flibanserin  (MedChemExpress)

Journal: Archives of biochemistry and biophysics

Article Title: Identifying novel aryl hydrocarbon receptor (AhR) modulators from clinically approved drugs: In silico screening and In vitro validation.

doi: 10.1016/j.abb.2024.109958

Figure Lengend Snippet: Fig. 5. Evolutions of structural properties of complex via RMSD over time (200ns) in of AhR ligands. A) stability of bound complexes with flibanserin, butoconazol, luliconazole, naftifine, and triclabendazole in presence of PAS-B alone. B) stability of bound complexes with rosiglitazone, empagliflozin, benperidol, nebivolol, and zucapsaicin.

Article Snippet: Flibanserin (S3716), naftifine HCl (S3156), zucapsaicin (S6409), triclabendazole (S4114), empagliflozin (S8022), butoconazole (S5359), and luliconazole (S4258) were purchased from Selleck Chemicals (Houston, TX, USA).

Techniques:

Journal: Archives of biochemistry and biophysics

Article Title: Identifying novel aryl hydrocarbon receptor (AhR) modulators from clinically approved drugs: In silico screening and In vitro validation.

doi: 10.1016/j.abb.2024.109958

Figure Lengend Snippet: Fig. 4. Evolutions of structural properties of the ligand heavy atoms via RMSD over time (200ns). A) stability of flibanserin, butoconazol, luliconazole, naftifine, and triclabendazole in presence of PAS-B alone. B) stability of rosiglitazone, empagliflozin, benperidol, nebivolol, and zucapsaicin.

Article Snippet: Flibanserin (S3716), naftifine HCl (S3156), zucapsaicin (S6409), triclabendazole (S4114), empagliflozin (S8022), butoconazole (S5359), and luliconazole (S4258) were purchased from Selleck Chemicals (Houston, TX, USA).

Techniques:

Journal: Archives of biochemistry and biophysics

Article Title: Identifying novel aryl hydrocarbon receptor (AhR) modulators from clinically approved drugs: In silico screening and In vitro validation.

doi: 10.1016/j.abb.2024.109958

Figure Lengend Snippet: Fig. 7. mode of binding from predominate cluster for each drug A) Flibanserin, B) Zucapsaicin, C) Rosiglitazone, D) Triclabendazole, E) Butoconazole, F) Benperidol, G) Naftifine, H) Nebivolol, I) Empagliflozin, and J) Luliconazole.

Article Snippet: Flibanserin (S3716), naftifine HCl (S3156), zucapsaicin (S6409), triclabendazole (S4114), empagliflozin (S8022), butoconazole (S5359), and luliconazole (S4258) were purchased from Selleck Chemicals (Houston, TX, USA).

Techniques: Binding Assay

Journal: Archives of biochemistry and biophysics

Article Title: Identifying novel aryl hydrocarbon receptor (AhR) modulators from clinically approved drugs: In silico screening and In vitro validation.

doi: 10.1016/j.abb.2024.109958

Figure Lengend Snippet: Fig. 6. Beta factor per residue backbone atoms over 200 ns MD trajectory in present of unbound protein (PAS-B) as reference and bound protein to ten selected drugs. A) Flibanserin, butoconazol, luliconazole, naftifine, and triclabendazole in presence of PAS-B alone. B) Rosiglitazone, empagliflozin, benperidol, nebivolol, and zucapsaicin.

Article Snippet: Flibanserin (S3716), naftifine HCl (S3156), zucapsaicin (S6409), triclabendazole (S4114), empagliflozin (S8022), butoconazole (S5359), and luliconazole (S4258) were purchased from Selleck Chemicals (Houston, TX, USA).

