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 | 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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P16662 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
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 | Comment | Organism |
---|---|---|
UGT2B7 | - |
Homo sapiens |
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 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 |