Effect of JWH-250, JWH-073 and their interaction on “tetrad”, sensorimotor, neurological and neurochemical responses in mice

Ossato, Andrea; Canazza, Isabella; Trapella, Claudio; Vincenzi, Fabrizio; Luca, Maria Antonietta De; Rimondo, Claudia; Varani, Katia; Borea, Pier Andrea; Serpelloni, Giovanni; Marti, Matteo

doi:10.1016/j.pnpbp.2016.01.007

Cited by 64 publications

(110 citation statements)

References 103 publications

(171 reference statements)

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“…The wide range of doses of 1‐cyclohexyl‐x‐methoxybenzene derivatives tested (0.1–100 mg/kg i.p.) were chosen based on previous safety pharmacology studies on NPS (Vigolo et al, ; Ossato et al, , ).…”

Section: Methodsmentioning

confidence: 99%

“…For the lateral visual response, a small dentist's mirror was moved into the mice's field of view in a horizontal arc, until the stimulus was between the mice's eyes. The procedure was conducted bilaterally (Ossato et al, , ) and was repeated three times. The score assigned was a value of 1 if there was a reflection in the mouse movement, or 0 if not.…”

Section: Methodsmentioning

confidence: 99%

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1‐cyclohexyl‐x‐methoxybenzene derivatives, novel psychoactive substances seized on the internet market. Synthesis and in vivo pharmacological studies in mice

Fantinati

Ossato

Bianco

et al. 2017

Human Psychopharmacology

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For the first time, this study demonstrates that systemic administration of 1-cyclohexyl-x-methoxybenzene compounds markedly inhibit visual response, promote analgesia, and induce core temperature alterations in mice. This data, although obtained in animal model, suggest their possible hazard for human health (i.e., hyperthermia and sensorimotor alterations). In particular, these novel psychoactive substances may have a negative impact in many daily activities, greatly increasing the risk factors for workplace accidents and traffic injuries.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

1‐cyclohexyl‐x‐methoxybenzene derivatives, novel psychoactive substances seized on the internet market. Synthesis and in vivo pharmacological studies in mice

Fantinati

Ossato

Bianco

et al. 2017

Human Psychopharmacology

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“…Nevertheless, controlled laboratory studies in animals have recently been performed and support the notion that high efficacy SCBs exhibit unexpected pro-convulsant effects. For example, the SCB AKB48 and its fluorinated analogue 5F-AKB48 [23] as well as the aminoalkylindoles JWH-015 and JWH-073 [60] all induced impaired visual, acoustic and tactile sensorimotor responses, convulsions, myoclonia and hyperreflexia in mice. Similarly, the aminoalkylindole SCBs JWH-018, JWH-073, JWH-210, AM-2201 and JWH-167 all increased central nervous system excitability in a functional observation battery in mice, with JWH-018 being “especially active” in this regard [61].…”

Section: Distinct Scb Toxicity In Humans - Issues For Special Concernmentioning

confidence: 99%

“…The selective CB 1 cannabinoid antagonist rimonabant reverses the effects of these SCBs in a functional observational battery in mice ( e.g., muscle tone, equilibrium, sensorimotor activity, alertness, ease of handling and autonomic effects). Furthermore, sensorimotor dysfunction in mice produced by JWH-018, JWH-250 and JWH-073 [60, 167], and impaired motor activity and seizures resulting from JWH-018 and JWH-018-Br [168] are all normalized by co-administration with CB 1 cannabinoid receptor antagonists rimonabant and AM-251. Finally, antinociception and hypothermic effects produced by the SCBs CP-55,950, WIN-55,212-2, JWH-073, A-834,735D and CP-47,497 are absent in CB 1 cannabinoid receptor knockout mice [169].…”

