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Janssen cannabinoid cb(2) receptor activation
Cannabinoid Cb(2) Receptor Activation, supplied by Janssen, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Article Title: The Leu/Val 6.51 Side Chain of Cannabinoid Receptors Regulates the Binding Mode of the Alkyl Chain of Δ 9 -Tetrahydrocannabinol.
Article Snippet: 1999, 7 (12), 2905−14. (48) Li, X.; Chang, H.; Bouma, J.; de Paus, L. V.; Mukhopadhyay, P.; Paloczi, J.; Mustafa, M.; van der Horst, C.; Kumar, S. S.; Wu, L.; Yu, Y.; van den Berg, R.; Janssen, A. P. A.; Lichtman, A.; Liu, Z. J.; Pacher, P.; van der Stelt, M.; Heitman, L. H.; Hua, T. Structural basis of selective cannabinoid CB(2) receptor activation.

Article Title: Platform Reagents Enable Synthesis of Ligand-Directed Covalent Probes: Study of Cannabinoid Receptor 2 in Live Cells.
Article Snippet: Pharmacological modulation of cannabinoid receptor type 2 (CB2R) holds promise for the treatment of neuroinflammatory disorders, such as Alzheimer’s disease.. Despite the importance of CB2R, its expression and downstream signaling are insufficiently understood in diseaseand tissue-specific contexts.. Herein, we report the first liganddirected covalent (LDC) labeling of CB2R enabled by a novel synthetic strategy and application of platform reagents.



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Schematic diagram of the experimental protocol. A , Kahweol (Kah) was administered 175 min after the local administration of prostaglandin E 2 (PGE 2 ) (2 µg) and the antinociceptive response was measured prior to and 180 min, 195 min, and 210 min after PGE 2 injection. B , Kah was administered in the right hind paw 175 min after local injection of PGE 2 . The cannabinoid drugs AM251, <t>AM630,</t> MAFP, JZL184, or VDM11 were given 10 min prior (165 min) to Kah intraplantar administration and measurements were performed prior to and 180 min after PGE 2 administration.
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Schematic diagram of the experimental protocol. A , Kahweol (Kah) was administered 175 min after the local administration of prostaglandin E 2 (PGE 2 ) (2 µg) and the antinociceptive response was measured prior to and 180 min, 195 min, and 210 min after PGE 2 injection. B , Kah was administered in the right hind paw 175 min after local injection of PGE 2 . The cannabinoid drugs AM251, AM630, MAFP, JZL184, or VDM11 were given 10 min prior (165 min) to Kah intraplantar administration and measurements were performed prior to and 180 min after PGE 2 administration.

Journal: Brazilian Journal of Medical and Biological Research

Article Title: Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation

doi: 10.1590/1414-431X2021e11071

Figure Lengend Snippet: Schematic diagram of the experimental protocol. A , Kahweol (Kah) was administered 175 min after the local administration of prostaglandin E 2 (PGE 2 ) (2 µg) and the antinociceptive response was measured prior to and 180 min, 195 min, and 210 min after PGE 2 injection. B , Kah was administered in the right hind paw 175 min after local injection of PGE 2 . The cannabinoid drugs AM251, AM630, MAFP, JZL184, or VDM11 were given 10 min prior (165 min) to Kah intraplantar administration and measurements were performed prior to and 180 min after PGE 2 administration.

Article Snippet: The CB 1 cannabinoid receptor antagonist AM251 ( N -[piperidin-1-yl]-5-[4-iodophenyl]-1-[2,4-dichlorophenyl]-4-methyl-1 H -pyrazole-3-carboxamide; purity>99%; Tocris) (20, 40, 80 μg/paw) and the CB 2 cannabinoid receptor antagonist AM630 (6-Iodo-2-methyl-1-[2-{4-morpholinyl}ethyl]-1H-indol-3-yl [4-ethoxyphenyl] methanone; purity >98%; Tocris) (100 μg/paw) were dissolved in 10% DMSO, whereas the hyperalgesic agent PGE 2 (purity ≥93%; Sigma-Aldrich, USA) was dissolved in 2% ethanol.

