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https://www.readbyqxmd.com/read/27899456/free-and-glucuronide-whole-blood-cannabinoids-pharmacokinetics-after-controlled-smoked-vaporized-and-oral-cannabis-administration-in-frequent-and-occasional-cannabis-users-identification-of-recent-cannabis-intake
#1
Matthew N Newmeyer, Madeleine J Swortwood, Allan J Barnes, Osama A Abulseoud, Karl B Scheidweiler, Marilyn A Huestis
BACKGROUND: There is increasing interest in markers of recent cannabis use because following frequent cannabis intake, Δ(9)-tetrahydrocannabinol (THC) may be detected in blood for up to 30 days. The minor cannabinoids cannabidiol, cannabinol (CBN), and THC-glucuronide were previously detected for ≤2.1 h in frequent and occasional smokers' blood after cannabis smoking. Cannabigerol (CBG), Δ(9)-tetrahydrocannabivarin (THCV), and 11-nor-9-carboxy-THCV might also be recent use markers, but their blood pharmacokinetics have not been investigated...
December 2016: Clinical Chemistry
https://www.readbyqxmd.com/read/27647820/cannabinoid-disposition-in-oral-fluid-after-controlled-smoked-vaporized-and-oral-cannabis-administration
#2
Madeleine J Swortwood, Matthew N Newmeyer, Maria Andersson, Osama A Abulseoud, Karl B Scheidweiler, Marilyn A Huestis
Oral fluid (OF) is an important matrix for monitoring drugs. Smoking cannabis is common, but vaporization and edible consumption also are popular. OF pharmacokinetics are available for controlled smoked cannabis, but few data exist for vaporized and oral routes. Frequent and occasional cannabis smokers were recruited as participants for four dosing sessions including one active (6.9% Δ(9) -tetrahydrocannabinol, THC) or placebo cannabis-containing brownie, followed by one active or placebo cigarette, or one active or placebo vaporized cannabis dose...
September 19, 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27573936/efficacy-and-safety-of-cannabidiol-and-tetrahydrocannabivarin-on-glycemic-and-lipid-parameters-in-patients-with-type-2-diabetes-a-randomized-double-blind-placebo-controlled-parallel-group-pilot-study
#3
Khalid A Jadoon, Stuart H Ratcliffe, David A Barrett, E Louise Thomas, Colin Stott, Jimmy D Bell, Saoirse E O'Sullivan, Garry D Tan
OBJECTIVE: Cannabidiol (CBD) and Δ(9)-tetrahydrocannabivarin (THCV) are nonpsychoactive phytocannabinoids affecting lipid and glucose metabolism in animal models. This study set out to examine the effects of these compounds in patients with type 2 diabetes. RESEARCH DESIGN AND METHODS: In this randomized, double-blind, placebo-controlled study, 62 subjects with noninsulin-treated type 2 diabetes were randomized to five treatment arms: CBD (100 mg twice daily), THCV (5 mg twice daily), 1:1 ratio of CBD and THCV (5 mg/5 mg, twice daily), 20:1 ratio of CBD and THCV (100 mg/5 mg, twice daily), or matched placebo for 13 weeks...
October 2016: Diabetes Care
https://www.readbyqxmd.com/read/27539096/long-term-stability-of-cannabinoids-in-oral-fluid-after-controlled-cannabis-administration
#4
Karl B Scheidweiler, Maria Andersson, Madeleine J Swortwood, Cristina Sempio, Marilyn A Huestis
Cannabinoid stability in oral fluid (OF) is important for assuring accurate results since OF has become a valid alternative matrix of choice for drug testing. We previously published OF cannabinoid stability studies using Quantisal™, Oral-Eze®, and StatSure™ devices stored at room temperature for 1 week, 4 °C for up to 4 weeks and in -20 °C up to 24 weeks. Extending refrigerated stability up to 3 months would be helpful for clinical and forensic testing, for reanalysis of OF samples and for batching research analyses...
August 18, 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27498155/pure-%C3%AE-9-tetrahydrocannabivarin-and-a-cannabis-sativa-extract-with-high-content-in-%C3%AE-9-tetrahydrocannabivarin-inhibit-nitrite-production-in-murine-peritoneal-macrophages
#5
Barbara Romano, Ester Pagano, Pierangelo Orlando, Raffaele Capasso, Maria Grazia Cascio, Roger Pertwee, Vincenzo Di Marzo, Angelo A Izzo, Francesca Borrelli
Historical and scientific evidence suggests that Cannabis use has immunomodulatory and anti-inflammatory effects. We have here investigated the effect of the non-psychotropic phytocannabinoid Δ(9)-tetrahydrocannabivarin (THCV) and of a Cannabis sativa extract with high (64.8%) content in THCV (THCV-BDS) on nitric oxide (NO) production, and on cannabinoid and transient receptor potential (TRP) channel expression in lipopolysaccharide (LPS)-stimulated murine peritoneal macrophages. THCV-BDS and THCV exhibited similar affinity in radioligand binding assays for CB1 and CB2 receptors, and inhibited, via CB2 but not CB1 cannabinoid receptors, nitrite production evoked by LPS in peritoneal macrophages...
August 3, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27422645/simultaneous-quantification-of-11-cannabinoids-and-metabolites-in-human-urine-by-liquid-chromatography-tandem-mass-spectrometry-using-wax-s-tips
#6
Maria Andersson, Karl B Scheidweiler, Cristina Sempio, Allan J Barnes, Marilyn A Huestis
A comprehensive cannabinoid urine quantification method may improve clinical and forensic result interpretation and is necessary to support our clinical research. A liquid chromatography tandem mass spectrometry quantification method for ∆(9)-tetrahydrocannabinol (THC), 11-hydroxy-THC (11-OH-THC), 11-nor-9-carboxy-THC (THCCOOH), ∆(9)-tetrahydrocannabinolic acid (THCAA), cannabinol (CBN), cannabidiol (CBD), cannabigerol (CBG), ∆(9)-tetrahydrocannabivarin (THCV), 11-nor-9-carboxy-THCV (THCVCOOH), THC-glucuronide (THC-gluc), and THCCOOH-glucuronide (THCCOOH-gluc) in urine was developed and validated according to the Scientific Working Group on Toxicology guidelines...
September 2016: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/27341312/simultaneous-quantification-of-major-cannabinoids-and-metabolites-in-human-urine-and-plasma-by-hplc-ms-ms-and-enzyme-alkaline-hydrolysis
#7
Oier Aizpurua-Olaizola, Iratxe Zarandona, Laura Ortiz, Patricia Navarro, Nestor Etxebarria, Aresatz Usobiaga
A high performance liquid chromatography coupled to tandem mass spectrometry (HPLC-MS/MS) method for simultaneous quantification of Δ9-tetrahydrocannabinol (THC), its two metabolites 11-hydroxy-Δ9-tetrahydrocannabinol (11-OH-THC) and 11-nor-9-carboxy-Δ9-tetrahydrocannabinol (THC-COOH), and four additional cannabinoids (cannabidiol (CBD), cannabigerol (CBG), tetrahydrocannabivarin (THCV), and cannabinol (CBN)) in 1 mL of human urine and plasma was developed and validated. The hydrolysis process was studied to ensure complete hydrolysis of glucuronide conjugates and the extraction of a total amount of analytes...
June 24, 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27236483/quantification-of-cannabinoids-and-their-free-and-glucuronide-metabolites-in-whole-blood-by-disposable-pipette-extraction-and-liquid-chromatography-tandem-mass-spectrometry
#8
Karl B Scheidweiler, Matthew N Newmeyer, Allan J Barnes, Marilyn A Huestis
Identifying recent cannabis intake is confounded by prolonged cannabinoid excretion in chronic frequent cannabis users. We previously observed detection times ≤2.1h for cannabidiol (CBD) and cannabinol (CBN) and Δ(9)-tetrahydrocannabinol (THC)-glucuronide in whole blood after smoking, suggesting their applicability for identifying recent intake. However, whole blood collection may not occur for up to 4h during driving under the influence of drugs investigations, making a recent-use marker with a 6-8h detection window helpful for improving whole blood cannabinoid interpretation...
