Journal: PLoS Neglected Tropical Diseases

Article Title: Automated High-Content Assay for Compounds Selectively Toxic to Trypanosoma cruzi in a Myoblastic Cell Line

doi: 10.1371/journal.pntd.0003493

Figure Lengend Snippet: List of compounds used to validate the assay.

Article Snippet: Those compounds not available in GSK chemical collection were purchased from Sigma-Aldrich except the following: amiodarone (Pfizer), cloroxylenol derivative CX1 (Chembridge), dihydroergocristine mesylate (Tocris Bioscience), hydrazide derivative PCH1 (InterBioScreen), LP10 (ChemDiv), loperamide (Enamine), posaconazole ( Sheckchem.com ), pubchem 1473168 and pubchem 3812524 (Bionet), and terconazole (AKSCI-USA).

Techniques:

Journal: Neurogastroenterology and Motility

Article Title: Acacetin Alleviates Loperamide‐Induced Functional Constipation by Inhibiting P53 ‐Mediated Apoptosis in Colonic Epithelial Cells

doi: 10.1111/nmo.70298

Figure Lengend Snippet: Acacetin improves gastrointestinal motility in loperamide‐induced constipation model. A loperamide‐induced constipation model was established in mice, different doses of acacetin were administered to the mice by oral gavaging (YWL‐high: 50 mg/kg/day; YWL‐medium: 25 mg/kg/day; YWL‐low: 10 mg/kg/day). The following parameters were monitored in an activated charcoal test after fasting treatment. (A‐D) Defecation initiation time; Fecal pellet counts at 8 h; Fecal water content; and intestinal propulsion rates. (E) Small intestine length measurements. (F) Gastrointestinal transit rates determined by activated charcoal propulsion. N = 6 animals in each group. * p < 0.05; ** p < 0.01; *** p < 0.001; **** p < 0.0001.

Article Snippet: A loperamide‐induced functional constipation mouse model was established using oral gavaging of loperamide hydrochloride (HY‐B0418A, MedChemExpress, Shanghai, China) suspension [ , ].

Techniques:

Journal: Neurogastroenterology and Motility

Article Title: Acacetin Alleviates Loperamide‐Induced Functional Constipation by Inhibiting P53 ‐Mediated Apoptosis in Colonic Epithelial Cells

doi: 10.1111/nmo.70298

Figure Lengend Snippet: Loperamide activates P53 signaling and reduces AKT1 activation, inducing apoptosis in colonic mucosal epithelial cells. (A) Cell viability analysis after loperamide treatment by CCK‐8 assay in colonic mucosal epithelial cells. (B) TUNEL staining showing apoptotic cells after loperamide treatment. (C) Immunoblotting of cleaved caspase‐3 and Bax expression. (D) Immunoblotting of phosphorylated and total P53 and AKT1 proteins. N = 3 independent experiments. * p < 0.05; ** p < 0.01; *** p < 0.001; **** p < 0.0001.

Article Snippet: A loperamide‐induced functional constipation mouse model was established using oral gavaging of loperamide hydrochloride (HY‐B0418A, MedChemExpress, Shanghai, China) suspension [ , ].

Techniques: Activation Assay, CCK-8 Assay, TUNEL Assay, Staining, Western Blot, Expressing

Journal: Neurogastroenterology and Motility

Article Title: Acacetin Alleviates Loperamide‐Induced Functional Constipation by Inhibiting P53 ‐Mediated Apoptosis in Colonic Epithelial Cells

doi: 10.1111/nmo.70298

Figure Lengend Snippet: YWL extract and acacetin protect against loperamide‐induced apoptosis in colonic mucosal epithelial cells. (A) Cell viability after treatment with increasing doses of YWL extract. (B) Cell viability after treatment with increasing doses of acacetin. (C) Cell viability rescue by YWL extract and acacetin against loperamide‐induced toxicity. (D) TUNEL staining showing suppression of loperamide‐induced apoptosis by YWL and acacetin. (E) Immunoblots of cleaved caspase‐3 and Bax levels. (F) Immunoblots of phospho‐ and total P53 and AKT1 levels. (G) P53 transcriptional activity analysis. N = 3 independent experiments. * p < 0.05; ** p < 0.01; *** p < 0.001; **** p < 0.0001.

