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Cytochrome P450 enzymes involved in the metabolism of tetrahydrocannabinols and cannabinol by human hepatic microsomes.
Results indicate that CYP2C9 and CYP3A4 are major enzymes involved in the 11-hydroxylation and the 8-(or the 7-) hydroxylations, respectively, of the cannabinoids by human hepatic microsomes.
Cannabidiol, a Major Phytocannabinoid, As a Potent Atypical Inhibitor for CYP2D6
The results indicated that CBD caused potent direct CYP2D6 inhibition, in which two phenolic hydroxyl groups and the pentyl side chain of CBD may play important roles.
Uridine receptor: discovery and its involvement in sleep mechanism.
It is suggested that uridine is released from steps of nucleic acid-nucleic protein biosynthesis (catabolism), and reaches the binding sites in the areas of the brain which regulate natural sleep as one of the triggering steps in inducing hypnotic activity.
Δ-Tetrahydrocannabinol induces cytotoxicity in macrophage J774-1 cells: involvement of cannabinoid receptor 2 and p38 MAPK.
Results suggest that the cytotoxicity of Δ⁸-THC to J774-1 cells is exerted mediated through the CB₂ receptor followed by the activation of p38 MAPK, which is associated with vacuole formation, cell swelling, chromatin condensation, and nuclear fragmentation.
Is the cannabinoid CB1 receptor a 2-arachidonoylglycerol receptor? Structural requirements for triggering a Ca2+ transient in NG108-15 cells.
The results suggest that the structure of 2-arachidonoylglycerol is strictly recognized by theCB1 receptor, which raises the possibility that the CB1 receptor is originally a 2-Arachidonoyslglycersol receptor.
Potent inhibition of human cytochrome P450 3A isoforms by cannabidiol: role of phenolic hydroxyl groups in the resorcinol moiety.
CBD most potently inhibited catalytic activity of human CYP3A enzymes, especially CYP1A4 and CYP2A5, and these results suggest that two phenolic hydroxyl groups in the resorcinol moiety of CBD may play an important role in the CYP 3A inhibition.
Identification of cytochrome P450 enzymes responsible for metabolism of cannabidiol by human liver microsomes.
In vitro metabolism of CBD with human liver microsomes indicated that CBD was extensively metabolized by HLMs, and suggested that CYP3A4 and CYP2C19 may be major isoforms responsible for 6α-, 6β-, 7-, and/or 4″-hydroxylations of CBD in HLMs.
Characterization of major phytocannabinoids, cannabidiol and cannabinol, as isoform-selective and potent inhibitors of human CYP1 enzymes.
Results indicated that CBD and CBN showed CYP1 isoform-selective direct inhibition and that CBD was characterized as a potent mechanism-based inhibitor of human CyP1 enzymes, especially CYP 1A1.
Cannabidiolic Acid as a Selective Cyclooxygenase-2 Inhibitory Component in Cannabis
The lines of evidence in this study suggest that naturally occurring CBDA in cannabis is a selective inhibitor for COX-2.
Conversion of cannabidiol to Δ9-tetrahydrocannabinol and related cannabinoids in artificial gastric juice, and their pharmacological effects in mice
Cannabidiol (CBD), a nonpsychoactive cannabinoid, was found to be converted to 9α-hydroxyhexahydrocannabinol (9α-OH-HHC) and 8-hydroxy-iso-hexahydrocannabinol (8-OH-iso-HHC) together with