loperamide and n-demethylloperamide

loperamide has been researched along with n-demethylloperamide in 22 studies

Research

Studies (22)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (31.82)29.6817
2010's14 (63.64)24.3611
2020's1 (4.55)2.80

Authors

AuthorsStudies
Bao, JQ; Bedwell, DW; Higgins, JW; Zamek-Gliszczynski, MJ1
Kang, J; Luo, Y; Rampe, D; Vaz, RJ1
Erve, JC; Hachey, DL; He, H; Sadeque, A; Wood, AJ1
Kalgutkar, AS; Nguyen, HT1
Allan, C; Fowler, D; Levine, B; Moore, KA; Sklerov, J1
Backman, JT; Fredrikson, H; Neuvonen, PJ; Niemi, M; Pasanen, MK; Tornio, A1
Gladding, RL; Hong, J; Innis, RB; Lazarova, N; Liow, JS; Pike, VW; Seneca, N; Taku, A; Tuan, E; Zoghbi, SS1
Gladding, RL; Herscovitch, P; Innis, RB; Kreisl, W; Lazarova, N; Liow, JS; Pike, VW; Seneca, N; Taku, A; Zoghbi, SS1
Gladding, RL; Herscovitch, P; Innis, RB; Jenko, K; Kreisl, W; Liow, JS; Pike, VW; Seneca, N; Taku, A; Zoghbi, SS1
Brimacombe, KR; Gottesman, MM; Hall, MD; Halldin, C; Innis, RB; Kannan, P; Liow, JS; Morse, C; Pike, VW; Taku, AK; Zoghbi, SS1
Herscovitch, P; Innis, RB; Kimura, N; Kreisl, WC; Liow, JS; Morse, CL; Pike, VW; Seneca, N; Zoghbi, SS1
Brimacombe, KR; Gottesman, MM; Hall, MD; Halldin, C; Innis, RB; Kannan, P; Kreisl, WC; Liow, JS; Pike, VW; Telu, S; Zhang, Y; Zoghbi, SS1
Boon, P; De Vos, F; Moerman, L; Raedt, R; Slaets, D; Wyffels, L1
Boon, P; De Vos, F; Dumolyn, C; Moerman, L1
Amano, N; Hirabayashi, H; Moriwaki, T; Sugimoto, H1
Bae, SA; Chong, DJ; Easwaramoorthy, B; Farwell, MD; Ichise, M; Iida, Y1
Gao, M; Wang, M; Zheng, QH1
Bhatia, R; Innis, RB; Kreisl, WC; Morse, CL; Pike, VW; Shetty, HU; Woock, AE; Zoghbi, SS1
Bauer, F; Erker, T; Filip, T; Kuntner, C; Langer, O; Löscher, W; Mairinger, S; Müller, M; Pahnke, J; Römermann, K; Sauberer, M; Stanek, J; Traxl, A; Wanek, T1
Auvity, S; Damont, A; Goutal, S; Kuhnast, B; Saba, W; Tournier, N; Valette, H1
Bhatti, Z; Norsworthy, J; Szombathy, T1
Anoshchenko, O; Storelli, F; Unadkat, JD1

Trials

3 trial(s) available for loperamide and n-demethylloperamide

ArticleYear
Itraconazole, gemfibrozil and their combination markedly raise the plasma concentrations of loperamide.
    European journal of clinical pharmacology, 2006, Volume: 62, Issue:6

    Topics: Adult; Aryl Hydrocarbon Hydroxylases; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Availability; Central Nervous System; Cross-Over Studies; Cytochrome P-450 CYP2C8; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Drug Interactions; Enzyme Inhibitors; Female; Gemfibrozil; Humans; Itraconazole; Loperamide; Male

2006
P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide.
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2010, Volume: 51, Issue:4

    Topics: Adult; ATP Binding Cassette Transporter, Subfamily B; Biological Transport; Blood-Brain Barrier; Cerebrovascular Circulation; Dose-Response Relationship, Drug; Drug-Related Side Effects and Adverse Reactions; Female; Humans; Kinetics; Loperamide; Magnetic Resonance Imaging; Male; Positron-Emission Tomography; Quinolines; Radioactive Tracers

2010
Increased permeability-glycoprotein inhibition at the human blood-brain barrier can be safely achieved by performing PET during peak plasma concentrations of tariquidar.
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2015, Volume: 56, Issue:1