Article Snippet: A loperamide‐induced functional constipation mouse model was established using oral gavaging of loperamide hydrochloride (HY‐B0418A, MedChemExpress, Shanghai, China) suspension [ , ].

Techniques: TUNEL Assay, Staining, Western Blot, Activity Assay

Journal: Neurogastroenterology and Motility

Article Title: Acacetin Alleviates Loperamide‐Induced Functional Constipation by Inhibiting P53 ‐Mediated Apoptosis in Colonic Epithelial Cells

doi: 10.1111/nmo.70298

Figure Lengend Snippet: Activating P53 signaling abrogates the protection of acacetin against loperamide‐induced apoptosis. (A) P53 transcriptional activity analysis after Nutlin‐3a treatment. (B) Immunoblotting of phospho‐P53 and phospho‐AKT1 levels. (C) Cell viability analysis by CCK‐8 assay showing abrogation of the protective effect of acacetin by Nutlin‐3a. (D) TUNEL staining demonstrating Nutlin‐3a abolishes the suppression of acacetin on loperamide‐induced apoptosis. N = 3 independent experiments. * p < 0.05; ** p < 0.01; *** p < 0.001; **** p < 0.0001.

Article Snippet: A loperamide‐induced functional constipation mouse model was established using oral gavaging of loperamide hydrochloride (HY‐B0418A, MedChemExpress, Shanghai, China) suspension [ , ].

Techniques: Activity Assay, Western Blot, CCK-8 Assay, TUNEL Assay, Staining

Journal: The Journal of pharmacology and experimental therapeutics

Article Title: Central Nervous System Distribution of an Opioid Agonist Combination with Synergistic Activity.

doi: 10.1124/jpet.121.000821

Figure Lengend Snippet: Fig. 2. Potency of oral loperamide with and without coadministration with OMI in ICR mice. Peripherally mediated thermal nociceptive responses in the Hargreaves assay were assessed. Following CFA- induced inflammation in the hindpaw, subjects were given an oral gavage of loperamide (Lo), OMI, or combination, and postdrug nocicep- tive responses were taken 1 hour postadministration. Responses are reported as % antihyperalgesia, which was used to generate dose- response curves. The data were analyzed by nonlinear regression, fit- ting an [agonist] vs. response curve to compare ED50 values by Graph- Pad Prism 8.4.

Article Snippet: Loperamide hydrochloride and naltrindole hydrochloride were obtained from Tocris Bioscience (via Fisher Scientific).

Techniques:

Journal: International Journal of Medical Sciences

Article Title: Zuojin Pill enhances gastrointestinal motility by modulating the pacemaker potentials in interstitial cells of Cajal through multiple signaling pathways

doi: 10.7150/ijms.103507

Figure Lengend Snippet: ZJP enhances intestinal transit rate in wild type mice and restores normal intestinal transit rate in GMD model mice. (A-C) ZJP increased ITR in wild type mice (A), and restored normal ITR in AA-induced GMD mice (B) and STZ-induced GMD mice (C). Results are presented as mean ± SE. ****p < 0.0001 vs. untreated wild type group. ###p < 0.001 and ####p < 0.0001 vs. loperamide-treated and control groups. ZJP: Zuojin Pill. CTRL: Control. Lop: Loperamide. AA: Acetic acid. STZ: Streptozotocin.

Article Snippet: Thapsigargin (Cat. No. 1138), Y25130 (0380), RS39604 (0991), SB269970 (1612), xestospongin C (1280), PD98059 (1213), SB203580 (1402), SP600125 (1496), and loperamide (0840) were purchased from Tocris Bioscience (Bristol, United Kingdom), while methoctramine (104807-46-7), 4-DAMP (1952-15-4), guanosine 5'‐O‐(2‐thiodiphosphate) (GDP‐β‐S; 97952-36-8), U-73312 (112648-68-7), staurosporine (62996-74-1), go6976 (136194-77-9), and rottlerin (82-08-6) were obtained from Sigma‐Aldrich (St Louis, MO, USA).

