PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 solute carrier organic anion transporter family member 1A2 Homo sapiens 42-49 28747995-1 2017 BACKGROUND: The objective of this study was to examine the inhibitory potential of darifenacin, fesoterodine, oxybutynin, propiverine, solifenacin, tolterodine and trospium chloride on the seven major human cytochrome P450 enzymes (CYP) by using a standardized and validated seven-in-one cytochrome P450 cocktail inhibition assay. trospium chloride 164-181 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 207-222 28747995-1 2017 BACKGROUND: The objective of this study was to examine the inhibitory potential of darifenacin, fesoterodine, oxybutynin, propiverine, solifenacin, tolterodine and trospium chloride on the seven major human cytochrome P450 enzymes (CYP) by using a standardized and validated seven-in-one cytochrome P450 cocktail inhibition assay. trospium chloride 164-181 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 288-303 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 solute carrier family 22 member 1 Homo sapiens 69-73 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 solute carrier family 22 member 5 Homo sapiens 83-88 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 solute carrier family 10 member 1 Homo sapiens 90-94 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 solute carrier family 10 member 2 Homo sapiens 100-104 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 phosphoglycolate phosphatase Homo sapiens 129-133 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 ATP binding cassette subfamily C member 2 Homo sapiens 135-139 25466967-4 2015 Affinity of TC to the uptake transporters OATP1A2, -1B1, -1B3, -2B1, OCT1, -2, -3, OCTN2, NTCP, and ASBT and the efflux carriers P-gp, MRP2 and MRP3 transfected in HEK293 and MDCK2 cells was measured. trospium chloride 12-14 ATP binding cassette subfamily C member 3 Homo sapiens 144-148 25466967-6 2015 TC was shown to be a substrate of OATP1A2 (Km = 6.9 +- 1.3 mumol/L; Vmax = 41.6 +- 1.8 pmol/mg min), OCT1 (Km = 106 +- 16 mumol/L; Vmax = 269 +- 18 pmol/mg min), and P-gp (Km = 34.9 +- 7.5 mumol/L; Vmax = 105 +- 9.1 pmol/mg min, lipovesicle assay). trospium chloride 0-2 solute carrier organic anion transporter family member 1A2 Homo sapiens 34-41 25466967-6 2015 TC was shown to be a substrate of OATP1A2 (Km = 6.9 +- 1.3 mumol/L; Vmax = 41.6 +- 1.8 pmol/mg min), OCT1 (Km = 106 +- 16 mumol/L; Vmax = 269 +- 18 pmol/mg min), and P-gp (Km = 34.9 +- 7.5 mumol/L; Vmax = 105 +- 9.1 pmol/mg min, lipovesicle assay). trospium chloride 0-2 solute carrier family 22 member 1 Homo sapiens 101-105 25466967-6 2015 TC was shown to be a substrate of OATP1A2 (Km = 6.9 +- 1.3 mumol/L; Vmax = 41.6 +- 1.8 pmol/mg min), OCT1 (Km = 106 +- 16 mumol/L; Vmax = 269 +- 18 pmol/mg min), and P-gp (Km = 34.9 +- 7.5 mumol/L; Vmax = 105 +- 9.1 pmol/mg min, lipovesicle assay). trospium chloride 0-2 phosphoglycolate phosphatase Homo sapiens 166-170 25466967-7 2015 The genetic OATP1A2 variants *2 and *3 were loss-of-function transporters for TC. trospium chloride 78-80 solute carrier organic anion transporter family member 1A2 Homo sapiens 12-19 25466967-11 2015 TC was taken up into HBU cells (Km = 18.5 +- 4.8 mumol/L; Vmax = 106 +- 11.3 pmol/mg min) by mechanisms that could be synergistically inhibited by naringin (IC50 = 10.8 (8.4; 13.8) mumol/L) and verapamil (IC50 = 4.6 (2.8; 7.5) mumol/L), inhibitors of OATP1A2 and OCT1, respectively. trospium chloride 0-2 solute carrier organic anion transporter family member 1A2 Homo sapiens 251-258 25466967-11 2015 TC was taken up into HBU cells (Km = 18.5 +- 4.8 mumol/L; Vmax = 106 +- 11.3 pmol/mg min) by mechanisms that could be synergistically inhibited by naringin (IC50 = 10.8 (8.4; 13.8) mumol/L) and verapamil (IC50 = 4.6 (2.8; 7.5) mumol/L), inhibitors of OATP1A2 and OCT1, respectively. trospium chloride 0-2 solute carrier family 22 member 1 Homo sapiens 263-267 25466967-12 2015 Affinity of TC to OCT1 and P-glycoprotein may be the reason for incomplete oral absorption, wide distribution into liver and kidneys, and substantial intestinal and renal secretions. trospium chloride 12-14 solute carrier family 22 member 1 Homo sapiens 18-22 25466967-12 2015 Affinity of TC to OCT1 and P-glycoprotein may be the reason for incomplete oral absorption, wide distribution into liver and kidneys, and substantial intestinal and renal secretions. trospium chloride 12-14 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 19389858-0 2009 The role of p-glycoprotein in limiting brain penetration of the peripherally acting anticholinergic overactive bladder drug trospium chloride. trospium chloride 124-141 phosphoglycolate phosphatase Mus musculus 12-26 19389858-1 2009 The aim of the present study was to characterize the role of the drug-efflux transporter P-glycoprotein (P-gp) for the disposition of trospium chloride, a widely used anticholinergic drug for the treatment of overactive bladder. trospium chloride 134-151 phosphoglycolate phosphatase Mus musculus 89-103 19389858-1 2009 The aim of the present study was to characterize the role of the drug-efflux transporter P-glycoprotein (P-gp) for the disposition of trospium chloride, a widely used anticholinergic drug for the treatment of overactive bladder. trospium chloride 134-151 phosphoglycolate phosphatase Mus musculus 105-109 19389858-3 2009 The concentrations of trospium chloride in the brain were up to 7 times higher in the mdr1a,b(-/-) knockout mice compared with wild-type mice (p < 0.05), making P-gp a limiting factor for the blood-brain barrier penetration of this drug. trospium chloride 22-39 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 86-91 19389858-3 2009 The concentrations of trospium chloride in the brain were up to 7 times higher in the mdr1a,b(-/-) knockout mice compared with wild-type mice (p < 0.05), making P-gp a limiting factor for the blood-brain barrier penetration of this drug. trospium chloride 22-39 phosphoglycolate phosphatase Mus musculus 164-168 19389858-5 2009 Apart from the blood-brain barrier, P-gp also had significant effects on the overall pharmacokinetics of trospium chloride. trospium chloride 105-122 phosphoglycolate phosphatase Mus musculus 36-40 19389858-7 2009 Our study indicates that the multidrug resistance transporter P-gp is a major determinant for the distribution of trospium chloride in the body and highly restricts its entry into the brain. trospium chloride 114-131 phosphoglycolate phosphatase Mus musculus 62-66 16809803-3 2006 The effect of trospium chloride on human P-glycoprotein-mediated transport of [3H]-digoxin was determined in vitro. trospium chloride 14-31 ATP binding cassette subfamily B member 1 Homo sapiens 41-55 10628907-10 1999 Thus, trospium chloride has negligible inhibitory effects on CYP3A4, CYP1A2, CYP2E1, CYP2C19, CYP2C9 and CYP2A6 activity but is a reasonably potent inhibitor of CYP2D6 in vitro. trospium chloride 6-23 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 161-167 10628907-11 1999 Compared to therapeutic trospium chloride peak plasma concentrations below 50 nM, the 1000-times higher competitive inhibition constant Ki however suggests that inhibition of CYP2D6 by trospium chloride is without any clinical relevance. trospium chloride 185-202 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 175-181 22120415-3 2013 METHODS: Trospium chloride at 1 mg/kg was intravenously administered to adult, middle-aged, and aged mice at 6, 12, and 24 months of age, respectively, and the absolute drug concentrations in the brain were analysed after 2 h. Furthermore, mRNA expression levels of relevant markers of blood-brain barrier integrity (occludin, claudin-5, and the drug efflux carrier P-glycoprotein) were analysed in brain samples from adult and aged mice. trospium chloride 9-26 occludin Mus musculus 317-325 22120415-3 2013 METHODS: Trospium chloride at 1 mg/kg was intravenously administered to adult, middle-aged, and aged mice at 6, 12, and 24 months of age, respectively, and the absolute drug concentrations in the brain were analysed after 2 h. Furthermore, mRNA expression levels of relevant markers of blood-brain barrier integrity (occludin, claudin-5, and the drug efflux carrier P-glycoprotein) were analysed in brain samples from adult and aged mice. trospium chloride 9-26 claudin 5 Mus musculus 327-336 22120415-7 2013 CONCLUSION: Based on our in vivo data in a mouse model, we conclude that trospium chloride permeation across the BBB is not increased in ageing per se, and therefore, the occurrence of adverse CNS drug effects is also not expected to increase with ageing. trospium chloride 73-90 ALMS1, centrosome and basal body associated Mus musculus 113-116 33375004-4 2020 In humans, the organic cation transporters OCT1 and OCT2 and the multidrug and toxin extrusion MATE1 and MATE2-K carriers showed TCl transport. trospium chloride 129-132 solute carrier family 22 member 1 Homo sapiens 43-47 33375004-4 2020 In humans, the organic cation transporters OCT1 and OCT2 and the multidrug and toxin extrusion MATE1 and MATE2-K carriers showed TCl transport. trospium chloride 129-132 solute carrier family 22 member 2 Homo sapiens 52-56 33375004-4 2020 In humans, the organic cation transporters OCT1 and OCT2 and the multidrug and toxin extrusion MATE1 and MATE2-K carriers showed TCl transport. trospium chloride 129-132 solute carrier family 47 member 1 Homo sapiens 95-100 33375004-4 2020 In humans, the organic cation transporters OCT1 and OCT2 and the multidrug and toxin extrusion MATE1 and MATE2-K carriers showed TCl transport. trospium chloride 129-132 solute carrier family 47 member 2 Homo sapiens 105-112 33375004-6 2020 Knockout mouse models lacking mOct1/mOct2 or mMate1 might help to clarify their role for the overall pharmacokinetics of TCl. trospium chloride 121-124 solute carrier family 22 (organic cation transporter), member 1 Mus musculus 30-35 33375004-6 2020 Knockout mouse models lacking mOct1/mOct2 or mMate1 might help to clarify their role for the overall pharmacokinetics of TCl. trospium chloride 121-124 solute carrier family 22 (organic cation transporter), member 2 Mus musculus 36-41 33375004-6 2020 Knockout mouse models lacking mOct1/mOct2 or mMate1 might help to clarify their role for the overall pharmacokinetics of TCl. trospium chloride 121-124 solute carrier family 47, member 1 Mus musculus 45-51 33375004-7 2020 METHOD: In preparation of such experiments, TCl transport was analyzed in HEK293 cells stably transfected with the mouse carriers mOct1, mOct2, mMate1, and mMate2, respectively. trospium chloride 44-47 solute carrier family 22 (organic cation transporter), member 1 Mus musculus 130-135 33375004-7 2020 METHOD: In preparation of such experiments, TCl transport was analyzed in HEK293 cells stably transfected with the mouse carriers mOct1, mOct2, mMate1, and mMate2, respectively. trospium chloride 44-47 solute carrier family 22 (organic cation transporter), member 2 Mus musculus 137-142 33375004-8 2020 RESULTS: Mouse mOct1, mOct2, and mMate1 showed significant TCl transport with Km values of 58.7, 78.5, and 29.3 microM, respectively. trospium chloride 59-62 solute carrier family 22 (organic cation transporter), member 1 Mus musculus 15-20 33375004-8 2020 RESULTS: Mouse mOct1, mOct2, and mMate1 showed significant TCl transport with Km values of 58.7, 78.5, and 29.3 microM, respectively. trospium chloride 59-62 solute carrier family 22 (organic cation transporter), member 2 Mus musculus 22-27 33375004-8 2020 RESULTS: Mouse mOct1, mOct2, and mMate1 showed significant TCl transport with Km values of 58.7, 78.5, and 29.3 microM, respectively. trospium chloride 59-62 solute carrier family 47, member 1 Mus musculus 33-39 33375004-9 2020 In contrast, mMate2 did not transport TCl but showed MPP+ transport with Km of 60.0 microM that was inhibited by the drugs topotecan, acyclovir, and levofloxacin. trospium chloride 38-41 solute carrier family 47, member 2 Mus musculus 13-19