Techniques: Injection

The CB 2 receptor antagonist did not block kahweol-induced peripheral antinociception in hyperalgesic paws. The antinociceptive response was measured by the paw pressure test. Prostaglandin E 2 (PGE 2 ) injection (2 µg/paw) was done at time 0, AM630 (100 µg/paw) was injected at time 165 min, and kahweol (Kah; 80 µg/paw) was given at 175 min. Measurements were made prior to and 180 min after PGE 2 administration. Data are reported as means±SE (n=5) of Δ nociceptive threshold measured in grams (g). *P<0.05 compared to PGE 2 + Veh 2 + Veh 3-injected group (ANOVA and Bonferroni's test). There was no significant difference between (PGE 2 + Veh 2 + Kah 80) and (PGE 2 + AM630 100 + Kah 80)-injected groups. Veh (vehicle) 2: 10% DMSO in saline; Veh 3: sterile saline solution (0.9% NaCl).

Journal: Brazilian Journal of Medical and Biological Research

Article Title: Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation

doi: 10.1590/1414-431X2021e11071

Figure Lengend Snippet: The CB 2 receptor antagonist did not block kahweol-induced peripheral antinociception in hyperalgesic paws. The antinociceptive response was measured by the paw pressure test. Prostaglandin E 2 (PGE 2 ) injection (2 µg/paw) was done at time 0, AM630 (100 µg/paw) was injected at time 165 min, and kahweol (Kah; 80 µg/paw) was given at 175 min. Measurements were made prior to and 180 min after PGE 2 administration. Data are reported as means±SE (n=5) of Δ nociceptive threshold measured in grams (g). *P<0.05 compared to PGE 2 + Veh 2 + Veh 3-injected group (ANOVA and Bonferroni's test). There was no significant difference between (PGE 2 + Veh 2 + Kah 80) and (PGE 2 + AM630 100 + Kah 80)-injected groups. Veh (vehicle) 2: 10% DMSO in saline; Veh 3: sterile saline solution (0.9% NaCl).

Article Snippet: The CB 1 cannabinoid receptor antagonist AM251 ( N -[piperidin-1-yl]-5-[4-iodophenyl]-1-[2,4-dichlorophenyl]-4-methyl-1 H -pyrazole-3-carboxamide; purity>99%; Tocris) (20, 40, 80 μg/paw) and the CB 2 cannabinoid receptor antagonist AM630 (6-Iodo-2-methyl-1-[2-{4-morpholinyl}ethyl]-1H-indol-3-yl [4-ethoxyphenyl] methanone; purity >98%; Tocris) (100 μg/paw) were dissolved in 10% DMSO, whereas the hyperalgesic agent PGE 2 (purity ≥93%; Sigma-Aldrich, USA) was dissolved in 2% ethanol.

Techniques: Blocking Assay, Randall–Selitto Test, Injection, Saline, Sterility

Effect of ZnONPs on aorta contractility. ( a ) Effect of ACPA (CB 1 receptor agonist) on contraction in aortic rings in different experimental groups. ( b ) Effect of HU308 (CB 2 receptor agonist) on contraction in aortic rings in different experimental groups. Blue bars correspond to the control non-treated group, green bars correspond to the ZnONPs treated-groups at different times; ( a ) there is a significant difference compared to the phenylephrine group with p < 0.05; ( b ) there is a significant difference compared to the control group with p < 0.05.

Journal: Nanomaterials

Article Title: ZnO Nanoparticles Induce Dyslipidemia and Atherosclerotic Lesions Leading to Changes in Vascular Contractility and Cannabinoid Receptors Expression as Well as Increased Blood Pressure

doi: 10.3390/nano11092319

Figure Lengend Snippet: Effect of ZnONPs on aorta contractility. ( a ) Effect of ACPA (CB 1 receptor agonist) on contraction in aortic rings in different experimental groups. ( b ) Effect of HU308 (CB 2 receptor agonist) on contraction in aortic rings in different experimental groups. Blue bars correspond to the control non-treated group, green bars correspond to the ZnONPs treated-groups at different times; ( a ) there is a significant difference compared to the phenylephrine group with p < 0.05; ( b ) there is a significant difference compared to the control group with p < 0.05.

Article Snippet: Next, aorta sections were blocked (Animal-free blocker and diluent, Vector laboratories Inc., Burlingame, CA, USA) and incubated with rabbit polyclonal Anti-CB 1 (1:100, Alomone, Labs, Jerusalem, Israel) or rabbit polyclonal Anti-CB 2 (1:100, Alomone, Labs, Jerusalem, Israel) primary antibody and co-labeled with mouse monoclonal Anti-alpha smooth muscle Actin antibody (1:200, Abcam, Cambrige, UK) overnight.