    Topics: Administration, Intravenous; Administration, Oral; Adult; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Blood-Brain Barrier; Dose-Response Relationship, Drug; Female; Humans; Loperamide; Male; Permeability; Positron-Emission Tomography; Quinolines; Safety

2015

Other Studies

19 other study(ies) available for loperamide and n-demethylloperamide

ArticleYear
Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:9

    Topics: Administration, Oral; Animals; Area Under Curve; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Availability; Biotransformation; Brain; Fluoresceins; Gene Knockout Techniques; Genotype; Half-Life; Loperamide; Male; Metabolic Clearance Rate; Paclitaxel; Phenotype; Rats; Rats, Sprague-Dawley; Rats, Transgenic; Rats, Wistar; Sulfasalazine; Tissue Distribution

2012
Molecular determinants of loperamide and N-desmethyl loperamide binding in the hERG cardiac K
    Bioorganic & medicinal chemistry letters, 2018, 02-01, Volume: 28, Issue:3

    Topics: Dose-Response Relationship, Drug; ERG1 Potassium Channel; Humans; Loperamide; Models, Molecular; Molecular Structure; Potassium Channel Blockers; Structure-Activity Relationship

2018
Quantitation of loperamide and N-demethyl-loperamide in human plasma using electrospray ionization with selected reaction ion monitoring liquid chromatography-mass spectrometry.
    Journal of chromatography. B, Biomedical sciences and applications, 2000, Jul-21, Volume: 744, Issue:2

    Topics: Adult; Calibration; Chromatography, High Pressure Liquid; Humans; Loperamide; Reproducibility of Results; Sensitivity and Specificity; Spectrometry, Mass, Electrospray Ionization

2000
Identification of an N-methyl-4-phenylpyridinium-like metabolite of the antidiarrheal agent loperamide in human liver microsomes: underlying reason(s) for the lack of neurotoxicity despite the bioactivation event.
    Drug metabolism and disposition: the biological fate of chemicals, 2004, Volume: 32, Issue:9

    Topics: 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; 1-Methyl-4-phenylpyridinium; Animals; Antidiarrheals; Bupropion; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme System; Dealkylation; Haloperidol; Humans; Hydroxylation; Ketoconazole; Loperamide; Male; Microsomes, Liver; NADP; Neurons; Pyridinium Compounds; Rats; Rats, Sprague-Dawley; Time Factors

2004
Tissue distribution of loperamide and N-desmethylloperamide following a fatal overdose.
    Journal of analytical toxicology, 2005, Volume: 29, Issue:7

    Topics: Adult; Antidiarrheals; Chromatography, High Pressure Liquid; Drug Overdose; Fatal Outcome; Forensic Pathology; Humans; Loperamide; Male; Tissue Distribution

2005
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.
    Journal of medicinal chemistry, 2008, Oct-09, Volume: 51, Issue:19

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; Brain; Carbon Radioisotopes; Injections, Intravenous; Loperamide; Macaca mulatta; Male; Mice; Mice, Knockout; Molecular Structure; Positron-Emission Tomography; Radiopharmaceuticals; Stereoisomerism; Time Factors

2008
P-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeys.
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2009, Volume: 50, Issue:1

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Humans; Loperamide; Macaca mulatta; Male; Positron-Emission Tomography; Radioactivity; Regional Blood Flow; Tissue Distribution

2009
Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoprotein.
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2009, Volume: 50, Issue:5

    Topics: Adult; ATP Binding Cassette Transporter, Subfamily B, Member 1; Body Burden; Brain; Female; Humans; Loperamide; Male; Metabolic Clearance Rate; Organ Specificity; Positron-Emission Tomography; Radiation Dosage; Radiometry; Radiopharmaceuticals; Tissue Distribution

2009
N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrier.
    Drug metabolism and disposition: the biological fate of chemicals, 2010, Volume: 38, Issue:6

    Topics: Animals; Anti-HIV Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP-Binding Cassette Transporters; Biological Transport; Blood-Brain Barrier; Brain; Cerebrovascular Circulation; Glycoproteins; Humans; Loperamide; Mice; Multidrug Resistance-Associated Proteins; Radiopharmaceuticals; Tissue Distribution; Tumor Cells, Cultured

2010
Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET.
    Proceedings of the National Academy of Sciences of the United States of America, 2011, Feb-08, Volume: 108, Issue:6

