دورية أكاديمية
In Vitro and In Vivo Pharmaco-Toxicological Characterization of 1-Cyclohexyl-x-methoxybenzene Derivatives in Mice: Comparison with Tramadol and PCP
| العنوان: | In Vitro and In Vivo Pharmaco-Toxicological Characterization of 1-Cyclohexyl-x-methoxybenzene Derivatives in Mice: Comparison with Tramadol and PCP |
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| المؤلفون: | Sabrine Bilel, Micaela Tirri, Raffaella Arfè, Chiara Sturaro, Anna Fantinati, Virginia Cristofori, Tatiana Bernardi, Federica Boccuto, Marco Cavallo, Alessandro Cavalli, Fabio De-Giorgio, Girolamo Calò, Matteo Marti |
| المصدر: | International Journal of Molecular Sciences, Vol 22, Iss 14, p 7659 (2021) |
| بيانات النشر: | MDPI AG, 2021. |
| سنة النشر: | 2021 |
| المجموعة: | LCC:Biology (General) LCC:Chemistry |
| مصطلحات موضوعية: | 1-cyclohexyl-x-methoxybenzene, opioid receptors, tramadol, PCP, behavior, mice, Biology (General), QH301-705.5, Chemistry, QD1-999 |
| الوصف: | 1-cyclohexyl-x-methoxybenzene is a novel psychoactive substance (NPS), first discovered in Europe in 2012 as unknown racemic mixture of its three stereoisomers: ortho, meta and para. Each of these has structural similarities with the analgesic tramadol and the dissociative anesthetic phencyclidine. In light of these structural analogies, and based on the fact that both tramadol and phencyclidine are substances that cause toxic effects in humans, the aim of this study was to investigate the in vitro and in vivo pharmacodynamic profile of these molecules, and to compare them with those caused by tramadol and phencyclidine. In vitro studies demonstrated that tramadol, ortho, meta and para were inactive at mu, kappa and delta opioid receptors. Systemic administration of the three stereoisomers impairs sensorimotor responses, modulates spontaneous motor activity, induces modest analgesia, and alters thermoregulation and cardiorespiratory responses in the mouse in some cases, with a similar profile to that of tramadol and phencyclidine. Naloxone partially prevents only the visual sensorimotor impairments caused by three stereoisomers, without preventing other effects. The present data show that 1-cyclohexyl-x-methoxybenzene derivatives cause pharmaco-toxicological effects by activating both opioid and non-opioid mechanisms and suggest that their use could potentially lead to abuse and bodily harm. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 22147659 1422-0067 1661-6596 |
| Relation: | https://www.mdpi.com/1422-0067/22/14/7659; https://doaj.org/toc/1661-6596; https://doaj.org/toc/1422-0067 |
| DOI: | 10.3390/ijms22147659 |
| URL الوصول: | https://doaj.org/article/9789d31ef7e94df4b761bc3bde2dcd1b |
| رقم الأكسشن: | edsdoj.9789d31ef7e94df4b761bc3bde2dcd1b |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 22147659 14220067 16616596 |
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| DOI: | 10.3390/ijms22147659 |