Techniques:

Effect of ZnONPs on the CB 1 and CB 2 receptors expression in the aorta wall. ( a ) CB 1 expression, ( b ) CB 2 expression. Blue bars correspond to the control non-treated group, green bars correspond to the ZnONPs treated-groups at different times; ( a ) there is a significant difference compared to the control group with p < 0.05.

Journal: Nanomaterials

Article Title: ZnO Nanoparticles Induce Dyslipidemia and Atherosclerotic Lesions Leading to Changes in Vascular Contractility and Cannabinoid Receptors Expression as Well as Increased Blood Pressure

doi: 10.3390/nano11092319

Figure Lengend Snippet: Effect of ZnONPs on the CB 1 and CB 2 receptors expression in the aorta wall. ( a ) CB 1 expression, ( b ) CB 2 expression. Blue bars correspond to the control non-treated group, green bars correspond to the ZnONPs treated-groups at different times; ( a ) there is a significant difference compared to the control group with p < 0.05.

Article Snippet: Next, aorta sections were blocked (Animal-free blocker and diluent, Vector laboratories Inc., Burlingame, CA, USA) and incubated with rabbit polyclonal Anti-CB 1 (1:100, Alomone, Labs, Jerusalem, Israel) or rabbit polyclonal Anti-CB 2 (1:100, Alomone, Labs, Jerusalem, Israel) primary antibody and co-labeled with mouse monoclonal Anti-alpha smooth muscle Actin antibody (1:200, Abcam, Cambrige, UK) overnight.

Techniques: Expressing

Representative images showed ZnONPs effect on CB 1 and CB 2 receptors expression in aorta wall. Transmitted light images (grey). Scale bar corresponds to 50 μm. Smooth muscle α-actin was detected with a specific antibody labeled with Alexa Fluor 568 (red). CB 1 and CB 2 located on the aorta ring were detected by specific antibodies and labeled with FITC (green). Image overlap indicates a high degree of colocalization of CB 1 or CB 2, and smooth muscle α-actin (yellow). Nuclei were counterstained with DAPI dye (blue).

Journal: Nanomaterials

Article Title: ZnO Nanoparticles Induce Dyslipidemia and Atherosclerotic Lesions Leading to Changes in Vascular Contractility and Cannabinoid Receptors Expression as Well as Increased Blood Pressure

doi: 10.3390/nano11092319

Figure Lengend Snippet: Representative images showed ZnONPs effect on CB 1 and CB 2 receptors expression in aorta wall. Transmitted light images (grey). Scale bar corresponds to 50 μm. Smooth muscle α-actin was detected with a specific antibody labeled with Alexa Fluor 568 (red). CB 1 and CB 2 located on the aorta ring were detected by specific antibodies and labeled with FITC (green). Image overlap indicates a high degree of colocalization of CB 1 or CB 2, and smooth muscle α-actin (yellow). Nuclei were counterstained with DAPI dye (blue).

Article Snippet: Next, aorta sections were blocked (Animal-free blocker and diluent, Vector laboratories Inc., Burlingame, CA, USA) and incubated with rabbit polyclonal Anti-CB 1 (1:100, Alomone, Labs, Jerusalem, Israel) or rabbit polyclonal Anti-CB 2 (1:100, Alomone, Labs, Jerusalem, Israel) primary antibody and co-labeled with mouse monoclonal Anti-alpha smooth muscle Actin antibody (1:200, Abcam, Cambrige, UK) overnight.

Techniques: Expressing, Labeling

Cannabinoid receptor binding affinities of cannabinoids tested in this study

Journal: Addiction biology

Article Title: Optogenetic brain-stimulation reward: A new procedure to re-evaluate the rewarding versus aversive effects of cannabinoids in dopamine transporter-Cre mice

doi: 10.1111/adb.13005

Figure Lengend Snippet: Cannabinoid receptor binding affinities of cannabinoids tested in this study

Article Snippet: Dual-labeling IHC was performed using a CB 2 R antibody (Alomone, #ACR-002, 1:250) and an anti-tyrosine hydroxylase (anti-TH) monoclonal antibody (1:500; Millipore, Billerica, MA, USA).

Techniques: Binding Assay