Agent 25I-NBOMe

et al. 2019

View full text Add to dashboard Cite

show abstract

“…On the contrary, 25N-NBOMe (0.01 mg/kg/infusion) weakly increased the number of infusions/session, but not the active lever pressing/session in mice (Seo J.Y. et al, 2019), whereas 25I-NBOMe (0.03 mg/kg/infusion) did not significantly affect these two SA parameters in rats (Jeon et al, 2019). These findings suggest that 25I-NBOMe, 25B-NBOMe, and 25N-NBOMe might have some dependence liability.…”

Section: Pharmacology Of Nbomesmentioning

confidence: 97%

“…Two behavioral tests, conditioned place preference (CPP) and self-administration (SA), are widely used in studies examining the abuse potential of drugs by analyzing their rewarding and reinforcing effects. 25I-NBOMe (0.3 mg/kg), 25B-NBOMe (1 mg/kg), and 25N-NBOMe (3 mg/kg) produced CPP in mice with a magnitude comparable to 1 mg/kg of methamphetamine (Custodio et al, 2019;Jeon et al, 2019;Seo J.Y. et al, 2019).…”

Section: Pharmacology Of Nbomesmentioning

confidence: 98%

NBOMes–Highly Potent and Toxic Alternatives of LSD

2020

View full text Add to dashboard Cite

Recently, a new class of psychedelic compounds named NBOMe (or 25X-NBOMe) has appeared on the illegal drug market. NBOMes are analogs of the 2C family of phenethylamine drugs, originally synthesized by Alexander Shulgin, that contain a N-(2-methoxy)benzyl substituent. The most frequently reported drugs from this group are 25I-NBOMe, 25B-NBOMe, and 25C-NBOMe. NBOMe compounds are ultrapotent and highly efficacious agonists of serotonin 5-HT 2A and 5-HT 2C receptors (Ki values in low nanomolar range) with more than 1000-fold selectivity for 5-HT 2A compared with 5-HT 1A. They display higher affinity for 5-HT 2A receptors than their 2C counterparts and have markedly lower affinity, potency, and efficacy at the 5-HT 2B receptor compared to 5-HT 2A or 5-HT 2C. The drugs are sold as blotter papers, or in powder, liquid, or tablet form, and they are administered sublingually/buccally, intravenously, via nasal insufflations, or by smoking. Since their introduction in the early 2010s, numerous reports have been published on clinical intoxications and fatalities resulting from the consumption of NBOMe compounds. Commonly observed adverse effects include visual and auditory hallucinations, confusion, anxiety, panic and fear, agitation, uncontrollable violent behavior, seizures, excited delirium, and sympathomimetic signs such mydriasis, tachycardia, hypertension, hyperthermia, and diaphoresis. Rhabdomyolysis, disseminated intravascular coagulation, hypoglycemia, metabolic acidosis, and multiorgan failure were also reported. This survey provides an updated overview of the pharmacological properties, pattern of use, metabolism, and desired effects associated with NBOMe use. Special emphasis is given to cases of nonfatal and lethal intoxication involving these compounds. As the analysis of NBOMes in biological materials can be challenging even for laboratories applying modern sensitive techniques, this paper also presents the analytical methods most commonly used for detection and identification of NBOMes and their metabolites.

show abstract

Tolerance to neurochemical and behavioral effects of the hallucinogen 25I-NBOMe

et al. 2021

View full text Add to dashboard Cite

Rationale 4-Iodo-2,5-dimethoxy-N-(2-methoxybenzyl)phenethylamine (25I-NBOMe) is a potent serotonin 5-HT2A/2C receptor agonist with hallucinogenic activity. There is no data on the 25I-NBOMe effect on brain neurotransmission and animal performance after chronic administration. Objectives We examined the effect of a 7-day treatment with 25I-NBOMe (0.3 mg/kg/day) on neurotransmitters’ release and rats’ behavior in comparison to acute dose. Methods Changes in dopamine (DA), serotonin (5-HT), acetylcholine (ACh), and glutamate release were studied using microdialysis in freely moving rats. The hallucinogenic activity was measured in the wet dog shake (WDS) test. The animal locomotion was examined in the open field (OF) test, short-term memory in the novel object recognition (NOR) test. The anxiogenic/anxiolytic properties of the drug were tested using the light/dark box (LDB) test. Results Repeated administration of 25I-NBOMe decreased the response to a challenge dose of DA, 5-HT, and glutamatergic neurons in the frontal cortex as well as weakened the hallucinogenic activity in comparison to acute dose. In contrast, striatal and accumbal DA and 5-HT release and accumbal but not striatal glutamate release in response to the challenge dose of 25I-NBOMe was increased in comparison to acute treatment. The ACh release was increased in all brain regions. Behavioral tests showed a motor activity reduction and memory deficiency in comparison to a single dose and induction of anxiety after the drug’s chronic and acute administration. Conclusions Our findings suggest that multiple injections of 25I-NBOMe induce tolerance to hallucinogenic activity and produce alterations in neurotransmission. 25I-NBOMe effect on short-term memory, locomotor function, and anxiety seems to be the result of complex interactions between neurotransmitter pathways.

show abstract

Abuse potential of 2-(4-iodo-2, 5-dimethoxyphenyl) N-(2-methoxybenzyl)ethanamine (25I NBOMe); in vivo and ex vivo approaches

Cited by 12 publications

References 40 publications

Neurochemical and Behavioral Profiling in Male and Female Rats of the Psychedelic Agent 25I-NBOMe

Neurochemical and Behavioral Profiling in Male and Female Rats of the Psychedelic Agent 25I-NBOMe

NBOMes–Highly Potent and Toxic Alternatives of LSD

Tolerance to neurochemical and behavioral effects of the hallucinogen 25I-NBOMe

Contact Info

Product

Resources

About