Page last updated: 2024-09-04

tariquidar and loperamide

tariquidar has been researched along with loperamide in 13 studies

Compound Research Comparison

Studies
(tariquidar)
Trials
(tariquidar)
Recent Studies (post-2010)
(tariquidar)
Studies
(loperamide)
Trials
(loperamide)
Recent Studies (post-2010) (loperamide)
210161381,358196488

Protein Interaction Comparison

ProteinTaxonomytariquidar (IC50)loperamide (IC50)
Cocaine esteraseHomo sapiens (human)5.7
Beta-2 adrenergic receptorHomo sapiens (human)3.005
ATP-dependent translocase ABCB1Homo sapiens (human)2.5
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 29.27
Cytochrome P450 2D6Homo sapiens (human)2
Histamine H2 receptorHomo sapiens (human)3.081
Sodium-dependent serotonin transporterHomo sapiens (human)2.202
Mu-type opioid receptorHomo sapiens (human)0.0014
D(3) dopamine receptorHomo sapiens (human)1.337
Delta-type opioid receptorHomo sapiens (human)0.896
Kappa-type opioid receptorHomo sapiens (human)3.125
5-hydroxytryptamine receptor 2BHomo sapiens (human)4.105
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)0.033
Sodium channel protein type 5 subunit alphaHomo sapiens (human)0.239
Sigma non-opioid intracellular receptor 1Homo sapiens (human)0.628

Research

Studies (13)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (15.38)29.6817
2010's11 (84.62)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Benet, LZ; Brouwer, KL; Chu, X; Dahlin, A; Evers, R; Fischer, V; Giacomini, KM; Hillgren, KM; Hoffmaster, KA; Huang, SM; Ishikawa, T; Keppler, D; Kim, RB; Lee, CA; Niemi, M; Polli, JW; Sugiyama, Y; Swaan, PW; Tweedie, DJ; Ware, JA; Wright, SH; Yee, SW; Zamek-Gliszczynski, MJ; Zhang, L1
Choo, EF; Glaeser, H; Higginbotham, JN; Kim, RB; Kurnik, D; Muszkat, M; Ohkubo, T; Shay, SD; Wilkinson, GR; Wood, AJ1
Donahue, JP; Kurnik, D; Muszkat, M; Nair, UB; Sofowora, GG; Wilkinson, GR; Wood, AJ1
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
Butelman, ER; Caspers, M; Kreek, MJ; Lovell, KM; Prisinzano, TE1
Li, H; Shen, GL; Sun, HX; Yuan, M; Zhuang, XM1
Amano, N; Hirabayashi, H; Moriwaki, T; Sugimoto, H1
Bae, SA; Chong, DJ; Easwaramoorthy, B; Farwell, MD; Ichise, M; Iida, Y1
Beduneau, A; Gromand, J; Lamprecht, A; Montesinos, RN; Moulari, B; Pellequer, Y1
Bhatia, R; Innis, RB; Kreisl, WC; Morse, CL; Pike, VW; Shetty, HU; Woock, AE; Zoghbi, SS1
Béduneau, A; Lamprecht, A; Nieto Montesinos, R; Pellequer, Y1
Ahn, JH; Ahn, S; Bae, MA; Chae, JS; Im, SH; Kim, GR; Kim, HR; Kim, P; Kim, SS; Lee, BH; Lee, KR; Lee, YR; Shin, DS; Song, JS; Woo, JC; Yang, JY; Yun, CS1

Reviews

1 review(s) available for tariquidar and loperamide

ArticleYear
Membrane transporters in drug development.
    Nature reviews. Drug discovery, 2010, Volume: 9, Issue:3

    Topics: Animals; Computer Simulation; Decision Trees; Drug Approval; Drug Discovery; Drug Evaluation, Preclinical; Drug Interactions; Humans; Membrane Transport Proteins; Mice; Mice, Knockout; Prescription Drugs

