Journal: ACS Omega

Article Title: Novel Machaeriol Analogues as Modulators of Cannabinoid Receptors: Structure–Activity Relationships of (+)-Hexahydrocannabinoids and Their Isoform Selectivities

doi: 10.1021/acsomega.1c02413

Figure Lengend Snippet: 2D diagram of atomic-level interaction of the CB 2 –11J complex with key CB 2 R residues during the 200 ns MD simulation.

Article Snippet: Expression clones containing CB 1 R and CB 2 R full-length cDNA were purchased OriGene (Rockville, MD, USA).

Techniques:

Journal: ACS Omega

Article Title: Novel Machaeriol Analogues as Modulators of Cannabinoid Receptors: Structure–Activity Relationships of (+)-Hexahydrocannabinoids and Their Isoform Selectivities

doi: 10.1021/acsomega.1c02413

Figure Lengend Snippet: 2D diagram of atomic-level interaction of the CB 2 –11H complex with key CB 2 R residues during the 200 ns MD simulation.

Article Snippet: Expression clones containing CB 1 R and CB 2 R full-length cDNA were purchased OriGene (Rockville, MD, USA).

Techniques:

Journal: International Journal of Neuropsychopharmacology

Article Title: Impaired 2-AG Signaling in Hippocampal Glutamatergic Neurons: Aggravation of Anxiety-Like Behavior and Unaltered Seizure Susceptibility

doi: 10.1093/ijnp/pyv091

Figure Lengend Snippet: Monoacylgycerol lipase (MAGL) overexpression in hippocampal pyramidal neurons leads to alteration in 2-arachidonoyl glycerol (2-AG) degradation and 2-AG levels. (A) Michaelis-Menten enzyme kinetics revealed highly elevated MAGL activity in adeno-associated virus (AAV)-Glu-MAGL mice compared with AAV-WT controls (n=4). (B) AAV-Glu-MAGL mice showed an increased maximum turnover rate of the substrate. (C-E) 2-AG levels were significantly lower in AAV-Glu-MAGL mice than in AAV-WT controls (n=6), while the levels of AEA and arachidonic acid were unchanged. *** P <.001. (F) Cannabinoid type-1 receptor (CB1R) protein levels were not altered in AAV-Glu-MAGL mice compared with AAV-WT (n=8). (G) Hippocampal homogenates were stimulated with increasing concentrations of WIN 55,212-2 (from 5 pM to 50 µM) to generate dose-response curves. EC 50 values were similar in the 2 animal groups analyzed (0.36 µM and 0.48 µM in AAV-WT and AAV-Glu-MAGL, respectively). WIN 55,212-2-stimulated [ 35 S]-GTPγS binding is expressed as percent of basal binding (n=4).

Article Snippet: Agonist-stimulated binding was measured by using increasing concentrations (from 5 pM to 50 μM) of the CB1R agonist WIN 55,212-2 (Biotrend).

Techniques: Over Expression, Activity Assay, Virus, Binding Assay

Journal: International Journal of Neuropsychopharmacology

Article Title: Impaired 2-AG Signaling in Hippocampal Glutamatergic Neurons: Aggravation of Anxiety-Like Behavior and Unaltered Seizure Susceptibility

doi: 10.1093/ijnp/pyv091

Figure Lengend Snippet: Hemagglutinin (HA)-tagged monoacylgycerol lipase (MAGL) colocalization with VGluT1 and cannabinoid type-1 receptor (CB1R) in glutamatergic terminals. (A) Overview of triple immunostaining in the hippocampus of adeno-associated virus (AAV)-Glu-MAGL mice to localize HA (A`), VGluT1 (A``), and CB1R (A```), respectively. Ectopic MAGL expression was found in the stratum oriens, stratum radiatum, and the inner third of the molecular layer, while cell somata of CA1 pyramidal neurons were spared. GC, granule cell layer; Hil, hilar region; LMol, stratum lacunosum-moleculare; Mol, stratum moleculare; Or, stratum oriens; Pyr, CA1/CA3 pyramidal cell layer; Rad, stratum radiatum. (B-C) Higher magnification micrographs as shown in A, indicating that HA-tagged MAGL colocalized with VGluT1 and CB1R.

Article Snippet: Agonist-stimulated binding was measured by using increasing concentrations (from 5 pM to 50 μM) of the CB1R agonist WIN 55,212-2 (Biotrend).

Techniques: Triple Immunostaining, Virus, Expressing