Morphine, oxycodone and loperamide were purchased from Sigma-Aldrich and applied to the vascular chamber at 41 µg/ml (143.7 µM) Morphine, 10 µg/ml (31.7 µM) oxycodone, or 1.5 µg/ml (3.1 µM) loperamide. These concentrations were chosen as those closest to physiological that could still be reliably detected after transport [17 (link)]. Each drug was perfused through the vascular chamber for 24 h to establish equilibrium. Perfusion with drug was then continued over a 1 h period, with active sample collection from both the vascular and brain chambers (120 µl total from each compartment). Samples were stored at − 80 °C until processing for mass spectrometry analysis. Opioid transport was calculated as the amount of opioid detected in the brain chamber compared to the total amount of opioid delivered to the vascular chamber (percent of opioid transported across the BMEC monolayer).
Loperamide
Manufactured by Merck Group
Sourced in United States, Germany
Loperamide is a pharmaceutical laboratory product manufactured by Merck Group. It is a synthetic opioid compound used for various research and analytical applications.
Automatically generated - may contain errors
Lab products found in correlation
Sodium dihydrogen phosphate, by Merck Group (4 mentions)
Ethanol, by Merck Group (4 mentions)
Evans blue, by Merck Group (4 mentions)
Verapamil, by Merck Group (4 mentions)
Methanol, by Merck Group (3 mentions)
Bovine serum albumin (bsa), by Merck Group (3 mentions)
Acetylcholine, by Merck Group (3 mentions)
Papaverine, by Merck Group (3 mentions)
Caffeine, by Merck Group (3 mentions)
Magnesium chloride, by Merck Group (2 mentions)
Potassium dihydrogen phosphate, by Merck Group (2 mentions)
Potassium chloride (kcl), by Merck Group (2 mentions)
Sodium bicarbonate, by Merck Group (2 mentions)
2 hydroxypropyl β cyclodextrin, by Merck Group (2 mentions)
Castor oil, by Merck Group (2 mentions)
Trichloroacetic acid, by Merck Group (2 mentions)
Sulfasalazine, by Merck Group (2 mentions)
Vinblastine, by Merck Group (2 mentions)
Quinidine, by Merck Group (2 mentions)
Lucifer yellow, by Merck Group (2 mentions)
52 protocols using loperamide
1
Quantifying Opioid Transport Across BMEC
2
Vascular Smooth Muscle Contractility Assay
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All the chemicals used in this study have high purity with research-grade quality. Acetylcholine (Ach), aspirin, carbamylcholine chloride HCl, Carbachol (CCh), verapamil HCl, phenylephrine (PE) were purchased from Sigma Chemical Company, St. Louis, MO, USA. While Potassium dihydrogen phosphate, magnesium chloride, sodium bicarbonate, sodium chloride, magnesium sulfate, sodium dihydrogen phosphate, calcium chloride, potassium chloride, ethylenediaminetetraacetic acid (EDTA), glucose were purchased from Merck, Dermstadat Germany. Furthermore, loperamide, and dicyclomine were supplied by Sigma Chemical company, St. Louis, MO, USA).
3
Loperamide-Induced Diarrhea Model
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The drugs, chemicals, and instruments that were used in the present study were loperamide (Sigma Aldrich, Steinheim, Germany), magnesium sulfate (Sigma Aldrich), castor oil, methanol (BDH Chemicals, London, England), SS agar (Liofilchem, Roseto degli Abruzzi, Italy), and metabolic cages.
4
Loperamide Behavioral Assay Protocol
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Loperamide (Sigma-Aldrich, Milwaukee, WI, USA) was suspended in a
20% solution of 2-hydroxypropyl-β-cyclodextrin (Sigma-Aldrich) in
saline and diluted to the proper dose concentration. Loperamide injections
were made intraperitoneally (i.p.) at 0.4, 0.6, 0.8, or 1.2 mg/kg.
Behavioral assays started 60 min post injection [1 (link), 22 (link)].
20% solution of 2-hydroxypropyl-β-cyclodextrin (Sigma-Aldrich) in
saline and diluted to the proper dose concentration. Loperamide injections
were made intraperitoneally (i.p.) at 0.4, 0.6, 0.8, or 1.2 mg/kg.
Behavioral assays started 60 min post injection [1 (link), 22 (link)].
5
BBB Permeability Evaluation Protocol
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To assess BBB permeability, we used caffeine (CAF), carbamazepine (CBZ), desipramine (DES), loperamide (LPM), cetirizine (CET), vincristine (VIN), nefazodone (NZD), donepezil (DPZ), and simvastatin (SIM) (all from Sigma-Aldrich). LP533401 (LP) was synthesized by the Center for Medicinal Chemistry at the Korea Research Institute of Chemical Technology (KRICT).
