lysine/cannabis

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Role of a conserved lysine residue in the peripheral cannabinoid receptor (CB2): evidence for subtype specificity.

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The human cannabinoid receptors, central cannabinoid receptor (CB1) and peripheral cannabinoid receptor (CB2), share only 44% amino acid identity overall, yet most ligands do not discriminate between receptor subtypes. Site-directed mutagenesis was employed as a means of mapping the ligand

A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN55212-2.

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Lys192 in the third transmembrane domain of the human CB1 cannabinoid receptor was converted to an alanine to study its role in receptor recognition and activation by agonists. HU-210, CP-55940, WIN55212-2, and anandamide, four cannabinoid agonists with distinct chemical structures, were used to

Cannabidiol, a Major Non-Psychotropic Cannabis Constituent Enhances Fracture Healing and Stimulates Lysyl Hydroxylase Activity in Osteoblasts.

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Cannabinoid ligands regulate bone mass, but skeletal effects of cannabis (marijuana and hashish) have not been reported. Bone fractures are highly prevalent, involving prolonged immobilization and discomfort. Here we report that the major non-psychoactive cannabis constituent, cannabidiol (CBD),

Histone methyltransferase G9a diminishes expression of cannabinoid CB1 receptors in primary sensory neurons in neuropathic pain.

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Type-1 cannabinoid receptors (CB1Rs) are expressed in the dorsal root ganglion (DRG) and contribute to the analgesic effect of cannabinoids. However, the epigenetic mechanism regulating the expression of CB1Rs in neuropathic pain is unknown. G9a (encoded by the Ehmt2 gene), a histone 3 at lysine 9

Structural basis of G protein-coupled receptor-Gi protein interaction: formation of the cannabinoid CB2 receptor-Gi protein complex.

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In this study, we applied a comprehensive G protein-coupled receptor-Gαi protein chemical cross-linking strategy to map the cannabinoid receptor subtype 2 (CB2)-Gαi interface and then used molecular dynamics simulations to explore the dynamics of complex formation. Three cross-link sites were

Conformational memories and the endocannabinoid binding site at the cannabinoid CB1 receptor.

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Endocannabinoid stucture-activity relationships (SAR) indicate that the CB1 receptor recognizes ethanolamides whose fatty acid acyl chains have 20 or 22 carbons, with at least three homoallylic double bonds and saturation in at least the last five carbons of the acyl chain. To probe the molecular

Development of a 3D model for the human cannabinoid CB1 receptor.

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A novel comparison model of the human cannabinoid CB1 receptor has been constructed using the bovine rhodopsin X-ray structure as a template. The model was subjected to a 500-ps molecular dynamics simulation, and thereafter new conformers of the receptor model were produced in a simulated annealing

Cannabinoid antagonist AM 281 reduces mortality rate and neurologic dysfunction after cecal ligation and puncture in rats.

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OBJECTIVE The purpose of this study was to examine whether anandamide, an endogenous cannabinoid receptor ligand, is involved in the pathogenesis of septic encephalopathy. METHODS Prospective, controlled study. METHODS Male Wistar rats (7 wks old) were randomly divided into four groups as follows:

The role of nitric oxide in the local antiallodynic and antihyperalgesic effects and expression of delta-opioid and cannabinoid-2 receptors during neuropathic pain in mice.

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Both delta-opioid receptor (DOPr) and cannabinoid-2 receptor (CB2R) agonists attenuate neuropathic pain, but the precise mechanism implicated in these effects is not completely elucidated. We investigated whether nitric oxide synthesized by neuronal (NOS1) or inducible (NOS2) nitric-oxide synthases

A non-cannabinoid immunogen used to elicit antibodies with broad cross-reactivity to cannabinoid metabolites.

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A benzpyran derivative was linked to the lysines of bovine thyroglobulin (BTG) where 69% of the available lysines were modified. This derivative was designed to elicit antibodies that were directed towards the conserved epitopes of cannabinoid metabolites that appear in urine. Polyclonal antibodies

Evaluating the quality of protein from hemp seed (Cannabis sativa L.) products through the use of the protein digestibility-corrected amino acid score method.

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The macronutrient composition and the quality of protein of hemp seed and products derived from hemp seed grown in Western Canada were determined. Thirty samples of hemp products (minimum 500 g), including whole hemp seed, hemp seed meal from cold-press expelling, dehulled, or shelled, hemp seed and

Physicochemical and functional properties of hemp (Cannabis sativa L.) protein isolate.

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The amino acid composition and physicochemical and functional properties of hemp (Cannabis sativa L.) protein isolate (HPI) were evaluated and compared with those of soy protein isolate (SPI). Edestin, a kind of hexameric legumin, was the major protein component. HPI had similar or higher levels of

The Cannabis Proteome Draft Map Project.

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Recently we have seen a relaxation of the historic restrictions on the use and subsequent research on the Cannabis plants, generally classified as Cannabis sativa and Cannabisindica. What research has been performed to date has centered on chemical analysis of plant

Functional characterization of putative cholesterol binding sequence (CRAC) in human type-1 cannabinoid receptor.

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Endocannabinoid signaling modulates a variety of neuroinflammatory and neurodegenerative diseases, mainly through the activation of type-1 and type-2 (CB(1)R and CB(2)R) cannabinoid receptors. CB(1)R is negatively regulated by membrane cholesterol, while CB(2)R is unaffected. Here, we identified in

Proenkephalin mediates the enduring effects of adolescent cannabis exposure associated with adult opiate vulnerability.

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BACKGROUND Marijuana use by teenagers often predates the use of harder drugs, but the neurobiological underpinnings of such vulnerability are unknown. Animal studies suggest enhanced heroin self-administration (SA) and dysregulation of the endogenous opioid system in the nucleus accumbens shell

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