Techniques: Control

Journal: Cell Communication and Signaling : CCS

Article Title: ER-phagy mediates the anti-tumoral synergism between HDAC inhibition and chemotherapy

doi: 10.1186/s12964-025-02198-9

Figure Lengend Snippet: The impact of HDACi/Gem on apoptosis and its link to clinical data. ( A ) Rel. mRNA expression of FAM134B and CHOP (mean of n=3 ± SD). Panc1 cells were treated with DMSO or the combination of 20 µM ISX and 1.0 µM Gem for different time periods. ( B ) Rel. mRNA expression of FAM134B and PERK (mean of n=3 ± SD). Panc1 cells were treated with DMSO, 20 µM ISX, 1.0 µM Gem, dual treatment (I/G), or 1.0 µM Thapsigargin (Th) in calcium-free or calcium-containing DMEM medium for 48h. ( C ) Flow cytometric quantification of IRE1 activity in Panc1 cells stably expressing an IRE1 reporter construct. Treatment as in ( B ) (n=3 ± SD). ( D ) Caspase 3/7 activity in Panc1 cells exposed to ISX (I, 20 µM) and Gem (G, 1.0 µM) for various time periods. Staurosporine (1.0 µM) was included as a positive control. The mean ± SD of two representative experiments measured in triplicates is shown. ( E ) Caspase 3/7 activity in Panc1 cells treated with the indicated drugs for 60h. ISX (I, 20 µM); Gem (G, 1.0 µM); IRE1-inh. 4µ8c (30µM); PERK-inh. ISRIB (1.0µM); ATF6-inh. Ceapin-A7 (6.0µM). Shown is the mean (± SD) of two representative experiments measured in quadruplicate each. Each dot represents one biological sample. ( F ) Western blot analysis of FAM134B protein levels in Panc1 cells treated for 48h with DMSO, 20 µM Loperamide, or 5/10 µM Nelfinavir. Shown is one representative experiment of n=5. β-Actin was used as a loading control. ( G , H , I ) FAM134B mRNA expression in bulk tissue from PDAC patients and corresponding healthy pancreatic tissue. Each dot represents one patient. ( J , K ) Kaplan-Meier plots representing the overall survival of patients with PDAC as a function of FAM134B expression (Scan-split; log-rank p). ( L ) Scheme illustrating the ER-phagy-induced mechanism by which HDACi and Gemcitabine synergize in their anti-tumor effectiveness

Article Snippet: The following chemicals were used: Ceapin-A7 (Sigma Aldrich/Merck, SML2330), Chidamide (Cayman Chemical Company, 13,686), Gemcitabine (Sigma Aldrich/Merck, G6423), Hygromycin B (Angene, AG00GAHS), Isoxazole 9 (ISX) (Biomol, 16,165), ISRIB (Sigma Aldrich/Merck, SML0843), Loperamide (LKT labs, L5660), Nelfinavir Mesylate (Cayman Chemical Company, 15,144), MS- 275 (AdipoGen Life Sciences, AG-CR1 - 0032), Puromycin dihydrochloride (PAA, P15 - 019), Staurosporine (Cayman Chemical Company, 81,590), 4μ8c (Cayman Chemical Company, 22,110), Thapsigargin (Cayman Chemical Company, AG-CN2 - 0003).

Techniques: Expressing, Activity Assay, Stable Transfection, Construct, Positive Control, Western Blot, Control

Journal:

Article Title: Competitive Substrates for P-Glycoprotein and Organic Anion Protein Transporters Differentially Reduce Blood Organ Transport of Fentanyl and Loperamide: Pharmacokinetics and Pharmacodynamics in Sprague Dawley Rats

doi: 10.1213/ane.0b013e31818e0bd1

Figure Lengend Snippet: The effect of verapamil on lung and brain partitioning of loperamide and fentanyl.