Techniques: Residue

Journal: Pharmaceuticals

Article Title: Cardioprotective Effect of Flibanserin against Isoproterenol-Induced Myocardial Infarction in Female Rats: Role of Cardiac 5-HT2A Receptor Gene/5-HT/Ca 2+ Pathway

doi: 10.3390/ph16040502

Figure Lengend Snippet: The ECG examination in different treated groups. ( a ): The electrocardiographic effect of FLP in different doses on ISO-induced MI in rats. ( b ): ECG in experimental rats pretreated with FLP (15, 30, and 45 mg/kg) in an ISO-induced MI model on HR, QT interval, R amplitude, and ST segment amplitude. ( A ) Normal group, ( B ) Iso group, ( C ) FLB 15 mg + Iso group, ( D ) FLB 30 mg + Iso group and FLB 45 mg + Iso group. Bars with different letters are significantly different according to DMRT at p < 0.001 level ( n = 5). Data are expressed as Mean ± SD. ECG = electrocardiogram, FLP = flibanserin, ISO = isoproterenol, MI = myocardial infarction, HR = heart rate, DMRT = Duncan’s multiple range test.

Article Snippet: Flibanserin was purchased from Rameda (Giza, Egypt) and was suspended in water.

Techniques:

Journal: Pharmaceuticals

Article Title: Cardioprotective Effect of Flibanserin against Isoproterenol-Induced Myocardial Infarction in Female Rats: Role of Cardiac 5-HT2A Receptor Gene/5-HT/Ca 2+ Pathway

doi: 10.3390/ph16040502

Figure Lengend Snippet: Histopathological examination in the different treated groups. ( A ): Photomicrograph for specimens from the heart stained with H&E 10× & 40× in different treated groups. In the normal group: [H&E 10×] shows Compact, uniformly arranged myocardial fibers (Black arrows), [H&E 40×] myocytes show preserved uniform nuclei (Black arrows) and cytoplasmic cross striation (Red arrows). In ISO group: [H&E 10×] shows a wide separation of myocardial fibers due to interstitial edema (Black arrows), areas of myocardial fibers loss of eosinophilic staining and becoming pallor in appearance (Arrowheads), the influx of inflammatory cells into myocardial fibers (Red arrows), [H&E 40×] shows pathological changes of MI, interstitial edema between myocardial fibers (Black arrows), loss of cytoplasmic striation of myocytes with shrinkage of nuclei and prominence of the cell membrane (Arrowheads), some myocytes show an absence of nuclei (Yellow arrows), the influx of macrophages, indicating an inflammatory response to remove dead fibers (Red arrows). In FLP (15 mg/kg) + ISO group: [H&E 10×] shows no significant difference when compared to the ISO group as there is still a wide separation of myocardial fibers due to interstitial edema (Black arrows), the influx of inflammatory cells into myocardial fibers (Red arrows), [H&E 40×] shows persistent pathological changes of MI, interstitial edema between myocardial fibers (Black arrows), loss of cytoplasmic striation of myocytes with shrinkage of nuclei and prominence of the cell membrane (Arrowheads), some myocytes show an absence of nuclei (Yellow arrows), the influx of macrophages indicating an inflammatory response to remove dead fibers (Red arrows). In FLP (30 mg/kg) + ISO group: [H&E 10×] still shows interstitial edema (Black arrows); however, a slight reduction in inflammatory cell influx is noticed (Red arrow), [H&E 40×] shows persistent pathological changes of MI, yet to a milder degree: interstitial edema between myocardial fibers (Black arrows), loss of cytoplasmic striation of few myocytes with shrinkage of nuclei and prominence of the cell membrane (Arrowheads), absence of nuclei in few myocytes (Yellow arrows), reduction in macrophages influx (Red arrows). In FLP (45 mg/kg) + ISO group: [H&E 10×] shows compact uniformly arranged myocardial fibers and absence of interstitial edema (Black arrows); few areas of chronic inflammatory cells are seen (Red arrow), [H&E 40×] myocytes show uniform nuclei and eosinophilic cytoplasm (Black arrows), few macrophages are seen (Red arrows). ( B ): histopathologic score in experimental rats pretreated with FLP (15, 30, and 45 mg/kg) in an ISO-induced MI model. Data were analyzed using Kruskal-Wallis followed by Dunn’s test for multiple comparisons against the normal group at p < 0.05., ** p < 0.01, *** p < 0.001, n = 6. H&E = hematoxylin and eosin, FLP = flibanserin, ISO = isoproterenol, MI = myocardial infarction.

