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Literature summary extracted from

  • Hara, Y.; Nakajima, M.; Miyamoto, K.; Yokoi, T.
    Morphine glucuronosyltransferase activity in human liver microsomes is inhibited by a variety of drugs that are co-administered with morphine (2007), Drug Metab. Pharmacokinet., 22, 103-112.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.4.1.17 medicine some drugs frequently coadministered with morphine (tamoxifen, tacrolimus, diclofenac, carbamazepine, imipramine, clomipramine, amitriptyline, diazepam, lorazepam and oxazepam) extensively inhibit the morphine 3- and 6-glucuronosyltransferase activities of UGT2B7. If patients receive morphine and these drugs simultaneously, the drug-drug interaction may change the levels of morphine and these glucuronides, resulting in altered analgesic efficacy and the risk of side effects Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 (5alpha)-17-allyl-3,14-dihydroxy-4,5-epoxymorphinan-6-one IC50 for morphine 3-glucuronide formation: 0.412 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.429 mM (competitive) Homo sapiens
2.4.1.17 amitriptyline IC50 for morphine 3-glucuronide formation: 0.159 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.136 mM (mixed type inhibition) Homo sapiens
2.4.1.17 carbamazepine IC50 for morphine 3-glucuronide formation: 0.431 mM (mixed type inhibition), IC50 for morphine 3-glucuronide formation: 0.456 mM (mixed type inhibition) Homo sapiens
2.4.1.17 clomipramine IC50 for morphine 3-glucuronide formation: 0.04 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.037 mM (mixed type inhibition) Homo sapiens
2.4.1.17 desipramine
-
 Homo sapiens
2.4.1.17 diazepam IC50 for morphine 3-glucuronide formation: 0.057 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.053 mM (noncompetitive) Homo sapiens
2.4.1.17 diclofenac IC50 for morphine 3-glucuronide formation: 0.032 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.031 mM (noncompetitive) Homo sapiens
2.4.1.17 imipramine IC50 for morphine 3-glucuronide formation: 0.129 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.116 mM (mixed type inhibition) Homo sapiens
2.4.1.17 lorazepam IC50 for morphine 3-glucuronide formation: 0.065 mM (mixed type inhibition), IC50 for morphine 3-glucuronide formation: 0.056 mM (mixed type inhibition) Homo sapiens
2.4.1.17 mycophenolate IC50 for morphine 3-glucuronide formation: 0.341 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.389 mM (noncompetitive) Homo sapiens
2.4.1.17 olanzapine IC50 for morphine 3-glucuronide formation: 0.368 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.4 mM (mixed type inhibition) Homo sapiens
2.4.1.17 oxazepam IC50 for morphine 3-glucuronide formation: 0.109 mM (competitive), IC50 for morphine 3-glucuronide formation: 0.119 mM (mixed type inhibition) Homo sapiens
2.4.1.17 tacrolimus IC50 for morphine 3-glucuronide formation: 0.384 mM (mixed type inhibition), IC50 for morphine 3-glucuronide formation: 0.488 mM (mixed type inhibition) Homo sapiens
2.4.1.17 tamoxifen IC50 for morphine 3-glucuronide formation: 0.093 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.107 mM (noncompetitive) Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens P16662
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 acetaminophen + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 amitriptyline + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 etoposide + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 lorazepam + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 milnacipran + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 morphine + UDP-glucuronate
-
 Homo sapiens UDP + morphine 3-glucuronide + morphine 6-glucuronide
-
 ?
