Any feedback?
Literature summary for 2.4.1.17 extracted from
- 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.
Application
| Application | Comment | Organism |
|---|---|---|
| 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
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (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 |  |
| 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 | |
| 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 | |
| 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 | |
| desipramine | - |
Homo sapiens | |
| diazepam | IC50 for morphine 3-glucuronide formation: 0.057 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.053 mM (noncompetitive) | Homo sapiens | |
| diclofenac | IC50 for morphine 3-glucuronide formation: 0.032 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.031 mM (noncompetitive) | Homo sapiens | |
| 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 | |
| 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 | |
| mycophenolate | IC50 for morphine 3-glucuronide formation: 0.341 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.389 mM (noncompetitive) | Homo sapiens | |
| 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 | |
| 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 | |
| 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 | |
| tamoxifen | IC50 for morphine 3-glucuronide formation: 0.093 mM (noncompetitive), IC50 for morphine 3-glucuronide formation: 0.107 mM (noncompetitive) | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P16662 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetaminophen + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
| amitriptyline + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
| etoposide + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
| lorazepam + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
| milnacipran + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
| morphine + UDP-glucuronate | - |
Homo sapiens | UDP + morphine 3-glucuronide + morphine 6-glucuronide | - |
? | |
| mycophenolate + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
| olanzapine + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
| oxazepam + UDP-glucuronate | - |
Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UGT2B7 | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.006 | - |
clomipramine | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.009 | - |
diazepam | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.017 | - |
lorazepam | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.019 | - |
clomipramine | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.02 | - |
clomipramine | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.022 | - |
diclofenac | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.024 | - |
diclofenac | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.027 | - |
tamoxifen | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.03 | - |
amitriptyline | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.033 | - |
imipramine | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.041 | - |
oxazepam | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.046 | - |
tacrolimus | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.047 | - |
diazepam | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.047 | - |
carbamazepine | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.053 | - |
lorazepam | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.06 | - |
imipramine | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.065 | - |
lorazepam | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.078 | - |
carbamazepine | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.081 | - |
imipramine | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.081 | - |
tamoxifen | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.093 | - |
oxazepam | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.095 | - |
tacrolimus | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.101 | - |
tacrolimus | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.111 | - |
desipramine | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.111 | - |
amitriptyline | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.118 | - |
carbamazepine | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.177 | - |
desipramine | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.196 | - |
olanzapine | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.239 | - |
lorazepam | Kis, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.243 | - |
carbamazepine | Kis, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.248 | - |
amitriptyline | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.266 | - |
olanzapine | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.296 | - |
mycophenolate | Kii, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.347 | - |
tacrolimus | Kis, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.458 | - |
desipramine | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
| 0.518 | - |
naloxone | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.519 | - |
oxazepam | Kis, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 0.713 | - |
mycophenolate | Kii, morphine 3-glucuronosyltransferase activity | Homo sapiens | |
| 1.298 | - |
naloxone | Kis, morphine 6-glucuronosyltransferase activity | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 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 | |
| 0.037 | - |
, IC50 for morphine 3-glucuronide formation: 0.037 mM (mixed type inhibition) | Homo sapiens | clomipramine | |
| 0.04 | - |
IC50 for morphine 3-glucuronide formation: 0.04 mM (noncompetitive) | Homo sapiens | clomipramine | |
| 0.053 | - |
IC50 for morphine 3-glucuronide formation: 0.053 mM (noncompetitive) | Homo sapiens | diazepam | |
| 0.056 | - |
IC50 for morphine 3-glucuronide formation: 0.056 mM (mixed type inhibition) | Homo sapiens | lorazepam | |
| 0.057 | - |
IC50 for morphine 3-glucuronide formation: 0.057 mM (noncompetitive) | Homo sapiens | diazepam | |
| 0.065 | - |
IC50 for morphine 3-glucuronide formation: 0.065 mM (mixed type inhibition) | Homo sapiens | lorazepam | |
| 0.093 | - |
IC50 for morphine 3-glucuronide formation: 0.093 mM (noncompetitive) | Homo sapiens | tamoxifen | |
| 0.107 | - |
IC50 for morphine 3-glucuronide formation: 0.107 mM (noncompetitive) | Homo sapiens | tamoxifen | |
| 0.109 | - |
IC50 for morphine 3-glucuronide formation: 0.109 mM (competitive) | Homo sapiens | oxazepam | |
| 0.116 | - |
, IC50 for morphine 3-glucuronide formation: 0.116 mM (mixed type inhibition) | Homo sapiens | imipramine | |
| 0.119 | - |
IC50 for morphine 3-glucuronide formation: 0.119 mM (mixed type inhibition) | Homo sapiens | oxazepam | |
| 0.129 | - |
IC50 for morphine 3-glucuronide formation: 0.129 mM (noncompetitive) | Homo sapiens | imipramine | |
| 0.136 | - |
IC50 for morphine 3-glucuronide formation: 0.136 mM (mixed type inhibition) | Homo sapiens | amitriptyline | |
| 0.159 | - |
IC50 for morphine 3-glucuronide formation: 0.159 mM (noncompetitive) | Homo sapiens | amitriptyline | |
| 0.341 | - |
IC50 for morphine 3-glucuronide formation: 0.341 mM (noncompetitive) | Homo sapiens | mycophenolate | |
| 0.368 | - |
IC50 for morphine 3-glucuronide formation: 0.368 mM (noncompetitive) | Homo sapiens | olanzapine | |
| 0.384 | - |
IC50 for morphine 3-glucuronide formation: 0.384 mM (mixed type inhibition) | Homo sapiens | tacrolimus | |
| 0.389 | - |
IC50 for morphine 3-glucuronide formation: 0.389 mM (noncompetitive) | Homo sapiens | mycophenolate | |
| 0.4 | - |
IC50 for morphine 3-glucuronide formation: 0.4 mM (mixed type inhibition) | Homo sapiens | tacrolimus | |
| 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 | |
| 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 | |
| 0.431 | - |
IC50 for morphine 3-glucuronide formation: 0.431 mM (mixed type inhibition) | Homo sapiens | carbamazepine | |
| 0.456 | - |
IC50 for morphine 3-glucuronide formation: 0.456 mM (mixed type inhibition) | Homo sapiens | carbamazepine | |
| 0.488 | - |
IC50 for morphine 3-glucuronide formation: 0.488 mM (mixed type inhibition) | Homo sapiens | tacrolimus | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