July 1, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/27094344/differential-effectiveness-of-selected-non-psychotropic-phytocannabinoids-on-human-sebocyte-functions-implicates-their-introduction-in-dry-seborrhoeic-skin-and-acne-treatment
#9
Attila Oláh, Arnold Markovics, Judit Szabó-Papp, Pálma Tímea Szabó, Colin Stott, Christos C Zouboulis, Tamás Bíró
Acne is a common skin disease characterized by elevated sebum production and inflammation of the sebaceous glands. We have previously shown that a non-psychotropic phytocannabinoid ((-)-cannabidiol [CBD]) exerted complex anti-acne effects by normalizing 'pro-acne agents'-induced excessive sebaceous lipid production, reducing proliferation and alleviating inflammation in human SZ95 sebocytes. Therefore, in this study we aimed to explore the putative anti-acne effects of further non-psychotropic phytocannabinoids ((-)-cannabichromene [CBC], (-)-cannabidivarin [CBDV], (-)-cannabigerol [CBG], (-)-cannabigerovarin [CBGV] and (-)-Δ(9) -tetrahydrocannabivarin [THCV])...
September 2016: Experimental Dermatology
https://www.readbyqxmd.com/read/26651563/determination-of-11-cannabinoids-in-biomass-and-extracts-of-different-varieties-of-cannabis-using-high-performance-liquid-chromatography
#10
Waseem Gul, Shahbaz W Gul, Mohamed M Radwan, Amira S Wanas, Zlatko Mehmedic, Ikhlas I Khan, Maged H M Sharaf, Mahmoud A ElSohly
An HPLC single-laboratory validation was performed for the detection and quantification of the 11 major cannabinoids in most cannabis varieties, namely, cannabidiolic acid (CBDA), cannabigerolic acid (CBGA), cannabigerol (CBG), cannabidiol (CBD), tetrahydrocannabivarin (THCV), cannabinol (CBN), Δ9-trans-tetrahydrocannabinol (Δ9-THC), Δ8-trans-tetrahydrocannabinol (Δ8-THC), cannabicyclol (CBL), cannabichromene (CBC), and Δ9-tetrahydrocannabinolic acid-A (THCAA). The analysis was carried out on the biomass and extracts of these varieties...
November 2015: Journal of AOAC International
https://www.readbyqxmd.com/read/26577065/the-effect-of-five-day-dosing-with-thcv-on-thc-induced-cognitive-psychological-and-physiological-effects-in-healthy-male-human-volunteers-a-placebo-controlled-double-blind-crossover-pilot-trial
#11
RANDOMIZED CONTROLLED TRIAL
Amir Englund, Zerrin Atakan, Aleksandra Kralj, Nigel Tunstall, Robin Murray, Paul Morrison
RATIONALE: Cannabis is mostly grown under illegal and unregulated circumstances, which seems to favour a product increasingly high in its main cannabinoid ∆-9-tetrahydrocannabinol (THC). ∆-9-tetrahydrocannabivarin (THCV) is a relatively untested cannabinoid which is said to be a cannabinoid receptor neutral antagonist, and may inhibit the effects of THC. OBJECTIVES: To explore the safety and tolerability of repeated THCV administration and its effects on symptoms normally induced by THC in a sample of healthy volunteers...
February 2016: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/26362774/the-cb1-neutral-antagonist-tetrahydrocannabivarin-reduces-default-mode-network-and-increases-executive-control-network-resting-state-functional-connectivity-in-healthy-volunteers
#12
Ewelina Rzepa, Luke Tudge, Ciara McCabe
BACKGROUND: The cannabinoid cannabinoid type 1 (CB1) neutral antagonist tetrahydrocannabivarin (THCv) has been suggested as a possible treatment for obesity, but without the depressogenic side-effects of inverse antagonists such as Rimonabant. However, how THCv might affect the resting state functional connectivity of the human brain is as yet unknown. METHOD: We examined the effects of a single 10mg oral dose of THCv and placebo in 20 healthy volunteers in a randomized, within-subject, double-blind design...
