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Potencies and efficacies of H 4 R ligands in the luciferase reporter gene assay at the hH 4 R, the mH 4 R and the rH 4 R.
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Image Search Results


Potencies and efficacies of H 4 R ligands in the luciferase reporter gene assay at the hH 4 R, the mH 4 R and the rH 4 R.

Journal: PLoS ONE

Article Title: Luciferase Reporter Gene Assay on Human, Murine and Rat Histamine H 4 Receptor Orthologs: Correlations and Discrepancies between Distal and Proximal Readouts

doi: 10.1371/journal.pone.0073961

Figure Lengend Snippet: Potencies and efficacies of H 4 R ligands in the luciferase reporter gene assay at the hH 4 R, the mH 4 R and the rH 4 R.

Article Snippet: The log (r - 1) values were plotted against the corresponding log [JNJ 7777120] values according to the Schild equation and analyzed by linear regression with GraphPad Prism 5.04.

Techniques: Luciferase, Reporter Gene Assay

Reference data of H 4 R ligands determined in the [ 35 S]GTPγS binding assay at the hH 4 R, the mH 4 R and the rH 4 R and reported in literature.

Journal: PLoS ONE

Article Title: Luciferase Reporter Gene Assay on Human, Murine and Rat Histamine H 4 Receptor Orthologs: Correlations and Discrepancies between Distal and Proximal Readouts

doi: 10.1371/journal.pone.0073961

Figure Lengend Snippet: Reference data of H 4 R ligands determined in the [ 35 S]GTPγS binding assay at the hH 4 R, the mH 4 R and the rH 4 R and reported in literature.

Article Snippet: The log (r - 1) values were plotted against the corresponding log [JNJ 7777120] values according to the Schild equation and analyzed by linear regression with GraphPad Prism 5.04.

Techniques: Binding Assay

(A) Potencies and efficacies of histamine (HA), thioperamide (THIO), UR-PI294 and JNJ 7777120 at the hH 4 R, (B) the mH 4 R and (C) the rH 4 R (agonist mode). (D) Reversal of the HA (100–150 nM) mediated inhibition of the forskolin-stimulated luciferase activity by JNJ 7777120 at the hH 4 R and the mH 4 R (antagonist mode), in the luciferase reporter gene assay in HEK293T cells. Reaction mixtures contained ligands at the concentrations indicated on the abscissa to achieve saturated concentration response curves. Data points shown are the mean ± SEM of at least three independent experiments performed in triplicate. Data points connected by dashed lines reflect H 4 R-independent increase in luciferase activity at high ligand concentrations. The corresponding values were therefore excluded from non-linear correlations (D).

Journal: PLoS ONE

Article Title: Luciferase Reporter Gene Assay on Human, Murine and Rat Histamine H 4 Receptor Orthologs: Correlations and Discrepancies between Distal and Proximal Readouts

doi: 10.1371/journal.pone.0073961

Figure Lengend Snippet: (A) Potencies and efficacies of histamine (HA), thioperamide (THIO), UR-PI294 and JNJ 7777120 at the hH 4 R, (B) the mH 4 R and (C) the rH 4 R (agonist mode). (D) Reversal of the HA (100–150 nM) mediated inhibition of the forskolin-stimulated luciferase activity by JNJ 7777120 at the hH 4 R and the mH 4 R (antagonist mode), in the luciferase reporter gene assay in HEK293T cells. Reaction mixtures contained ligands at the concentrations indicated on the abscissa to achieve saturated concentration response curves. Data points shown are the mean ± SEM of at least three independent experiments performed in triplicate. Data points connected by dashed lines reflect H 4 R-independent increase in luciferase activity at high ligand concentrations. The corresponding values were therefore excluded from non-linear correlations (D).

Article Snippet: The log (r - 1) values were plotted against the corresponding log [JNJ 7777120] values according to the Schild equation and analyzed by linear regression with GraphPad Prism 5.04.

Techniques: Inhibition, Luciferase, Activity Assay, Reporter Gene Assay, Concentration Assay

Representative H 4 R-independent increase in the forskolin (1 µM) stimulated luciferase activity by ciproxyfan (CIP), proxyfan (PRO), JNJ 7777120 and thioperamide (THIO) in HEK293T-CRE-Luc cells, stably expressing the CRE-controlled luciferase and devoid of the H 4 R.

Journal: PLoS ONE

Article Title: Luciferase Reporter Gene Assay on Human, Murine and Rat Histamine H 4 Receptor Orthologs: Correlations and Discrepancies between Distal and Proximal Readouts

doi: 10.1371/journal.pone.0073961

Figure Lengend Snippet: Representative H 4 R-independent increase in the forskolin (1 µM) stimulated luciferase activity by ciproxyfan (CIP), proxyfan (PRO), JNJ 7777120 and thioperamide (THIO) in HEK293T-CRE-Luc cells, stably expressing the CRE-controlled luciferase and devoid of the H 4 R.

Article Snippet: The log (r - 1) values were plotted against the corresponding log [JNJ 7777120] values according to the Schild equation and analyzed by linear regression with GraphPad Prism 5.04.

Techniques: Luciferase, Activity Assay, Stable Transfection, Expressing

Concentration response curves of histamine (A) and clozapine (B) alone and in the presence of JNJ7777120 at increasing concentrations, determined on hH 4 R expressing HEK293T-CRE-Luc cells in the luciferase reporter gene assay, and corresponding Schild plots (C). The pA 2 values determined for JNJ 7777120 from Schild regression were 8.39 (slope: 0.83±0.02) and 8.17 (slope: 0.45±0.01) versus histamine and clozapine, respectively. Data points shown are the mean ± SEM of at least three (histamine) or five (clozapine) independent experiments performed in triplicate.

Journal: PLoS ONE

Article Title: Luciferase Reporter Gene Assay on Human, Murine and Rat Histamine H 4 Receptor Orthologs: Correlations and Discrepancies between Distal and Proximal Readouts

doi: 10.1371/journal.pone.0073961

Figure Lengend Snippet: Concentration response curves of histamine (A) and clozapine (B) alone and in the presence of JNJ7777120 at increasing concentrations, determined on hH 4 R expressing HEK293T-CRE-Luc cells in the luciferase reporter gene assay, and corresponding Schild plots (C). The pA 2 values determined for JNJ 7777120 from Schild regression were 8.39 (slope: 0.83±0.02) and 8.17 (slope: 0.45±0.01) versus histamine and clozapine, respectively. Data points shown are the mean ± SEM of at least three (histamine) or five (clozapine) independent experiments performed in triplicate.

Article Snippet: The log (r - 1) values were plotted against the corresponding log [JNJ 7777120] values according to the Schild equation and analyzed by linear regression with GraphPad Prism 5.04.

Techniques: Concentration Assay, Expressing, Luciferase, Reporter Gene Assay