Search results for " Cannabinoid"
showing 10 items of 163 documents
Behavioural and pharmacological characterization of a novel cannabinomimetic adamantane-derived indole, APICA, and considerations on the possible mis…
2015
The novel adamantane derivative APICA (N-(adamantan-1-yl)-1-pentyl-1H-indole-3-carboxamide) was recently identified as a cannabinomimetic indole of abuse. Despite its novel structure, APICA recalls cannabinomimetic indoles, such as representative member JWH-018.In present study, the effects of APICA (1-3 mg/kg, i.p.) were tested in C57BL/6J mice, in the Tetrad task which includes the assessment of: body temperature; locomotor activity and behavioural reactivity; nociception; motor coordination; declarative memory. Furthermore, pre-treatment with the CB1 antagonist AM251 (3 mg/kg, i.p.) or the CB2 antagonist AM630 (3 mg/kg, i.p.) was carried out to characterize APICA activity.Our results sho…
Sensitive screening of synthetic cannabinoids using liquid chromatography quadrupole time-of-flight mass spectrometry after solid phase extraction.
2021
Analysis of synthetic cannabinoids still poses a challenge for many institutions due to the number of available substances and the constantly changing drug market. Both new and well-known substances keep appearing and disappearing on the market, making it hard to adapt analytical methods in a timely manner. In this study, we developed a qualitative screening approach for synthetic cannabinoids and their metabolites by means of liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOF-MS). Samples were measured in data-dependent auto-MS/MS mode and identified by fragment spectra, retention time and accurate mass. Two established solid phase extractions were compared using fo…
Endocannabinoid signals in the control of emotion.
2008
The appropriate control of emotional responses evoked by environmental stimuli is an important innate mechanism for ensuring quality of life and even for survival. Inappropriate responses and decreased abilities to adjust to changed environmental situations can lead to psychiatric disorders, such as posttraumatic stress disorders, phobia and depression. Endocannabinoid signalling has emerged as one of the regulatory systems of the brain supporting appropriate emotional responses. As various components of the endocannabinoid system have become therapeutic targets, understanding the endocannabinoids’ mechanism of action is an important research topic for a rationalized drug design and optimal…
Presynaptic CB1 Receptors Regulate Synaptic Plasticity at Cerebellar Parallel Fiber Synapses
2011
Endocannabinoids are potent regulators of synaptic strength. They are generally thought to modify neurotransmitter release through retrograde activation of presynaptic type 1 cannabinoid receptors (CB1Rs). In the cerebellar cortex, CB1Rs regulate several forms of synaptic plasticity at synapses onto Purkinje cells, including presynaptically expressed short-term plasticity and, somewhat paradoxically, a postsynaptic form of long-term depression (LTD). Here we have generated mice in which CB1Rs were selectively eliminated from cerebellar granule cells, whose axons form parallel fibers. We find that in these mice, endocannabinoid-dependent short-term plasticity is eliminated at parallel fiber…
Central side-effects of therapies based on CB1 cannabinoid receptor agonists and antagonists: focus on anxiety and depression
2009
Both agonists (e.g. Delta(9)-tetrahydrocannabinol, nabilone) and antagonists (e.g. rimonabant, taranabant) of the cannabinoid type-1 (CB(1)) receptor have been explored as therapeutic agents in diverse fields of medicine such as pain management and obesity with associated metabolic dysregulation, respectively. CB(1) receptors are widely distributed in the central nervous system and are involved in the modulation of emotion, stress and habituation responses, behaviours that are thought to be dysregulated in human psychiatric disorders. Accordingly, CB(1) receptor activation may, in some cases, precipitate episodes of psychosis and panic, while its inhibition may lead to behaviours reminiscen…
Ion mobility spectrometry and high resolution mass-spectrometry as methodologies for rapid identification of the last generation of new psychoactive …
2018
A new drug trafficking trend has been observed in the last years by the introduction in the black market of new psychoactive substances (NPS) in order to difficult competent authority controls. In this study, ion mobility spectrometry (IMS) and high-resolution mass-spectrometry (HRMS) were proposed as vanguard and rearguard methodologies for the rapid identification of the last generation of NPS in seizures. The combined use of IMS and HRMS has been evaluated through the analysis of 24 NPS seized from 2016 to 2018 in Valencia (Spain) to demonstrate the utility of this approach. The characteristic reduced mobility (K0) values for seized NPS were determined and mass-mobility relationships wer…
Evidences of cannabinoids-induced modulation of paroxysmal events in an experimental model of partial epilepsy in the rat
2010
Different studies have been shown a clear anticonvulsant activity exerted by cannabinoids (CB) through the CB1 receptor activation. The purpose of this study was to evaluate, in an in vivo experimental model of temporal lobe epilepsy (maximal dentate gyrus activation - MDA) in the rat, the protective effect of (R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo[1,2,3-de]-1,4-benzoxazin-6-Yl]-1-naphthalenylmethanone (WIN 55,212-2, CB agonist) alone or in combination with N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (AM251, selective CB1 antagonist). Pre-treatment with AM251 (1 mg kg-1, 30 min interval) dramatically reduced the signif…
Sintētisko kanabinoīdu un katinonu identifikācijas iespējas
2016
Vēl aizvien nelegālajā apritē parādās jaunas psihoaktīvās vielas, kuru identificēšanas iespējas ir apgrūtinātas un maz pētītas. Jaunās psihoaktīvās vielas ir potenciāls sabiedrības veselības drauds. Populārākās ir sintētiskie kanabinoīdi un sintētiskie katinoni. To iedarbība uz cilvēka organismu ir maz pētīta un neparedzama. Lai pētītu to iedarbību uz cilvēka organismu, ir nepieciešamas efektīvas un visaptverošas pētniecības metodes. Darba ir apkopoti dati par Latvijā biežāk sastopamajām jaunajām psihoaktīvajām vielām, kā arī apkopoti un analizēti dati par šo vielu noteikšanas metodēm, kā pielietojamāko metodi nosakot jauno psihoaktīvo vielu noteikšanu, var uzskatīt GH-MS/MS metodi. Atslēgv…
Determination of Third-Generation Synthetic Cannabinoids in Oral Fluids.
2020
Abstract A procedure has been developed for the determination of third-generation synthetic cannabinoids in oral fluid samples by using a semi-automated microextraction by packed sorbent (MEPS) procedure and gas chromatography–mass spectrometry (GC–MS) determination. Five synthetic cannabinoids were employed as model compounds 5F-ADB, MMB-CHMICA, THJ-2201, CUMYL-4CN-BINACA and MDMB-CHMCZCA. The most adequate operative conditions for MEPS were evaluated giving quantitative recoveries, from 89 to 124%, in synthetic and field saliva samples spiked with 125 and 250 μg/L of the studied cannabinoids, with the exception of MDMB-CHMCZCA in field saliva samples that provided slightly lower recoverie…