September 10, 2015: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/26197538/effect-of-non-psychotropic-plant-derived-cannabinoids-on-bladder-contractility-focus-on-cannabigerol
#13
Ester Pagano, Vittorino Montanaro, Antonio Di Girolamo, Antonio Pistone, Vincenzo Altieri, Jordan K Zjawiony, Angelo A Izzo, Raffaele Capasso
There are anecdotal reports that some Cannabis preparations may be useful for bladder dysfunctions. Here, we investigated the effect of a number of non- psychotropic phytocannabinoids, namely cannabidiol (CBD), cannabigerol (CBG), cannabidivarin (CBDV), Δ9-tetrahydrocannabivarin (THCV) and cannabichromene (CBC) on mouse bladder contractility in vitro. CBG, THCV, CBD and CBDV, but not CBC, at concentration ranging from 10(-8) M to 10(-4) M, decreased (with similar potency), the contractions induced by acetylcholine without significantly modifying the contractions induced by electrical stimulation...
June 2015: Natural Product Communications
https://www.readbyqxmd.com/read/25595882/two-non-psychoactive-cannabinoids-reduce-intracellular-lipid-levels-and-inhibit-hepatosteatosis
#14
Cristoforo Silvestri, Debora Paris, Andrea Martella, Dominique Melck, Irene Guadagnino, Mike Cawthorne, Andrea Motta, Vincenzo Di Marzo
BACKGROUND & AIMS: Obesity and associated metabolic syndrome have quickly become a pandemic and a major detriment to global human health. The presence of non-alcoholic fatty liver disease (NAFLD; hepatosteatosis) in obesity has been linked to the worsening of the metabolic syndrome, including the development of insulin resistance and cardiovascular disease. Currently, there are few options to treat NAFLD, including life style changes and insulin sensitizers. Recent evidence suggests that the cannabinoids Δ(9)-tetrahydrocannabivarin (THCV) and cannabidiol (CBD) improve insulin sensitivity; we aimed at studying their effects on lipid levels...
June 2015: Journal of Hepatology
https://www.readbyqxmd.com/read/25542687/neural-effects-of-cannabinoid-cb1-neutral-antagonist-tetrahydrocannabivarin-on-food-reward-and-aversion-in-healthy-volunteers
#15
RANDOMIZED CONTROLLED TRIAL
Luke Tudge, Clare Williams, Philip J Cowen, Ciara McCabe
BACKGROUND: Disturbances in the regulation of reward and aversion in the brain may underlie disorders such as obesity and eating disorders. We previously showed that the cannabis receptor subtype (CB1) inverse agonist rimonabant, an antiobesity drug withdrawn due to depressogenic side effects, diminished neural reward responses yet increased aversive responses (Horder et al., 2010). Unlike rimonabant, tetrahydrocannabivarin is a neutral CB1 receptor antagonist (Pertwee, 2005) and may therefore produce different modulations of the neural reward system...
December 25, 2014: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/25428610/quantification-of-six-cannabinoids-and-metabolites-in-oral-fluid-by-liquid-chromatography-tandem-mass-spectrometry
#16
Nathalie A Desrosiers, Karl B Scheidweiler, Marilyn A Huestis
Δ(9) -Tetrahydrocannabinol (THC) is the most commonly analyzed cannabinoid in oral fluid (OF); however, its metabolite 11-nor-9-carboxy-THC (THCCOOH) offers the advantage of documenting active consumption, as it is not detected in cannabis smoke. Analytical challenges such as low (ng/L) THCCOOH OF concentrations hampered routine OF THCCOOH monitoring. Presence of minor cannabinoids like cannabidiol and cannabinol offer the advantage of identifying recent cannabis intake. Published OF cannabinoids methods have limitations, including few analytes and lengthy derivatization...
