Pharmacokinetics and oral bioavailability of cannabidiol in horses after intravenous and oral administration with oil and micellar formulations.

Background: Intravenous pharmacokinetics and oral bioavailability of cannabidiol (CBD) with different formulations have not been investigated in horses and may represent a starting point for clinical studies.

Objectives: To describe pharmacokinetics after intravenous and oral administrations with oil and micellar formulations and simulate different treatments.

Study Design: Single intravenous experiment and two-way randomised oral experiments, Latin-square design.

Exogenous application of stress-related signaling molecules affect growth and cannabinoid accumulation in medical cannabis ( L.).

Medical cannabis ( L.) is a source of bioactive phytochemicals with promising pharmacological and therapeutic applications. Enhancing the accumulation of valuable bioactive compounds is potentially a way of increasing the economic importance of this crop.

Effect of temperature in the degradation of cannabinoids: From a brief residence in the gas chromatography inlet port to a longer period in thermal treatments.

The substantial increase in legalization and subsequent regulation of cannabis has intensified the control and analytical monitoring of cannabis products to assure sample quality and control the cannabinoid content of the crop. In this sense, the restriction on cultivating legal cannabis plants has been limited to 0.2-0.

Regulation of Expression of Cannabinoid CB and Serotonin 5HT Receptor Complexes by Cannabinoids in Animal Models of Hypoxia and in Oxygen/Glucose-Deprived Neurons.

Cannabidiol (CBD) is a phytocannabinoid with potential in one of the most prevalent syndromes occurring at birth, the hypoxia of the neonate. CBD targets a variety of proteins, cannabinoid CB and serotonin 5HT receptors included. These two receptors may interact to form heteromers (CB-5HT-Hets) that are also a target of CBD.

A Temporary Immersion System to Improve Micropropagation.

The aim of this study was to propagate axillary shoots of L. using liquid medium in temporary immersion bioreactors. The effect of immersion frequency (3 or 6 immersions per day), explant type (apical or basal sections), explant number (8, 10, and 16 explants), mineral medium (Murashige and Skoog half-strength nitrates, -A and -H, all supplemented with 2-μM metatopoline), sucrose supplementation (2, 0.

Pharmacological data of cannabidiol- and cannabigerol-type phytocannabinoids acting on cannabinoid CB, CB and CB/CB heteromer receptors.

Background: Recent approved medicines whose active principles are ΔTetrahidrocannabinol (Δ-THC) and/or cannabidiol (CBD) open novel perspectives for other phytocannabinoids also present in Cannabis sativa L. varieties. Furthermore, solid data on the potential benefits of acidic and varinic phytocannabinoids in a variety of diseases are already available.

Pharmacological potential of varinic-, minor-, and acidic phytocannabinoids.

While natural Δ-tetrahidrocannabinol (ΔTHC), cannabidiol (CBD), and their therapeutic potential have been extensively researched, some cannabinoids have been less extensively investigated. The present article compiles data from the literature that highlight the health benefits and therapeutic potential of lesser known phytocannabinoids, which we have divided into varinic, acidic, and "minor" (i.e.

Untargeted characterization of extracts from Cannabis sativa L. cultivars by gas and liquid chromatography coupled to mass spectrometry in high resolution mode.

Elucidation of Cannabis composition is required to evaluate the potential of this plant for pharmacological uses, but also for implementation in breeding programs with agronomical purposes. The aim of the present study was to develop a method for untargeted analysis of polar and non-polar Cannabis extracts. For this purpose, extracts from 17 cultivars of Cannabis sativa L.

Potentiation of cannabinoid signaling in microglia by adenosine A receptor antagonists.

Neuroprotective M2-skewed microglia appear as promising to alter the course of neurodegenerative diseases and G protein-coupled receptors (GPCRs) are potential targets to achieve such microglial polarization. A common feature of adenosine A (A R) and cannabinoid CB (CB R) GPCRs in microglia is that their expression is upregulated in Alzheimer's disease (AD). On the one hand, CB R seems a target for neuroprotection, delaying neurodegenerative processes like those associated to AD or Parkinson's diseases.

Cannabidiol skews biased agonism at cannabinoid CB and CB receptors with smaller effect in CB-CB heteroreceptor complexes.

Currently, biased agonism is at the center stage of drug development approaches. We analyzed effects of a battery of cannabinoids plus/minus cannabidiol (CBD) in four functional parameters (cAMP levels, phosphorylation of extracellular signal-regulated kinases (ERK1/2), β-arrestin recruitment and label-free/DMR) in HEK-293T cells expressing cannabinoid receptors, CB or CB, or CB-CB heteroreceptor complexes. In all cases two natural agonists plus two selective synthetic agonists were used.

The potential of near infrared spectroscopy to estimate the content of cannabinoids in Cannabis sativa L.: A comparative study.

Unlabelled: Cannabis has been one of the oldest source of food, textile fiber and psychotropic substances. Cannabinoids are the main biologically active constituents of the Cannabis genus, with a demonstrated medicinal value. Its production is becoming legalized and regulated in many countries, thus increasing the need for a rapid analysis method to assess the content of cannabinoids.

Cannabigerol Action at Cannabinoid CB and CB Receptors and at CB-CB Heteroreceptor Complexes.

Cannabigerol (CBG) is one of the major phytocannabinoids present in L. that is attracting pharmacological interest because it is non-psychotropic and is abundant in some industrial hemp varieties. The aim of this work was to investigate in parallel the binding properties of CBG to cannabinoid CB (CBR) and CB (CBR) receptors and the effects of the compound on agonist activation of those receptors and of CB-CB heteroreceptor complexes.