Section: Scb Toxicity - Cb1 Versus Non-cb1 Cannabinoid Receptor Targetsmentioning

confidence: 99%

“…Since SCBs lack appreciable affinity for non-CB 1 cannainoid receptor targets [61] and almost all acute SCB responses in animals are blocked by co-administration with CB 1 cannabinoid receptor antagonists ( e.g., rimonabant or AM-251) [60, 61, 167–169], it is unfortunate that clinical studies to examine the potential use of CB 1 cannabinoid receptor antagonists for treatment of acute SCB overdose in emergency departments have not been conducted. The CB 1 cannabinoid receptor antagonist/inverse agonist rimonabant was withdrawn from clinical trials for use in obesity by the European Medicines Agency in October of 2008 due to adverse psychiatric consequences [184].…”

Section: “Antidote” For Acute Scb Toxicity – Selective Cb1 Cannabinoimentioning

confidence: 99%

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Synthetic Pot: Not Your Grandfather’s Marijuana

Ford

Tai

Fantegrossi

et al. 2017

Trends in Pharmacological Sciences

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In the early 2000’s in Europe and shortly thereafter in the USA, it was reported that “legal” forms of marijuana were being sold under the name K2 and/or Spice. Active ingredients in K2/Spice products were determined to be synthetic cannabinoids (SCBs), producing psychotropic actions via CB1 cannabinoid receptors, similar to those of Δ9-THC, the primary active constituent in marijuana. Often abused by adolescents and military personnel to elude detection in drug tests due to their lack of structural similarity to Δ9-THC, SCBs are falsely marketed as safe marijuana substitutes. Instead, SCBs are a highly structural diverse group of compounds, easily synthesized, which produce very dangerous adverse effects occurring by, as of yet, unknown mechanisms. Therefore, available evidence indicates that K2/Spice products are clearly not safe marijuana alternatives.

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Doping control analysis of four JWH‐250 metabolites in equine urine by liquid chromatography–tandem mass spectrometry

You

Proctor

Vasilko

et al. 2018

Drug Testing and Analysis

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JWH-250 is a synthetic cannabinoid. Its use is prohibited in equine sport according to the Association of Racing Commissioners International (ARCI) and the Fédération Équestre Internationale (FEI). A doping control method to confirm the presence of four JWH-250 metabolites (JWH-250 4-OH-pentyl, JWH-250 5-OH-pentyl, JWH-250 5-OH-indole, and JWH-250 N-pentanoic acid) in equine urine was developed and validated. Urine samples were treated with acetonitrile and evaporated to concentrate the analytes prior to the analysis by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The chromatographic separation was carried out using a Phenomenex Lux ® 3 μm AMP column (150 x 3.0 mm). A triple quadrupole mass spectrometer was used for detection of the analytes in positive mode electrospray ionization using multiple reaction monitoring (MRM). The limits of detection, quantification, and confirmation for these metabolites were 25, 50, and 50 pg/mL, respectively. The linear dynamic range of quantification was 50-10000 pg/mL. Enzymatic hydrolysis indicated that JWH-250 4-OH-pentyl, JWH-250 5-OH-pentyl, and JWH-250 5-OH indole are highly conjugated whereas JWH-250 N-pentanoic acidis not conjugated. Relative retention time and product ion intensity ratios were employed as the criteria to confirm the presence of these metabolites in equine urine.The method was successfully applied to post-race urine samples collected from horses suspected of being exposed to JWH-250. All four JWH-250 metabolites were confirmed in these samples, demonstrating the method applicability for equine doping control analysis. KEYWORDSDoping control analysis, Equine urine, JWH-250 metabolites, LC-MS/MS

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Effect of JWH-250, JWH-073 and their interaction on “tetrad”, sensorimotor, neurological and neurochemical responses in mice

Cited by 64 publications

References 103 publications

1‐cyclohexyl‐x‐methoxybenzene derivatives, novel psychoactive substances seized on the internet market. Synthesis and in vivo pharmacological studies in mice

1‐cyclohexyl‐x‐methoxybenzene derivatives, novel psychoactive substances seized on the internet market. Synthesis and in vivo pharmacological studies in mice

Synthetic Pot: Not Your Grandfather’s Marijuana

Doping control analysis of four JWH‐250 metabolites in equine urine by liquid chromatography–tandem mass spectrometry

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