6
Antioxidant and Anti-inflammatory Assay Protocol
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2,2′-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS); bovine
catalase; bovine serum albumin (BSA); butylated hydroxyl toluene (BHT); eosin;
epinephrine; Folin-Ciocalteu; hydrochloric acid (HCl); hematoxylin; hydrogen
peroxide (H2O2); mEthanol; paraffin; potassium dihydrogen
phosphate (KH2PO4); dipotassium hydrogen phosphate (K2HPO4); rutin; sodium
hydroxide (NaOH); sodium pentobarbital (C11H18N2O3); tannic acid;
2-thio-barbituric acid (TBA) and trichloroacetic acid (TCA) were purchased
products from Sigma Chemical Co. (Sigma-Aldrich GmbH, Steinheim, Germany).
Ethanol (EtOH); sulfasalazine; sodium chloride (NaCl); loperamide; and castor
oil were supplied by the Central Pharmacy of Tunisia. All other reagents used
were of analytical quality.
catalase; bovine serum albumin (BSA); butylated hydroxyl toluene (BHT); eosin;
epinephrine; Folin-Ciocalteu; hydrochloric acid (HCl); hematoxylin; hydrogen
peroxide (H2O2); mEthanol; paraffin; potassium dihydrogen
phosphate (KH2PO4); dipotassium hydrogen phosphate (K2HPO4); rutin; sodium
hydroxide (NaOH); sodium pentobarbital (C11H18N2O3); tannic acid;
2-thio-barbituric acid (TBA) and trichloroacetic acid (TCA) were purchased
products from Sigma Chemical Co. (Sigma-Aldrich GmbH, Steinheim, Germany).
Ethanol (EtOH); sulfasalazine; sodium chloride (NaCl); loperamide; and castor
oil were supplied by the Central Pharmacy of Tunisia. All other reagents used
were of analytical quality.
7
In Vitro Permeability Assay Using Caco-2 Cells and Mouse Liver Microsomes
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Paromomycin sulfate (Cat # P9297) was purchased from Sigma, Germany. Loperamide (Cat # L4762) was purchased from Sigma, Germany. Caco-2 cell line was procured from National Centre for Cell Science, Pune, India. Pooled mouse liver microsomes (MLMs) (Cat # 452220) were purchased from BD Gentest, MA, USA (B6C3F1– pool of ~ 100 mice, 9–10 weeks of age; Cat # 452220). Dulbecco's Modified Eagles medium (Cat # D5671), trypsin-EDTA solution (Cat # T4049) and Hank's buffered salt solution (HBSS) Buffer (Cat # H6648) were purchased from Sigma, Germany. Fetal Bovine Serum (Cat # 14-502F) was purchased from Lonza, Walkersville, MD, USA. Glasswares such as T-75 flasks and pipettes were procured from Grenier-Bio-one, Germany. Mill cell-24 well PET membrane 1 μm plates (Cat # PSRP010 R5) were from Millipore Corporation, Billerica MA.
8
Myricetin and Exendin 9-39 Protocol
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Myricetin (95%) was obtained from Acros Organics (Thermo Fisher, Geel, Belgium). Exendin 9–39 (Ex9), loperamide and naloxone and other chemicals or reagents were purchased from Sigma-Aldrich (St. Louis, MO, USA).
9
Jarrah Honey Alleviates Loperamide-Induced Constipation in Mice
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As shown in Figure 1a and Table 1 , mice were randomized into three groups (n = 10 for each group): the control group, the constipation group, and the honey group. After one‐week adaptive feeding, loperamide (Sigma) was used to induce slow‐transit constipation in mice. The constipation and honey groups were given loperamide at a dose of 5 mg/kg body weight, once per day (18:00) via oral gavage from day 1 to day 5. Mice in the honey group were given Jarrah honey (Elixir, TA (total activity) 45+ Eucalyptus marginata, purchased from Dalian aoxinbaiying International Trade Co., Ltd) suspended at a dose of 7.5 g/kg body weight in 0.2 ml PBS once a day (9:00) for 12 days, while the constipation group was administrated 0.2 ml of PBS as vehicle. The control group was given PBS by gavage twice a day (9:00 and 18:00) from day 1 to day 5, and once a day (9:00) from day 6 to day 12. Mortality, body weight, and fecal output were recorded daily. At 24 hr after final treatment, all animals were anesthetized before sacrifice. The gastrointestinal tract was removed and emptied of contents. The transverse colon, blood, and feces of mice were collected and immediately placed at −80°C until detection.
10
Pharmacological Modulation of Membrane Permeability
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The following were used in the experiments: Evans Blue (Sigma Aldrich, St. Louis, MO, USA), WIN 55,212-2 (Cayman Chemicals, Ann Arbor, MI, USA); CP 55,940 (Sigma Aldrich); bethanechol (Sigma Aldrich), loperamide (Sigma Aldrich), JZL184 (Cayman Chemicals).
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