2010

Trials

3 trial(s) available for tariquidar and loperamide

ArticleYear
Tariquidar, a selective P-glycoprotein inhibitor, does not potentiate loperamide's opioid brain effects in humans despite full inhibition of lymphocyte P-glycoprotein.
    Anesthesiology, 2008, Volume: 109, Issue:6

    Topics: Adult; Analgesics, Opioid; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Brain; Cross-Over Studies; Double-Blind Method; Drug Synergism; Female; Humans; Loperamide; Lymphocytes; Male; Pupil; Quinolines; Young Adult

2008
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

9 other study(ies) available for tariquidar and loperamide

ArticleYear
Differential in vivo sensitivity to inhibition of P-glycoprotein located in lymphocytes, testes, and the blood-brain barrier.
    The Journal of pharmacology and experimental therapeutics, 2006, Volume: 317, Issue:3

    Topics: Acridines; Analgesics; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Dose-Response Relationship, Drug; Loperamide; Male; Mice; Mice, Inbred Strains; Mice, Knockout; Pain; Quinolines; T-Lymphocytes; Testis; Tetrahydroisoquinolines; Tissue Distribution

2006
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
Behavioral effects and central nervous system levels of the broadly available κ-agonist hallucinogen salvinorin A are affected by P-glycoprotein modulation in vivo.
    The Journal of pharmacology and experimental therapeutics, 2012, Volume: 341, Issue:3

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; Blepharoptosis; Blood-Brain Barrier; Central Nervous System; Discrimination, Psychological; Diterpenes, Clerodane; Dose-Response Relationship, Drug; Facial Muscles; Female; Hallucinogens; Loperamide; Macaca mulatta; Male; Quinolines; Receptors, Opioid, kappa; Salvia

2012
[Evaluation of P-glycoprotein mediated in vitro loperamide biliary excretion with sandwich-cultured rat hepatocytes model].
    Yao xue xue bao = Acta pharmaceutica Sinica, 2012, Volume: 47, Issue:4

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biliary Tract; Cells, Cultured; Chromatography, High Pressure Liquid; Cyclosporine; Hepatocytes; Loperamide; Male; Quinidine; Quinolines; Rats; Rats, Sprague-Dawley; Rhodamine 123; Tandem Mass Spectrometry

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
Coadministration of P-glycoprotein modulators on loperamide pharmacokinetics and brain distribution.
    Drug metabolism and disposition: the biological fate of chemicals, 2014, Volume: 42, Issue:4

    Topics: Acridines; Analgesics; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Brain; Chromatography, High Pressure Liquid; Dose-Response Relationship, Drug; Drug Therapy, Combination; Loperamide; Male; Mass Spectrometry; Quinolines; Rats; Rats, Sprague-Dawley; Receptors, Opioid, mu; Tetrahydroisoquinolines; Tissue Distribution

2014
Liposomes Coloaded with Elacridar and Tariquidar To Modulate the P-Glycoprotein at the Blood-Brain Barrier.
    Molecular pharmaceutics, 2015, Nov-02, Volume: 12, Issue:11

    Topics: Acridines; Animals; Antidiarrheals; ATP Binding Cassette Transporter, Subfamily B; Biological Transport; Blood-Brain Barrier; Brain; Chromatography, Liquid; Dose-Response Relationship, Drug; Drug Therapy, Combination; Gene Expression Regulation; Liposomes; Loperamide; Male; Quinolines; Rats; Rats, Sprague-Dawley; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; Tetrahydroisoquinolines; Tissue Distribution

2015
Zebrafish as a Screening Model for Testing the Permeability of Blood-Brain Barrier to Small Molecules.
    Zebrafish, 2017, Volume: 14, Issue:4

    Topics: Animals; Antidiarrheals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Blood-Brain Barrier; Brain; Cell Membrane Permeability; Drug Delivery Systems; High-Throughput Screening Assays; Loperamide; Male; Mice; Mice, Inbred ICR; Models, Animal; Quinolines; Zebrafish

2017