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Cell Line, Tumor; Humans; Isotope Labeling; Loperamide; Lysosomes; Mice; Positron-Emission Tomography; Quinolines; Radiography; Tritium

2011
Antiepileptic drugs modulate P-glycoproteins in the brain: a mice study with (11)C-desmethylloperamide.
    Epilepsy research, 2011, Volume: 94, Issue:1-2

    Topics: Analysis of Variance; Animals; Anticonvulsants; ATP Binding Cassette Transporter, Subfamily B; Blood-Brain Barrier; Brain; Carbon Isotopes; Dose-Response Relationship, Drug; Drug Interactions; Loperamide; Male; Mice; Mice, Knockout; Radioligand Assay; Radionuclide Imaging; Time Factors

2011
The influence of mass of [11C]-laniquidar and [11C]-N-desmethyl-loperamide on P-glycoprotein blockage at the blood-brain barrier.
    Nuclear medicine and biology, 2012, Volume: 39, Issue:1

    Topics: Animals; Antidiarrheals; ATP Binding Cassette Transporter, Subfamily B; Benzazepines; Biological Transport; Blood-Brain Barrier; Brain; Carbon Radioisotopes; Case-Control Studies; Drug Carriers; Loperamide; Male; Mice; Mice, Knockout; Quinolines; Tissue Distribution

2012
Retrospective analysis of P-glycoprotein-mediated drug-drug interactions at the blood-brain barrier in humans.
    Drug metabolism and disposition: the biological fate of chemicals, 2013, Volume: 41, Issue:4

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Drug Interactions; Humans; LLC-PK1 Cells; Loperamide; Quinolines; Swine; Verapamil

2013
Imaging P-glycoprotein function in rats using [(11)C]-N-desmethyl-loperamide.
    Annals of nuclear medicine, 2013, Volume: 27, Issue:7

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; Brain; Cyclosporine; Kinetics; Loperamide; Male; Positron-Emission Tomography; Quinolines; Rats; Rats, Sprague-Dawley

2013
A high-yield route to synthesize the P-glycoprotein radioligand [11C]N-desmethyl-loperamide and its parent radioligand [11C]loperamide.
    Bioorganic & medicinal chemistry letters, 2013, Oct-01, Volume: 23, Issue:19

    Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Carbon Radioisotopes; Chromatography, High Pressure Liquid; Ligands; Loperamide; Molecular Structure; Radiopharmaceuticals; Solid Phase Extraction

2013
Factors Governing P-Glycoprotein-Mediated Drug-Drug Interactions at the Blood-Brain Barrier Measured with Positron Emission Tomography.
    Molecular pharmaceutics, 2015, Sep-08, Volume: 12, Issue:9

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP-Binding Cassette Transporters; Biological Transport; Blood-Brain Barrier; Brain; Calcium Channel Blockers; Carbon Radioisotopes; Drug Interactions; Female; Humans; Loperamide; Mice; Mice, Inbred C57BL; Mice, Knockout; Positron-Emission Tomography; Radiopharmaceuticals; Verapamil

2015
Imaging the impact of cyclosporin A and dipyridamole on P-glycoprotein (ABCB1) function at the blood-brain barrier: A [(11)C]-N-desmethyl-loperamide PET study in nonhuman primates.
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2016, Aug-25, Volume: 91

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Carbon Radioisotopes; Cyclosporine; Dipyridamole; Loperamide; Male; Papio; Positron-Emission Tomography

2016
Loperamide metabolite-induced cardiomyopathy and QTc prolongation.
    Clinical toxicology (Philadelphia, Pa.), 2017, Volume: 55, Issue:7

    Topics: Adult; Antidiarrheals; Biotransformation; Cardiomyopathies; Drug Overdose; Electrocardiography; Female; Humans; Long QT Syndrome; Loperamide; Predictive Value of Tests; Suicide, Attempted

2017
Successful Prediction of Human Steady-State Unbound Brain-to-Plasma Concentration Ratio of P-gp Substrates Using the Proteomics-Informed Relative Expression Factor Approach.
    Clinical pharmacology and therapeutics, 2021, Volume: 110, Issue:2

    Topics: Algorithms; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Brain; Brain Chemistry; Dogs; Endothelial Cells; Extracellular Fluid; Forecasting; Gene Expression Regulation; Humans; Loperamide; Madin Darby Canine Kidney Cells; Metoclopramide; Positron-Emission Tomography; Proteomics; Verapamil

2021