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cb2r antagonist sr144528 (MedChemExpress)

Name: cb2r antagonist sr144528
Brand: MedChemExpress
Rating: 92 (12 reviews)

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MedChemExpress cb2r antagonist sr144528
Cb2r Antagonist Sr144528, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 92/100, based on 12 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 92 stars, based on 12 article reviews

cb2r antagonist sr144528 - by Bioz Stars, 2026-02

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PM289 attenuates TNFα-induced upregulation of ICAM-1. A. hCMEC/D3 cells were treated with 100 ng/mL TNFα for 24 h with or without concentrations with PM289 (10 nM, 100 nM, 1 μM and 10 μM). Controls included untreated cells and cells treated with PM289 only. One group included TNFα, PM289 and SR144528. Cells were harvested in lysis buffer and proteins were separated by SDS-page for Western blot analysis. The adhesion molecule ICAM-1and β-Actin were resolved at 110 and 42 kDa respectively. B–E. Quantification of changes in ICAM-1 expression normalized to the untreated condition for PM289 concentrations 10 nM (B), 100 nM (C), 1 μM (D) and 10 μM (E). For all concentrations PM289 significantly reduced ICAM-1 expression in response to TNFα. Treatment with the CB2R antagonist SR144528 prevented the effects of PM289. All experiments were performed with n=3. **p<0.01.

Journal: Neuroimmune Pharmacology and Therapeutics

Article Title: Activation of CB2R by synthetic CB2R agonist, PM289, improves brain endothelial barrier properties, decreases inflammatory response and enhances endothelial repair

doi: 10.1515/nipt-2023-0016

Figure Lengend Snippet: PM289 attenuates TNFα-induced upregulation of ICAM-1. A. hCMEC/D3 cells were treated with 100 ng/mL TNFα for 24 h with or without concentrations with PM289 (10 nM, 100 nM, 1 μM and 10 μM). Controls included untreated cells and cells treated with PM289 only. One group included TNFα, PM289 and SR144528. Cells were harvested in lysis buffer and proteins were separated by SDS-page for Western blot analysis. The adhesion molecule ICAM-1and β-Actin were resolved at 110 and 42 kDa respectively. B–E. Quantification of changes in ICAM-1 expression normalized to the untreated condition for PM289 concentrations 10 nM (B), 100 nM (C), 1 μM (D) and 10 μM (E). For all concentrations PM289 significantly reduced ICAM-1 expression in response to TNFα. Treatment with the CB2R antagonist SR144528 prevented the effects of PM289. All experiments were performed with n=3. **p<0.01.

Article Snippet: The commercially available CB2R antagonist, SR144528 was purchased from Cayman Chemical Company (Ann Arbor, MI) and resuspended in dimethyl sulfoxide (DMSO), purchased from Millipore Sigma (St. Louis, MO).

Techniques: Lysis, SDS Page, Western Blot, Expressing

Pharmacological activation of CB2R ameliorates PA-induced alveolar damage and decline in lung function. C57BL/6 J WT mice were treated with vehicle (V) or JWH133 (J) or SR144528 (SR) + JWH133 (J) and exposed to either PBS (control) or PA. Lung injury was assessed after 24 h. Total cell number ( a ) and total protein content ( b ) in the BALF were determined from the mice treated with varying doses of JWH133 and exposed to PA infection (0 mg/kg JWH133:vehicle). c Representative H&E images of mice lungs. Total protein content in the BALF ( d ) was determined. e The lung bacterial burden was evaluated by measuring the bacterial load in the whole lung. f Tissue dampening (G), g tissue elastance (H), and, h static lung compliance (Cst) were examined using the FlexiVent system. n = 5–8, **p < 0.01, ***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Journal: Respiratory Research

Article Title: Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation

doi: 10.1186/s12931-022-02253-w

Figure Lengend Snippet: Pharmacological activation of CB2R ameliorates PA-induced alveolar damage and decline in lung function. C57BL/6 J WT mice were treated with vehicle (V) or JWH133 (J) or SR144528 (SR) + JWH133 (J) and exposed to either PBS (control) or PA. Lung injury was assessed after 24 h. Total cell number ( a ) and total protein content ( b ) in the BALF were determined from the mice treated with varying doses of JWH133 and exposed to PA infection (0 mg/kg JWH133:vehicle). c Representative H&E images of mice lungs. Total protein content in the BALF ( d ) was determined. e The lung bacterial burden was evaluated by measuring the bacterial load in the whole lung. f Tissue dampening (G), g tissue elastance (H), and, h static lung compliance (Cst) were examined using the FlexiVent system. n = 5–8, **p < 0.01, ***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Article Snippet: CB2R agonist JWH133 (1738, Tocris Biosciences) and CB2R antagonist SR144528 (5039, Tocris Biosciences) were dissolved in a vehicle (1% DMSO + 1% Tween-80 in PBS).

