PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 21725799-0 2011 Validation of quinidine as a probe substrate for the in vitro P-gp inhibition assay in Caco-2 cell monolayer. Quinidine 14-23 phosphoglycolate phosphatase Homo sapiens 62-66 24947467-2 2014 For five P-gp substrates (indinavir, quinidine, loperamide, paclitaxel, and verapamil) and one nonsubstrate (diazepam), in vitro P-gp transport activities were determined by measuring transcellular transport across monolayers of cynomolgus monkey P-gp-transfected LLC-PK1 and parental cells. Quinidine 37-46 phosphoglycolate phosphatase Homo sapiens 129-133 24947467-2 2014 For five P-gp substrates (indinavir, quinidine, loperamide, paclitaxel, and verapamil) and one nonsubstrate (diazepam), in vitro P-gp transport activities were determined by measuring transcellular transport across monolayers of cynomolgus monkey P-gp-transfected LLC-PK1 and parental cells. Quinidine 37-46 phosphoglycolate phosphatase Homo sapiens 129-133 23976943-12 2013 We also find that P-gp substrates with relatively low passive permeability such as digoxin, loperamide and vinblastine kinetically require basolateral uptake transport over that allowed by +GF120918 passive permeability, while highly permeable P-gp substrates such as amprenavir, quinidine, ketoconazole and verapamil do not, regardless of whether they actually use the basolateral transporter. Quinidine 280-289 phosphoglycolate phosphatase Homo sapiens 18-22 21725799-1 2011 Although quinidine has been recommended as a probe substrate for the P-gp inhibition assay using Caco-2 cell monolayer, it has not been studied widely in the in vitro system. Quinidine 9-18 phosphoglycolate phosphatase Homo sapiens 69-73 21725799-2 2011 In the present investigation, in vitro permeability studies using Caco-2 cell monolayer were carried out in order to optimize and validate quinidine as a P-gp probe substrate. Quinidine 139-148 phosphoglycolate phosphatase Homo sapiens 154-158 21725799-6 2011 Overall, quinidine was found to be a good probe substrate for routine use to assess the in vitro inhibitory potency of NCEs on Pgp-mediated transport. Quinidine 9-18 phosphoglycolate phosphatase Homo sapiens 127-130 19248230-8 2009 Concentration dependent decrease of this secretion was obtained by the P-gp inhibitors verapamil, erythromycin and quinidine, while no effect was evident by the MRP2 inhibitor MK-571 and the BCRP inhibitor FTC, indicating that P-gp is the transporter mediates the intestinal efflux of cimetidine and famotidine. Quinidine 115-124 phosphoglycolate phosphatase Homo sapiens 71-75 20196146-5 2011 Rhodamine assay also revealed that hydrocinchonine, cinchonine, and quinidine effectively enhanced the accumulation of a P-gp substrate, rhodamine in TAX-treated MES-SA/DX5 cells compared with TAX-treated control. Quinidine 68-77 phosphoglycolate phosphatase Homo sapiens 121-125 20196146-6 2011 In addition, hydrocinchonine, cinchonine, and quinidine effectively cleaved poly (ADP-ribose) polymerase (PARP), activated caspase-3, and downregulated P-gp expression as well as increased sub-G1 apoptotic portion in TAX-treated MES-SA/DX5 cells. Quinidine 46-55 phosphoglycolate phosphatase Homo sapiens 152-156 22028772-9 2011 The P-gp efflux rate constants for quinidine and digoxin were about 3-fold smaller than reported ATP hydrolysis rate constants from P-gp proteoliposomes. Quinidine 35-44 phosphoglycolate phosphatase Homo sapiens 4-8 22028772-9 2011 The P-gp efflux rate constants for quinidine and digoxin were about 3-fold smaller than reported ATP hydrolysis rate constants from P-gp proteoliposomes. Quinidine 35-44 phosphoglycolate phosphatase Homo sapiens 132-136 19816852-8 2010 The efflux ratio for quinidine (100 nm) alone was 10.8, which reduced to less than 2 in the presence of the classical P-gp inhibitors verapamil and ketoconazole (100 mum each). Quinidine 21-30 phosphoglycolate phosphatase Homo sapiens 118-122 15501934-9 2005 For three P-gp substrates (amprenavir, loperamide, and quinidine), we have successfully fitted the elementary rate constants, i.e., drug association to P-gp from the apical membrane inner monolayer, drug dissociation back into the apical membrane inner monolayer, and drug efflux from P-gp into the apical chamber, as well as the density of efflux active P-gp. Quinidine 55-64 phosphoglycolate phosphatase Homo sapiens 10-14 15501934-9 2005 For three P-gp substrates (amprenavir, loperamide, and quinidine), we have successfully fitted the elementary rate constants, i.e., drug association to P-gp from the apical membrane inner monolayer, drug dissociation back into the apical membrane inner monolayer, and drug efflux from P-gp into the apical chamber, as well as the density of efflux active P-gp. Quinidine 55-64 phosphoglycolate phosphatase Homo sapiens 152-156 15501934-9 2005 For three P-gp substrates (amprenavir, loperamide, and quinidine), we have successfully fitted the elementary rate constants, i.e., drug association to P-gp from the apical membrane inner monolayer, drug dissociation back into the apical membrane inner monolayer, and drug efflux from P-gp into the apical chamber, as well as the density of efflux active P-gp. Quinidine 55-64 phosphoglycolate phosphatase Homo sapiens 152-156 15501934-9 2005 For three P-gp substrates (amprenavir, loperamide, and quinidine), we have successfully fitted the elementary rate constants, i.e., drug association to P-gp from the apical membrane inner monolayer, drug dissociation back into the apical membrane inner monolayer, and drug efflux from P-gp into the apical chamber, as well as the density of efflux active P-gp. Quinidine 55-64 phosphoglycolate phosphatase Homo sapiens 152-156 15266218-7 2004 These values were also comparable with the inhibitory effect of quinidine in Caco-2 cells, a well-known inhibitor of P-gp, on ritonavir efflux from Caco-2 cells. Quinidine 64-73 phosphoglycolate phosphatase Homo sapiens 117-121 26354948-6 2015 At clinically relevant quinidine plasma concentrations, P-gp inhibition resulted in a 60% increase in (11)C-radioactivity distribution across the human BBB as measured by the brain extraction ratio (ER) of (11)C-radioactivity. Quinidine 23-32 phosphoglycolate phosphatase Homo sapiens 56-60 26354948-8 2015 Although our findings demonstrated that quinidine did not completely inhibit P-gp at the human BBB, it has the potential to produce clinically significant CNS drug interactions with P-gp substrate drugs that exhibit a narrow therapeutic window and are significantly excluded from the brain by P-gp. Quinidine 40-49 phosphoglycolate phosphatase Homo sapiens 182-186 26354948-8 2015 Although our findings demonstrated that quinidine did not completely inhibit P-gp at the human BBB, it has the potential to produce clinically significant CNS drug interactions with P-gp substrate drugs that exhibit a narrow therapeutic window and are significantly excluded from the brain by P-gp. Quinidine 40-49 phosphoglycolate phosphatase Homo sapiens 182-186