Article Snippet: Flibanserin was purchased from Rameda (Giza, Egypt) and was suspended in water.

Techniques: Staining, Membrane

Journal: Pharmaceuticals

Article Title: Cardioprotective Effect of Flibanserin against Isoproterenol-Induced Myocardial Infarction in Female Rats: Role of Cardiac 5-HT2A Receptor Gene/5-HT/Ca 2+ Pathway

doi: 10.3390/ph16040502

Figure Lengend Snippet: Serum cardiac enzymes levels in experimental rats pretreated with FLP (15, 30, and 45 mg/kg) in an ISO-induced MI model ( A ): The cardiac serum level of Tnl ( B ): The cardiac serum level of CK-MB, ( C ): The cardiac serum level of LDH. ( D ): The cardiac serum level of CK. Bars with different letters are significantly different according to DMRT at p < 0.001 level ( n = 5). Data are expressed as Mean ± SD. FLP = flibanserin, ISO = isoproterenol, MI = myocardial infarction, Tnl = troponin I, CK-MB = creatinine kinase-MB, LDH = lactate dehydrogenase, CK = creatine kinase, DMRT = Duncan’s multiple range test.

Article Snippet: Flibanserin was purchased from Rameda (Giza, Egypt) and was suspended in water.

Techniques:

Journal: Pharmaceuticals

Article Title: Cardioprotective Effect of Flibanserin against Isoproterenol-Induced Myocardial Infarction in Female Rats: Role of Cardiac 5-HT2A Receptor Gene/5-HT/Ca 2+ Pathway

doi: 10.3390/ph16040502

Figure Lengend Snippet: Effect of FLP in different doses on heart tissue level of GSH and MDA. ( A ): Heart level of GSH in experimental rats pretreated with FLP (15, 30, and 45 mg/kg) in an ISO-induced MI model. ( B ) Heart level of MDA in experimental rats pretreated with FLP (15, 30, and 45 mg/kg) in an ISO-induced MI model. Bars with different letters are significantly different according to DMRT at p < 0.001 level ( n = 5). Data are expressed as Mean ± SD. FLP = flibanserin, GSH = reduced glutathione, MDA = malondialdehyde, ISO = isoproterenol, DMRT = Duncan’s multiple range test.

Article Snippet: Flibanserin was purchased from Rameda (Giza, Egypt) and was suspended in water.

Techniques:

Journal: Pharmaceuticals

Article Title: Cardioprotective Effect of Flibanserin against Isoproterenol-Induced Myocardial Infarction in Female Rats: Role of Cardiac 5-HT2A Receptor Gene/5-HT/Ca 2+ Pathway

doi: 10.3390/ph16040502

Figure Lengend Snippet: Proposed FLP action on DA, NE, and 5-HT centers of the brain. The figure represents the dopaminergic system ( A ) before and ( B ) after the administration of flibanserin. While noradrenergic system ( C ) before and ( D ) after administration of flibanserin. Finally, serotonergic system ( E ) before and ( F ) after administration of flibanserin. Glu = Glutamate, GABA = Gamma-aminobutyric acid, NE = Norepinephrine, DA = Dopamine, 5-HT = Serotonin, FLP = Flibanserin.

Article Snippet: Flibanserin was purchased from Rameda (Giza, Egypt) and was suspended in water.