August 2015: Drug Testing and Analysis
https://www.readbyqxmd.com/read/25363799/the-phytocannabinoid-%C3%AE-%C3%A2-tetrahydrocannabivarin-can-act-through-5-ht%C3%A2-a-receptors-to-produce-antipsychotic-effects
#17
Maria Grazia Cascio, Erica Zamberletti, Pietro Marini, Daniela Parolaro, Roger G Pertwee
BACKGROUND AND PURPOSE: This study aimed to address the questions of whether Δ(9)-tetrahydrocannabivarin (THCV) can (i) enhance activation of 5-HT1 A receptors in vitro and (ii) induce any apparent 5-HT₁A receptor-mediated antipsychotic effects in vivo. EXPERIMENTAL APPROACH: In vitro studies investigated the effect of THCV on targeting by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) of 5-HT₁A receptors in membranes obtained from rat brainstem or human 5-HT₁A CHO cells, using [(35)S]-GTPγS and 8-[(3)H]-OH-DPAT binding assays...
March 2015: British Journal of Pharmacology
https://www.readbyqxmd.com/read/25338935/identification-and-quantification-of-cannabinoids-in-cannabis-sativa-l-plants-by-high-performance-liquid-chromatography-mass-spectrometry
#18
Oier Aizpurua-Olaizola, Jone Omar, Patricia Navarro, Maitane Olivares, Nestor Etxebarria, Aresatz Usobiaga
High performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) has been successfully applied to cannabis plant extracts in order to identify cannabinoid compounds after their quantitative isolation by means of supercritical fluid extraction (SFE). MS conditions were optimized by means of a central composite design (CCD) approach, and the analysis method was fully validated. Six major cannabinoids [tetrahydrocannabinolic acid (THCA), tetrahydrocannabinol (THC), cannabidiol (CBD), tetrahydrocannabivarin (THCV), cannabigerol (CBG), and cannabinol (CBN)] were quantified (RSD < 10%), and seven more cannabinoids were identified and verified by means of a liquid chromatograph coupled to a quadrupole-time-of-flight (Q-ToF) detector...
November 2014: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/25257544/are-cannabidiol-and-%C3%AE-9-tetrahydrocannabivarin-negative-modulators-of-the-endocannabinoid-system-a-systematic-review
#19
REVIEW
John M McPartland, Marnie Duncan, Vincenzo Di Marzo, Roger G Pertwee
Based upon evidence that the therapeutic properties of Cannabis preparations are not solely dependent upon the presence of Δ(9) -tetrahydrocannabinol (THC), pharmacological studies have been recently carried out with other plant cannabinoids (phytocannabinoids), particularly cannabidiol (CBD) and Δ(9) -tetrahydrocannabivarin (THCV). Results from some of these studies have fostered the view that CBD and THCV modulate the effects of THC via direct blockade of cannabinoid CB1 receptors, thus behaving like first-generation CB1 receptor inverse agonists, such as rimonabant...
February 2015: British Journal of Pharmacology
https://www.readbyqxmd.com/read/23902479/evaluation-of-the-potential-of-the-phytocannabinoids-cannabidivarin-cbdv-and-%C3%AE-9-tetrahydrocannabivarin-thcv-to-produce-cb1-receptor-inverse-agonism-symptoms-of-nausea-in-rats
#20
COMPARATIVE STUDY
Erin M Rock, Martin A Sticht, Marnie Duncan, Colin Stott, Linda A Parker
BACKGROUND AND PURPOSE: The cannabinoid 1 (CB1 ) receptor inverse agonists/antagonists, rimonabant (SR141716, SR) and AM251, produce nausea and potentiate toxin-induced nausea by inverse agonism (rather than antagonism) of the CB1 receptor. Here, we evaluated two phytocannabinoids, cannabidivarin (CBDV) and Δ(9) -tetrahydrocannabivarin (THCV), for their ability to produce these behavioural effect characteristics of CB1 receptor inverse agonism in rats. EXPERIMENTAL APPROACH: In experiment 1, we investigated the potential of THCV and CBDV to produce conditioned gaping (measure of nausea-induced behaviour) in the same manner as SR and AM251...
October 2013: British Journal of Pharmacology
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