Techniques: Activation Assay, Infection

JWH133 treatment reduces PA-induced lung inflammation in mice. C57BL/6 J WT mice were treated with vehicle or JWH133 or SR144528 + JWH133 and exposed to either PBS (control) or PA. BALF was collected after 24 h and total cell number ( a ), and neutrophil population ( b ) were determined. The levels of inflammatory cytokines IL-1β ( c ), IL-6 ( d ), TNF-α ( e ), and chemokines KC ( f ) and MIP-2( g ) were tested. Mouse primary AMs were exposed to PA and the levels of IL-1β ( h ) and TNF-α ( i ) in the cell culture supernatant were evaluated after 16 h of PA exposure. n = 5–8, **p < 0.01, ***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Journal: Respiratory Research

Article Title: Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation

doi: 10.1186/s12931-022-02253-w

Figure Lengend Snippet: JWH133 treatment reduces PA-induced lung inflammation in mice. C57BL/6 J WT mice were treated with vehicle or JWH133 or SR144528 + JWH133 and exposed to either PBS (control) or PA. BALF was collected after 24 h and total cell number ( a ), and neutrophil population ( b ) were determined. The levels of inflammatory cytokines IL-1β ( c ), IL-6 ( d ), TNF-α ( e ), and chemokines KC ( f ) and MIP-2( g ) were tested. Mouse primary AMs were exposed to PA and the levels of IL-1β ( h ) and TNF-α ( i ) in the cell culture supernatant were evaluated after 16 h of PA exposure. n = 5–8, **p < 0.01, ***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Article Snippet: CB2R agonist JWH133 (1738, Tocris Biosciences) and CB2R antagonist SR144528 (5039, Tocris Biosciences) were dissolved in a vehicle (1% DMSO + 1% Tween-80 in PBS).

Techniques: Cell Culture

Genetic deletion of CB2R worsens PA-induced lung injury and inflammation. CB2KO and WT mice were pre-treated with JWH133 and exposed PA. Control mice received i.t. injections of PBS. BALF was collected after 24 h and total cell number ( a ), and total protein content ( b ) were determined. ELISA detection of inflammatory cytokines IL-1β ( c ), TNF-α ( d ), and chemokines KC ( e ) and MIP-2 ( f ) in the BALF at 24 h after PA exposure. n = 5-8, **p < 0.01, ***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Journal: Respiratory Research

Article Title: Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation

doi: 10.1186/s12931-022-02253-w

Figure Lengend Snippet: Genetic deletion of CB2R worsens PA-induced lung injury and inflammation. CB2KO and WT mice were pre-treated with JWH133 and exposed PA. Control mice received i.t. injections of PBS. BALF was collected after 24 h and total cell number ( a ), and total protein content ( b ) were determined. ELISA detection of inflammatory cytokines IL-1β ( c ), TNF-α ( d ), and chemokines KC ( e ) and MIP-2 ( f ) in the BALF at 24 h after PA exposure. n = 5-8, **p < 0.01, ***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Article Snippet: CB2R agonist JWH133 (1738, Tocris Biosciences) and CB2R antagonist SR144528 (5039, Tocris Biosciences) were dissolved in a vehicle (1% DMSO + 1% Tween-80 in PBS).

Techniques: Enzyme-linked Immunosorbent Assay

CB2R regulates PA-induced neutrophil activation. a Representative Immunostaining image of MPO (red) in WT mice lung pre-treated with vehicle (WT-V) or JWH133 (WT-J) and CB2KO mice lung pre-treated with JWH133 (CB2KO-J) and exposed to PBS (control) or PA for 24 h. T1α staining (green) was used to indicate the epithelial cells. BALF was collected at 24 h after PA infection and the release of CitH3 and H2B were analyzed by immunoblot. Representative immunoblot ( b ) and quantification ( c ) of CitH3 and H2B in BALF from WT mice pretreated with vehicle or JWH133 and exposed to PBS (control) or PA. Representative immunoblot ( d ) and quantification ( e ) of CitH3 and H2B in BALF from WT Vs CB2KO mice pretreated with vehicle or JWH133 and exposed to PBS (control) or PA. n = 4, **p < 0.01***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Journal: Respiratory Research

Article Title: Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation

doi: 10.1186/s12931-022-02253-w

Figure Lengend Snippet: CB2R regulates PA-induced neutrophil activation. a Representative Immunostaining image of MPO (red) in WT mice lung pre-treated with vehicle (WT-V) or JWH133 (WT-J) and CB2KO mice lung pre-treated with JWH133 (CB2KO-J) and exposed to PBS (control) or PA for 24 h. T1α staining (green) was used to indicate the epithelial cells. BALF was collected at 24 h after PA infection and the release of CitH3 and H2B were analyzed by immunoblot. Representative immunoblot ( b ) and quantification ( c ) of CitH3 and H2B in BALF from WT mice pretreated with vehicle or JWH133 and exposed to PBS (control) or PA. Representative immunoblot ( d ) and quantification ( e ) of CitH3 and H2B in BALF from WT Vs CB2KO mice pretreated with vehicle or JWH133 and exposed to PBS (control) or PA. n = 4, **p < 0.01***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Article Snippet: CB2R agonist JWH133 (1738, Tocris Biosciences) and CB2R antagonist SR144528 (5039, Tocris Biosciences) were dissolved in a vehicle (1% DMSO + 1% Tween-80 in PBS).

Techniques: Activation Assay, Immunostaining, Staining, Infection, Western Blot

CB2R regulates NLRP3 inflammasome activation in PA pneumonia. C57BL/6 J WT mice received either vehicle (V) or JWH133 (J) and were exposed to PBS or PA. Lung NLRP3 inflammasome activation was assessed by measuring the protein levels of NLRP3, ASC, and (p20) caspase-1. Representative immunoblot images are shown in panel ( a ) and densitometry data are presented in panel ( b ). CB2KO and WT mice received JWH133 and were exposed to PBS or PA and the protein levels of NLRP3, ASC, and (p20) caspase-1 were analyzed by immunoblot. Representative immunoblot images are shown in panel ( c ) and densitometry data are presented in panel ( d ). n = 5, **p < 0.01***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Journal: Respiratory Research

Article Title: Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation

doi: 10.1186/s12931-022-02253-w

Figure Lengend Snippet: CB2R regulates NLRP3 inflammasome activation in PA pneumonia. C57BL/6 J WT mice received either vehicle (V) or JWH133 (J) and were exposed to PBS or PA. Lung NLRP3 inflammasome activation was assessed by measuring the protein levels of NLRP3, ASC, and (p20) caspase-1. Representative immunoblot images are shown in panel ( a ) and densitometry data are presented in panel ( b ). CB2KO and WT mice received JWH133 and were exposed to PBS or PA and the protein levels of NLRP3, ASC, and (p20) caspase-1 were analyzed by immunoblot. Representative immunoblot images are shown in panel ( c ) and densitometry data are presented in panel ( d ). n = 5, **p < 0.01***p < 0.001, ****p < 0.0001. Data are presented as mean ± SEM

Article Snippet: CB2R agonist JWH133 (1738, Tocris Biosciences) and CB2R antagonist SR144528 (5039, Tocris Biosciences) were dissolved in a vehicle (1% DMSO + 1% Tween-80 in PBS).

Techniques: Activation Assay, Western Blot

CB2R activation reduces NF-κB activation in PA pneumonia: C57BL/6 J WT mice received either vehicle (V) or JWH133 (J) and were exposed to PBS (control) or PA. NF-κB activation was assessed by measuring the protein levels of P-p65 and p65 in the lung. Representative immunoblot images are shown in panel ( a ) and densitometry data are presented in panel ( b ). n = 5, **p < 0.01***p < 0.001. Data are presented as mean ± SEM

Journal: Respiratory Research

Article Title: Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation

doi: 10.1186/s12931-022-02253-w

Figure Lengend Snippet: CB2R activation reduces NF-κB activation in PA pneumonia: C57BL/6 J WT mice received either vehicle (V) or JWH133 (J) and were exposed to PBS (control) or PA. NF-κB activation was assessed by measuring the protein levels of P-p65 and p65 in the lung. Representative immunoblot images are shown in panel ( a ) and densitometry data are presented in panel ( b ). n = 5, **p < 0.01***p < 0.001. Data are presented as mean ± SEM

Article Snippet: CB2R agonist JWH133 (1738, Tocris Biosciences) and CB2R antagonist SR144528 (5039, Tocris Biosciences) were dissolved in a vehicle (1% DMSO + 1% Tween-80 in PBS).