Binding and Signaling Studies Disclose a Potential Allosteric Site for Cannabidiol in Cannabinoid CB Receptors.

The mechanism of action of cannabidiol (CBD), the main non-psychotropic component of L., is not completely understood. First assumed that the compound was acting via cannabinoid CB receptors (CBRs) it is now suggested that it interacts with non-cannabinoid G-protein-coupled receptors (GPCRs); however, CBD does not bind with high affinity to the orthosteric site of any GPCR.

Tetrahydrocannabinolic acid is a potent PPARγ agonist with neuroprotective activity.

Background And Purpose: Phytocannabinoids are produced in Cannabis sativa L. in acidic form and are decarboxylated upon heating, processing and storage. While the biological effects of decarboxylated cannabinoids such as Δ -tetrahydrocannabinol have been extensively investigated, the bioactivity of Δ -tetahydrocannabinol acid (Δ -THCA) is largely unknown, despite its occurrence in different Cannabis preparations.

Quantitative analytical method to evaluate the metabolism of vitamin D.

A method for quantitative analysis of vitamin D (both D2 and D3) and its main metabolites - monohydroxylated vitamin D (25-hydroxyvitamin D2 and 25-hydroxyvitamin D3) and dihydroxylated metabolites (1,25-dihydroxyvitamin D2, 1,25-dihydroxyvitamin D3 and 24,25-dihydroxyvitamin D3) in human serum is here reported. The method is based on direct analysis of serum by an automated platform involving on-line coupling of a solid-phase extraction workstation to a liquid chromatograph-tandem mass spectrometer. Detection of the seven analytes was carried out by the selected reaction monitoring (SRM) mode, and quantitative analysis was supported on the use of stable isotopic labeled internal standards (SIL-ISs).

Stable isotopic internal standard correction for quantitative analysis of hydroxyeicosatetraenoic acids (HETEs) in serum by on-line SPE-LC-MS/MS in selected reaction monitoring mode.

The influence of the inclusion of a stable isotopic labeled internal standard (SIL-IS) on the quantitative analysis of hydroxyeicosatetranoic acids (HETEs) in human serum is evaluated in this research. A solid-phase extraction-liquid chromatography-tandem mass spectrometry (SPE-LC-MS/MS) platform, one of the preferred approaches for targeted analysis of biofluids through the selected reaction monitoring (SRM) operational mode, was used to determine HETEs. These compounds were chosen as targeted metabolites because of their involvement in cardiovascular disease, cancer and osteoporosis.

Effects of arachidonic acid on the concentration of hydroxyeicosatetraenoic acids in culture media of mesenchymal stromal cells differentiating into adipocytes or osteoblasts.

Metabolites derived from the polyunsaturated fatty acids (PUFA) may modulate the mesenchymal stromal cell (MSC) differentiation. Such cells can differentiate into different cellular types, including adipocytes and osteoblasts. Aging favors the bone marrow MSC differentiation toward the former, causing a loss of bone density associated with pathologies like osteoporosis.

Anthocyanidins, proanthocyanidins, and anthocyanins profiling in wine lees by solid-phase extraction-liquid chromatography coupled to electrospray ionization tandem mass spectrometry with data-dependent methods.

A method has been developed to study the content of anthocyanidins, proanthocyanidicins, and anthocyanins in wine lees, an abundant byproduct from wineries. Detection/quantitation of the target compounds was carried out by a hyphenated system consisting of a solid-phase extraction workstation (Prospekt-2 unit) online coupled to a liquid chromatograph-triple-quadrupole tandem mass spectrometer (LC-MS/MS), where standards were used for identification/quantitation of both anthocyanidins and proanthocyanidins. Owing to the lack of anthocyanins standards, advantages from the use of data-dependent methods were taken for their identification and confirmatory analysis.

Global metabolomic profiling of human serum from obese individuals by liquid chromatography-time-of-flight/mass spectrometry to evaluate the intake of breakfasts prepared with heated edible oils.

The metabolic profile of human serum after intake of breakfasts prepared with different heated vegetable oils has been studied. Four oils (olive and sunflower oils, pure and enriched with natural and artificial oxidation inhibitors) were subjected to a simulated heated process prior to breakfast preparation. A metabolomics global profiling approach performed on post-basal serum samples revealed statistical differences among individuals based on breakfast intake, and identified compounds responsible for such differences.

Integrated identification/confirmatory and targeted analysis of epoxyeicosatrienosic acids in human serum by LC-TOF MS and automated on-line SPE-LC-QqQ MS/MS.

A combined strategy is here proposed for qualitative/quantitative targeted analysis of epoxyeicosatrienoic acids (EETs) in human serum. Identification of EET regioisomers was initially carried out by LC-TOF MS in high accuracy mode under optimum conditions for chromatographic separation of the four isomers with an isocratic method using 40:40:20 (v/v/v) methanol-acetonitrile-water containing 0.02% acetic acid.

An approach for quantitative analysis of vitamins D and B9 and their metabolites in human biofluids by on-line orthogonal sample preparation and sequential mass spectrometry detection.

An approach for quantitative analysis of two vitamins with different polarities (vitamins D and B9) and their metabolites is presented here. The approach is based on an experimental setup based on hyphenation of an automated workstation for preparation of liquid samples and an LC-MS/MS system with a triple quadrupole mass spectrometer. This configuration enabled development of an orthogonal protocol for sequential SPE retention of analytes with different polarities for subsequent elution and chromatographic separation prior to detection.