2.4.1.17 mycophenolate + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 olanzapine + UDP-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 oxazepam + UDP-glucuronate
-
 Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UGT2B7
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.006
-
 clomipramine Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.009
-
 diazepam Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.017
-
 lorazepam Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.019
-
 clomipramine Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.02
-
 clomipramine Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.022
-
 diclofenac Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.024
-
 diclofenac Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.027
-
 tamoxifen Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.03
-
 amitriptyline Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.033
-
 imipramine Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.041
-
 oxazepam Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.046
-
 tacrolimus Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.047
-
 diazepam Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.047
-
 carbamazepine Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.053
-
 lorazepam Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.06
-
 imipramine Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.065
-
 lorazepam Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.078
-
 carbamazepine Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.081
-
 imipramine Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.081
-
 tamoxifen Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.093
-
 oxazepam Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.095
-
 tacrolimus Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.101
-
 tacrolimus Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.111
-
 desipramine Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.111
-
 amitriptyline Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.118
-
 carbamazepine Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.177
-
 desipramine Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.196
-
 olanzapine Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.239
-
 lorazepam Kis, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.243
-
 carbamazepine Kis, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.248
-
 amitriptyline Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.266
-
 olanzapine Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.296
-
 mycophenolate Kii, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.347
-
 tacrolimus Kis, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.458
-
 desipramine Kis, morphine 6-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.518
-
 naloxone Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.519
-
 oxazepam Kis, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 0.713
-
 mycophenolate Kii, morphine 3-glucuronosyltransferase activity Homo sapiens
2.4.1.17 1.298
-
 naloxone Kis, morphine 6-glucuronosyltransferase activity Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.031 0.032 IC50 for morphine 3-glucuronide formation: 0.032 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.031 mM (noncompetitive) Homo sapiens diclofenac
2.4.1.17 0.037
-
 , IC50 for morphine 3-glucuronide formation: 0.037 mM (mixed type inhibition) Homo sapiens clomipramine
2.4.1.17 0.04
-
 IC50 for morphine 3-glucuronide formation: 0.04 mM (noncompetitive) Homo sapiens clomipramine
2.4.1.17 0.053
-
 IC50 for morphine 3-glucuronide formation: 0.053 mM (noncompetitive) Homo sapiens diazepam
2.4.1.17 0.056
-
 IC50 for morphine 3-glucuronide formation: 0.056 mM (mixed type inhibition) Homo sapiens lorazepam
2.4.1.17 0.057
-
 IC50 for morphine 3-glucuronide formation: 0.057 mM (noncompetitive) Homo sapiens diazepam
2.4.1.17 0.065
-
 IC50 for morphine 3-glucuronide formation: 0.065 mM (mixed type inhibition) Homo sapiens lorazepam
2.4.1.17 0.093
-
 IC50 for morphine 3-glucuronide formation: 0.093 mM (noncompetitive) Homo sapiens tamoxifen
2.4.1.17 0.107
-
 IC50 for morphine 3-glucuronide formation: 0.107 mM (noncompetitive) Homo sapiens tamoxifen
2.4.1.17 0.109
-
 IC50 for morphine 3-glucuronide formation: 0.109 mM (competitive) Homo sapiens oxazepam
2.4.1.17 0.116
-
 , IC50 for morphine 3-glucuronide formation: 0.116 mM (mixed type inhibition) Homo sapiens imipramine
2.4.1.17 0.119
-
 IC50 for morphine 3-glucuronide formation: 0.119 mM (mixed type inhibition) Homo sapiens oxazepam
2.4.1.17 0.129
-
 IC50 for morphine 3-glucuronide formation: 0.129 mM (noncompetitive) Homo sapiens imipramine
2.4.1.17 0.136
-
 IC50 for morphine 3-glucuronide formation: 0.136 mM (mixed type inhibition) Homo sapiens amitriptyline
2.4.1.17 0.159
-
 IC50 for morphine 3-glucuronide formation: 0.159 mM (noncompetitive) Homo sapiens amitriptyline
2.4.1.17 0.341
-
 IC50 for morphine 3-glucuronide formation: 0.341 mM (noncompetitive) Homo sapiens mycophenolate
2.4.1.17 0.368
-
 IC50 for morphine 3-glucuronide formation: 0.368 mM (noncompetitive) Homo sapiens olanzapine
2.4.1.17 0.384
-
 IC50 for morphine 3-glucuronide formation: 0.384 mM (mixed type inhibition) Homo sapiens tacrolimus
2.4.1.17 0.389
-
 IC50 for morphine 3-glucuronide formation: 0.389 mM (noncompetitive) Homo sapiens mycophenolate
2.4.1.17 0.4
-
 IC50 for morphine 3-glucuronide formation: 0.4 mM (mixed type inhibition) Homo sapiens tacrolimus
2.4.1.17 0.412
-
 IC50 for morphine 3-glucuronide formation: 0.412 mM (noncompetitive) Homo sapiens (5alpha)-17-allyl-3,14-dihydroxy-4,5-epoxymorphinan-6-one
2.4.1.17 0.429
-
 IC50 for morphine 3-glucuronide formation: 0.429 mM (competitive) Homo sapiens (5alpha)-17-allyl-3,14-dihydroxy-4,5-epoxymorphinan-6-one
2.4.1.17 0.431
-
 IC50 for morphine 3-glucuronide formation: 0.431 mM (mixed type inhibition) Homo sapiens carbamazepine
2.4.1.17 0.456
-
 IC50 for morphine 3-glucuronide formation: 0.456 mM (mixed type inhibition) Homo sapiens carbamazepine
2.4.1.17 0.488
-
 IC50 for morphine 3-glucuronide formation: 0.488 mM (mixed type inhibition) Homo sapiens tacrolimus