Techniques:

Journal: Pharmaceutics

Article Title: Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment

doi: 10.3390/pharmaceutics14122627

Figure Lengend Snippet: Diagnostic plots for particle size of FLB-SPLs. ( A ) Normal probability plot; ( B ) predicted vs. actual values plot; ( C ) studentized residuals vs. predicted values plot; ( D ) externally studentized residuals vs. run number plot. Abbreviations: FLB, flibanserin; SPL, spanlastics.

Article Snippet: The active ingredient of flibanserin was procured from Qingdao-Sigma Chemical Co., Ltd. (Qingdao, China).

Techniques: Diagnostic Assay

Journal: Pharmaceutics

Article Title: Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment

doi: 10.3390/pharmaceutics14122627

Figure Lengend Snippet: Diagnostic plots for zeta potential of FLB-SPLs. ( A ) Normal probability plot; ( B ) predicted vs. actual values plot; ( C ) studentized residuals vs. predicted values plot; ( D ) externally studentized residuals vs. run number plot. Abbreviations: FLB, flibanserin; SPL, spanlastics.

Article Snippet: The active ingredient of flibanserin was procured from Qingdao-Sigma Chemical Co., Ltd. (Qingdao, China).

Techniques: Diagnostic Assay

Journal: Pharmaceutics

Article Title: Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment

doi: 10.3390/pharmaceutics14122627

Figure Lengend Snippet: Linear plots showing individual effects on FLB-SPLs’ size. ( A ) Span: EA ratio; ( B ) ST; ( C ) EA type. Abbreviations: FLB, flibanserin; SPL, spanlastics; EA, edge activator; ST, sonication time; PVA, polyvinyl alcohol; SDC, sodium deoxycholate; TPGS, D-α-tocopheryl polyethylene glycol succinate.

Article Snippet: The active ingredient of flibanserin was procured from Qingdao-Sigma Chemical Co., Ltd. (Qingdao, China).

Techniques: Sonication

Journal: Pharmaceutics

Article Title: Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment

doi: 10.3390/pharmaceutics14122627

Figure Lengend Snippet: Linear plots showing individual effects on FLB-SPLs’ zeta potential. ( A ) Span: EA ratio, ( B ) ST; ( C ) EA type. Abbreviations: FLB, flibanserin; SPL, spanlastics; EA, edge activator; ST, sonication time; PVA, polyvinyl alcohol; SDC, sodium deoxycholate; TPGS, D-α-tocopheryl polyethylene glycol succinate.

Article Snippet: The active ingredient of flibanserin was procured from Qingdao-Sigma Chemical Co., Ltd. (Qingdao, China).

Techniques: Sonication

Journal: Pharmaceutics

Article Title: Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment

doi: 10.3390/pharmaceutics14122627

Figure Lengend Snippet: ( A ) Ramp graphs for the optimized variable levels and predicted responses of the optimized FLB-SPLs; ( B ) bar graph for the desirability of the optimization process. Abbreviations: FLB, flibanserin; SPL, spanlastics; EA, edge activator; ST, sonication time; PVA, polyvinyl alcohol; SDC, sodium deoxycholate; TPGS, D-α-tocopheryl polyethylene glycol succinate; PS, particle size; ZP, zeta potential.

Article Snippet: The active ingredient of flibanserin was procured from Qingdao-Sigma Chemical Co., Ltd. (Qingdao, China).

Techniques: Sonication

Journal: Pharmaceutics

Article Title: Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment

doi: 10.3390/pharmaceutics14122627

Figure Lengend Snippet: Mean ( A ) plasma concentrations; ( B ) brain concentrations vs. time of FLB after nasal administration of optimized FLB-SPLs compared to raw FLB in rats at a dose of 10 mg/kg. (Results presented as mean ± SD, n = 3). Abbreviations: FLB, flibanserin; SPL, spanlastics.

Article Snippet: The active ingredient of flibanserin was procured from Qingdao-Sigma Chemical Co., Ltd. (Qingdao, China).

Techniques: