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Literature summary for 7.6.2.2 extracted from

  • Feng, B.; Mills, J.B.; Davidson, R.E.; Mireles, R.J.; Janiszewski, J.S.; Troutman, M.D.; de Morais, S.M.
    In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system (2008), Drug Metab. Dispos., 36, 268-275.
    View publication on PubMed
Search for more literature for 7.6.2.2

Application

Application Comment Organism
analysis use of in vitro transporter assays for analysis of the role of P-glycoprotein mediated efflux activity. The transwell assay is a valuable tool to evaluate human P-glycoprotein interaction with compounds for assessing brain penetration of new chemical entities Homo sapiens
analysis use of in vitro transporter assays for analysis of the role of P-glycoprotein mediated efflux activity. The transwell assay is a valuable tool to evaluate P-glycoprotein interaction with compounds for assessing brain penetration of new chemical entities Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
expression in MDCK cell Mus musculus
expression in MDCK cell Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0014
-
 ATP pH 6.8, 37°C, presence of loratidine Homo sapiens
0.009
-
 ATP pH 6.8, 37°C, presence of verapamil Homo sapiens
0.0094
-
 ATP pH 6.8, 37°C, presence of sertraline Homo sapiens
0.0113
-
 ATP pH 6.8, 37°C, presence of ritonavir Homo sapiens
0.0114
-
 ATP pH 6.8, 37°C, presence of loperamide Homo sapiens
0.0137
-
 ATP pH 6.8, 37°C, presence of quinidine Homo sapiens
0.0262
-
 ATP pH 6.8, 37°C, presence of paroxetine Homo sapiens
0.0361
-
 ATP pH 6.8, 37°C, presence of risperidone Homo sapiens
0.041
-
 ATP pH 6.8, 37°C, presence of chlorpromazine Homo sapiens
0.0444
-
 ATP pH 6.8, 37°C, presence of midazoloam Homo sapiens
0.0516
-
 ATP pH 6.8, 37°C, presence of fluoxetine Homo sapiens
0.0546
-
 ATP pH 6.8, 37°C, presence of prazosin Homo sapiens
0.056
-
 ATP pH 6.8, 37°C, presence of nortryptiline Homo sapiens
0.0774
-
 ATP pH 6.8, 37°C, presence of cyclobenzaprine Homo sapiens
0.1
-
 ATP pH 6.8, 37°C, presence of hydroxyzine Homo sapiens
0.118
-
 ATP pH 6.8, 37°C, presence of buspirone Homo sapiens
0.141
-
 ATP pH 6.8, 37°C, presence of diazepam Homo sapiens
0.172
-
 ATP pH 6.8, 37°C, presence of trazodone Homo sapiens
0.177
-
 ATP pH 6.8, 37°C, presence of 9-hydroxyrisperidone Homo sapiens
0.18
-
 ATP pH 6.8, 37°C, presence of fluvoxamine Homo sapiens
0.18
-
 ATP pH 6.8, 37°C, presence of propoxyphene Homo sapiens
0.198
-
 ATP pH 6.8, 37°C, presence of zolpidem Homo sapiens
0.291
-
 ATP pH 6.8, 37°C, presence of prednisone Homo sapiens
0.441
-
 ATP pH 6.8, 37°C, presence of citalopram Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isoform MDR1
-
Mus musculus
-
 isoform Mdr1a
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + 9-hydroxyrisperidone/in
-
 Mus musculus ADP + phosphate + 9-hydroxyrisperidone/out
-
 ?
ATP + H2O + 9-hydroxyrisperidone/in
-
 Homo sapiens ADP + phosphate + 9-hydroxyrisperidone/out
-
 ?
ATP + H2O + buspirone/in
-
 Mus musculus ADP + phosphate + buspirone/out
-
 ?
ATP + H2O + buspirone/in
-
 Homo sapiens ADP + phosphate + buspirone/out
-
 ?
ATP + H2O + chlorpromazine/in
-
 Mus musculus ADP + phosphate + chlorpromazine/out
-
 ?
ATP + H2O + chlorpromazine/in
-
 Homo sapiens ADP + phosphate + chlorpromazine/out
-
 ?
ATP + H2O + citalopram/in
-
 Mus musculus ADP + phosphate + citalopram/out
-
 ?
ATP + H2O + citalopram/in
-
 Homo sapiens ADP + phosphate + citalopram/out
-
 ?
ATP + H2O + cyclobenzaprine/in
-
 Mus musculus ADP + phosphate + cyclobenzaprine/out
-
 ?
ATP + H2O + cyclobenzaprine/in
-
 Homo sapiens ADP + phosphate + cyclobenzaprine/out
-
 ?
ATP + H2O + diazepam/in
-
 Mus musculus ADP + phosphate + diazepam/out
-
 ?
ATP + H2O + diazepam/in
-
 Homo sapiens ADP + phosphate + diazepam/out
-
 ?
ATP + H2O + fluoxetine/in
-
 Mus musculus ADP + phosphate + fluoxetine/out
-
 ?
ATP + H2O + fluoxetine/in
-
 Homo sapiens ADP + phosphate + fluoxetine/out
-
 ?
ATP + H2O + fluvoxamine/in
-
 Mus musculus ADP + phosphate + fluvoxamine/out
-
 ?
ATP + H2O + fluvoxamine/in
-
 Homo sapiens ADP + phosphate + fluvoxamine/out
-
 ?
ATP + H2O + hydroxyzine/in
-
 Mus musculus ADP + phosphate + hydroxyzine/out
-
 ?
ATP + H2O + hydroxyzine/in
-
 Homo sapiens ADP + phosphate + hydroxyzine/out
-
 ?
ATP + H2O + loperamide/in
-
 Mus musculus ADP + phosphate + loperamide/out
-
 ?
ATP + H2O + loperamide/in
-
 Homo sapiens ADP + phosphate + loperamide/out
-
 ?
ATP + H2O + midazolam/in
-
 Mus musculus ADP + phosphate + midazolam/out
-
 ?
ATP + H2O + midazolam/in
-
 Homo sapiens ADP + phosphate + midazolam/out
-
 ?
ATP + H2O + nortryptiline/in
-
 Mus musculus ADP + phosphate + nortryptiline/out
-
 ?
ATP + H2O + nortryptiline/in
-
 Homo sapiens ADP + phosphate + nortryptiline/out
-
 ?
ATP + H2O + paroxetine/in
-
 Mus musculus ADP + phosphate + paroxetine/out
-
 ?
ATP + H2O + paroxetine/in
-
 Homo sapiens ADP + phosphate + paroxetine/out
-
 ?
ATP + H2O + prazosin/in
-
 Mus musculus ADP + phosphate + prazosin/out
-
 ?
ATP + H2O + prazosin/in
-
 Homo sapiens ADP + phosphate + prazosin/out
-
 ?
ATP + H2O + prednisone/in
-
 Mus musculus ADP + phosphate + prednisone/out
-
 ?
ATP + H2O + prednisone/in
-
 Homo sapiens ADP + phosphate + prednisone/out
-
 ?
ATP + H2O + propoxyphene/in
-
 Mus musculus ADP + phosphate + propoxyphene/out
-
 ?
ATP + H2O + propoxyphene/in
-
 Homo sapiens ADP + phosphate + propoxyphene/out
-
 ?
ATP + H2O + quinidine/in
-
 Mus musculus ADP + phosphate + quinidine/out
-
 ?
ATP + H2O + quinidine/in
-
 Homo sapiens ADP + phosphate + quinidine/out
-
 ?
ATP + H2O + risperidone/in
-
 Mus musculus ADP + phosphate + risperidone/out
-
 ?
ATP + H2O + risperidone/in
-
 Homo sapiens ADP + phosphate + risperidone/out
-
 ?
ATP + H2O + ritonavir/in
-
 Mus musculus ADP + phosphate + ritonavir/out
-
 ?
ATP + H2O + ritonavir/in
-
 Homo sapiens ADP + phosphate + ritonavir/out
-
 ?
ATP + H2O + sertraline/in
-
 Mus musculus ADP + phosphate + sertraline/out
-
 ?
ATP + H2O + sertraline/in
-
 Homo sapiens ADP + phosphate + sertraline/out
-
 ?
ATP + H2O + trazodone/in
-
 Mus musculus ADP + phosphate + trazodone/out
-
 ?
ATP + H2O + trazodone/in
-
 Homo sapiens ADP + phosphate + trazodone/out
-
 ?
ATP + H2O + verapamil/in
-
 Mus musculus ADP + phosphate + verapamil/out
-
 ?
ATP + H2O + verapamil/in
-
 Homo sapiens ADP + phosphate + verapamil/out
-
 ?
ATP + H2O + zolpidem/in
-
 Mus musculus ADP + phosphate + zolpidem/out
-
 ?
ATP + H2O + zolpidem/in
-
 Homo sapiens ADP + phosphate + zolpidem/out
-
 ?
additional information no substrate: loratidine Mus musculus ?
-
 ?
additional information no substrate: loratidine Homo sapiens ?
-
 ?