Techniques: Activation Assay, Western Blot

CB2R-dependent inhibition of FSK-stimulated cAMP and CB2R-dependent recruitment of βarrestin2. CHO cells stably expressing h CB2R were treated with 0.10 nM–10 μM compounds for 90 min, and cAMP inhibition (a,b) or βarrestin2 recruitment (c,d) was measured. cAMP and βarrestin2 recruitment data are expressed as the % CP55,940 response. Data were fitted to a nonlinear regression (three-parameter model, GraphPad v. 9.0). Data are mean ± S.E.M. of 6 independent experiments performed in triplicate. Data from these graphs is presented in Table . Statistical data for these graphs are presented in Table S1 .

Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: CB2R-dependent inhibition of FSK-stimulated cAMP and CB2R-dependent recruitment of βarrestin2. CHO cells stably expressing h CB2R were treated with 0.10 nM–10 μM compounds for 90 min, and cAMP inhibition (a,b) or βarrestin2 recruitment (c,d) was measured. cAMP and βarrestin2 recruitment data are expressed as the % CP55,940 response. Data were fitted to a nonlinear regression (three-parameter model, GraphPad v. 9.0). Data are mean ± S.E.M. of 6 independent experiments performed in triplicate. Data from these graphs is presented in Table . Statistical data for these graphs are presented in Table S1 .

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Inhibition, Stable Transfection, Expressing

CB2R-dependent inhibition of FSK-stimulated cAMP CHO cells stably expressing h CB2R. cAMP inhibition data are expressed as the % CP55,940 response. Cells were treated with ligands simultaneously as indicated. 10 nM FM-6b (a), 50 nM FD-22a (b), and 5 nM FD-24a (c) were chosen after the completion of preliminary experiments with compounds alone for ease of calculations to approximate the EC 50 for each compound alone. Addition of 100 nM SR144528 to 0.1 nM–10 μM of FD-22a (d) or of FD-24a (e). Data were fitted to a nonlinear regression (three-parameter model, GraphPad v. 9.0). Data are mean ± S.E.M. of 3–6 independent experiments performed in triplicate. Data from these graphs is presented in Table . Statistical data for these graphs are presented in Table S2 .

Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: CB2R-dependent inhibition of FSK-stimulated cAMP CHO cells stably expressing h CB2R. cAMP inhibition data are expressed as the % CP55,940 response. Cells were treated with ligands simultaneously as indicated. 10 nM FM-6b (a), 50 nM FD-22a (b), and 5 nM FD-24a (c) were chosen after the completion of preliminary experiments with compounds alone for ease of calculations to approximate the EC 50 for each compound alone. Addition of 100 nM SR144528 to 0.1 nM–10 μM of FD-22a (d) or of FD-24a (e). Data were fitted to a nonlinear regression (three-parameter model, GraphPad v. 9.0). Data are mean ± S.E.M. of 3–6 independent experiments performed in triplicate. Data from these graphs is presented in Table . Statistical data for these graphs are presented in Table S2 .

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Inhibition, Stable Transfection, Expressing

[ H]CP55, 940 binding to CB1R (a) and CB2R (b). Membranes from CHO cells stably expressing h CB1R or h CB2R were treated with 1 nM [ H]CP55,940 and 0.10 nM–10 μM compounds for 2 h. Data are expressed as %[ H]CP55,940 bound. Data were fitted to a nonlinear regression (three-parameter model, GraphPad v. 9.0). Data are mean ± S.E.M. of 3 independent experiments performed in duplicate. Data from these graphs is presented in Table . Statistical data for these graphs are presented in Table S3 .

Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: [ H]CP55, 940 binding to CB1R (a) and CB2R (b). Membranes from CHO cells stably expressing h CB1R or h CB2R were treated with 1 nM [ H]CP55,940 and 0.10 nM–10 μM compounds for 2 h. Data are expressed as %[ H]CP55,940 bound. Data were fitted to a nonlinear regression (three-parameter model, GraphPad v. 9.0). Data are mean ± S.E.M. of 3 independent experiments performed in duplicate. Data from these graphs is presented in Table . Statistical data for these graphs are presented in Table S3 .

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Binding Assay, Stable Transfection, Expressing

Ability of FD-22a (A,C) and FD-24a (B,D) to decrease the inflammatory phenotype of LPS-stimulated BV2 microglial cells by the modulation of CB2R. Bars represent the release (pg/mL) of ILs in the presence of the drugs. Data represent mean ± (bars) from n = 3 independent experiments performed in duplicate. Statistical analysis was performed by ordinary one-way ANOVA followed by Tukey’s multiple comparison test. * p < 0.05, ** p < 0.01 and *** p < 0.001.

Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: Ability of FD-22a (A,C) and FD-24a (B,D) to decrease the inflammatory phenotype of LPS-stimulated BV2 microglial cells by the modulation of CB2R. Bars represent the release (pg/mL) of ILs in the presence of the drugs. Data represent mean ± (bars) from n = 3 independent experiments performed in duplicate. Statistical analysis was performed by ordinary one-way ANOVA followed by Tukey’s multiple comparison test. * p < 0.05, ** p < 0.01 and *** p < 0.001.

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Comparison

Release of inflammatory (IL-6) (A) and anti-inflammatory (IL-10) (B) interleukins induced by different concentrations of FD-22a . Data represent means ± S.E.M. from n = 3 independent experiments performed in duplicate. The selective CB2R agonist JWH133 was used as positive control. Statistical analysis was performed by ordinary one-way ANOVA followed by Tukey’s multiple comparison test. ** p < 0.01 and *** p < 0.001 compared to cells treated with LPS and TNFα.

Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: Release of inflammatory (IL-6) (A) and anti-inflammatory (IL-10) (B) interleukins induced by different concentrations of FD-22a . Data represent means ± S.E.M. from n = 3 independent experiments performed in duplicate. The selective CB2R agonist JWH133 was used as positive control. Statistical analysis was performed by ordinary one-way ANOVA followed by Tukey’s multiple comparison test. ** p < 0.01 and *** p < 0.001 compared to cells treated with LPS and TNFα.

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Positive Control, Comparison

Ability of FD-22a to decrease the inflammatory phenotype of LPS + TNFα–stimulated HMC3 by the modulation of CB2R. Bars represent the release (pg/mL) of IL-6 (A) and IL-10 (B) in the presence of the drugs at the indicated concentrations. Data represent means ± S.E.M. from n = 3 independent experiments performed in duplicate. Statistical analysis was performed by ordinary one-way ANOVA followed by Tukey’s multiple comparison test.* p < 0.05, ** p < 0.01 and *** p < 0.001.

Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: Ability of FD-22a to decrease the inflammatory phenotype of LPS + TNFα–stimulated HMC3 by the modulation of CB2R. Bars represent the release (pg/mL) of IL-6 (A) and IL-10 (B) in the presence of the drugs at the indicated concentrations. Data represent means ± S.E.M. from n = 3 independent experiments performed in duplicate. Statistical analysis was performed by ordinary one-way ANOVA followed by Tukey’s multiple comparison test.* p < 0.05, ** p < 0.01 and *** p < 0.001.

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Comparison

Effects of CB2 antagonism on FD-22a pain relieving efficacy. The response to a thermal stimulus was evaluated by the cold plate test measuring the latency (s) to pain-related behaviors (lifting or licking of the paw). Mice were daily treated i.p . with oxaliplatin 2.4 mg kg –1 . Tests were performed on day 15. The selective CB2R antagonists MC21 and SR144528 (10 mg kg –1 ) were administered i.p. 15 min before FD-22a (20 mg kg –1 p.o. ). Measurements were performed 15, 30, 45, 60, and 75 min after the injection of FD-22a . Control mice were treated with a vehicle. Each value represents the mean of 16 mice per group performed in 2 different experimental sets. **p < 0.01 vs vehicle + vehicle treated mice ^p < 0.05 and ^^p < 0.01 vs oxaliplatin + vehicle treated mice.

Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: Effects of CB2 antagonism on FD-22a pain relieving efficacy. The response to a thermal stimulus was evaluated by the cold plate test measuring the latency (s) to pain-related behaviors (lifting or licking of the paw). Mice were daily treated i.p . with oxaliplatin 2.4 mg kg –1 . Tests were performed on day 15. The selective CB2R antagonists MC21 and SR144528 (10 mg kg –1 ) were administered i.p. 15 min before FD-22a (20 mg kg –1 p.o. ). Measurements were performed 15, 30, 45, 60, and 75 min after the injection of FD-22a . Control mice were treated with a vehicle. Each value represents the mean of 16 mice per group performed in 2 different experimental sets. **p < 0.01 vs vehicle + vehicle treated mice ^p < 0.05 and ^^p < 0.01 vs oxaliplatin + vehicle treated mice.

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Injection, Control

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Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: Inhibition of Forskolin-Stimulated cAMP a

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Inhibition

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Journal: Journal of Medicinal Chemistry

Article Title: Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands

doi: 10.1021/acs.jmedchem.2c00582

Figure Lengend Snippet: [ 3 H] CP55,940 Binding a

Article Snippet: The selective CB2R antagonists SR144528 (Tocris Bioscience, UK) and MC21 were dissolved in saline solution with 5% DMSO and 5% Tween 20.

Techniques: Binding Assay

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