Article Snippet: Infusions Intravenous infusions of fentanyl citrate (5 min, 5.25 μg/kg/min) or loperamide hydrochloride (5 min, 0.95 mg/kg/min loperamide alone and 0.475mg/kg/min when administered with verapamil) were administered (Abbott Laboratories, North Chicago, IL).

Techniques:

Journal:

Article Title: Competitive Substrates for P-Glycoprotein and Organic Anion Protein Transporters Differentially Reduce Blood Organ Transport of Fentanyl and Loperamide: Pharmacokinetics and Pharmacodynamics in Sprague Dawley Rats

doi: 10.1213/ane.0b013e31818e0bd1

Figure Lengend Snippet: Loperamide (A–C) and fentanyl (D–F) concentration in Sprague-Dawley rats’ arterial plasma (A, D), lung (B, E), and brain (C, F) in the absence and presence of verapamil (n = 4 per time point per protocol). The symbols represent measured drug concentrations, whereas the lines represent drug concentrations predicted by the model: Solid line – modeled opioid only, dashed line – modeled opioid with verapamil, circles – measured opioid only, upright triangles – measured opioid with verapamil.

Article Snippet: Infusions Intravenous infusions of fentanyl citrate (5 min, 5.25 μg/kg/min) or loperamide hydrochloride (5 min, 0.95 mg/kg/min loperamide alone and 0.475mg/kg/min when administered with verapamil) were administered (Abbott Laboratories, North Chicago, IL).

Techniques: Concentration Assay, Clinical Proteomics

Journal:

Article Title: Competitive Substrates for P-Glycoprotein and Organic Anion Protein Transporters Differentially Reduce Blood Organ Transport of Fentanyl and Loperamide: Pharmacokinetics and Pharmacodynamics in Sprague Dawley Rats

doi: 10.1213/ane.0b013e31818e0bd1

Figure Lengend Snippet: The effect of loperamide and fentanyl on lung and brain partitioning of verapamil.

Article Snippet: Infusions Intravenous infusions of fentanyl citrate (5 min, 5.25 μg/kg/min) or loperamide hydrochloride (5 min, 0.95 mg/kg/min loperamide alone and 0.475mg/kg/min when administered with verapamil) were administered (Abbott Laboratories, North Chicago, IL).

Techniques:

Journal:

Article Title: Competitive Substrates for P-Glycoprotein and Organic Anion Protein Transporters Differentially Reduce Blood Organ Transport of Fentanyl and Loperamide: Pharmacokinetics and Pharmacodynamics in Sprague Dawley Rats

doi: 10.1213/ane.0b013e31818e0bd1

Figure Lengend Snippet: Fentanyl (A,B) and loperamide (C,D) concentrations in arterial plasma and the delta wave electroencephalogram (EEG) response in the absence (A,C) and presence of loperamide (B,D) in Sprague-Dawley rats (n = 4 per time point in pk studies, each animal (n = 4) was studied with pharmacokinetics (pk) drug and its competitive inhibitor except for n=3 for loperamide alone for EEG studies). Data presented as mean ± S.E.M.

Article Snippet: Infusions Intravenous infusions of fentanyl citrate (5 min, 5.25 μg/kg/min) or loperamide hydrochloride (5 min, 0.95 mg/kg/min loperamide alone and 0.475mg/kg/min when administered with verapamil) were administered (Abbott Laboratories, North Chicago, IL).

Techniques: Clinical Proteomics, Drug discovery

Journal:

Article Title: Competitive Substrates for P-Glycoprotein and Organic Anion Protein Transporters Differentially Reduce Blood Organ Transport of Fentanyl and Loperamide: Pharmacokinetics and Pharmacodynamics in Sprague Dawley Rats

doi: 10.1213/ane.0b013e31818e0bd1

Figure Lengend Snippet: Fentanyl and loperamide concentrations at 50% maximum electroencephalogram effect.

Article Snippet: Infusions Intravenous infusions of fentanyl citrate (5 min, 5.25 μg/kg/min) or loperamide hydrochloride (5 min, 0.95 mg/kg/min loperamide alone and 0.475mg/kg/min when administered with verapamil) were administered (Abbott Laboratories, North Chicago, IL).

Techniques: