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Drug-Target Interaction

Drug

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PubChem ID:10789
Structure:
Synonyms:
0TR
2,4,6-Cycloheptatrien-1-one, 2-hydroxy-
2-Hydroxy-2,4,6-cycloheptatrien-1-one
2-Hydroxy-2,4,6-cycloheptatrienone
2-hydroxycyclohepta-2,4,6-trien-1-one
2-Hydroxycyclohepta-2,4,6-trienone
2-Hydroxytropone
4-08-00-00159 (Beilstein Handbook Reference)
533-75-5
93555_FLUKA
AC-15250
AC1L1VY5
AIDS-228516
AIDS228516
BRN 1904978
C15474
CCG-35867
CCRIS 6609
CHEBI:300727
CHEMBL121188
CI TROPOLONE 8
EINECS 208-577-2
I14-0049
LS-56180
MDYOLVRUBBJPFM-UHFFFAOYSA-
NCI60_041986
NCIMech_000829
NSC 89303
NSC89303
Purpurocatechol
ST50998276
T0606
T89702_ALDRICH
Tropolone
ZINC00392003

Target

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Uniprot ID:COMT_RAT
Synonyms:
Catechol O-methyltransferase
EC-Numbers:2.1.1.6
Organism:Rat
Rattus norvegicus
PDB IDs:1H1D 1JR4 1VID 2CL5 2ZLB 2ZTH 2ZVJ
Structure:
2ZVJ

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

3561526
Effects of extraneuronal uptake inhibitors on the positive chronotropic response to isoprenaline and on the accumulation of isoprenaline in perfused rat heart after inhibition of catechol-O-methyl transferase.. T Magaribuchi; T Hama; K Kurahashi; M Fujiwara (1987) Naunyn-Schmiedeberg's archives of pharmacology display abstract
Experiments were carried out in isolated perfused rat hearts. The presence of tropolone (100 mumol/l), an inhibitor of catechol-O-methyl transferase (COMT), significantly potentiated the positive chronotropic response to isoprenaline (0.1, 1, 3 and 10 nmol/l). Two uptake2 inhibitors, 3-O-methylisoprenaline (100 mumol/l) and normetanephrine (100 mumol/l), induced a positive chronotropic response, but corticosterone (100 mumol/l) and hydrocortisone (100 mumol/l) had no such effect. 3-O-methylisoprenaline (100 mumol/l) and normetanephrine (100 mumol/l) enhanced the positive chronotropic response to isoprenaline (0.1, 1, 3 and 10 nmol/l). Corticosterone (100 mumol/l) potentiated the positive chronotropic response to isoprenaline (0.1 and 1 nmol/l). Hydrocortisone (30 mumol/l) enhanced the response to 0.1 nmol/l isoprenaline but did not affect the positive chronotropic responses to 1, 3 or 10 nmol/l isoprenaline. The addition of uptake2 inhibitors (3-O-methylisoprenaline, 100 mumol/l; normetanephrine, 100 mumol/l; corticosterone, 100 mumol/l) to the perfusion medium significantly reduced the positive chronotropic response to the perfusion with isoprenaline (3 nmol/l) and tropolone (100 mumol/l). The accumulation of 3H-isoprenaline in the heart perfused with 3H-isoprenaline (1, 10 and 100 nmol/l) was significantly increased by the presence of tropolone (100 mumol/l): the accumulation for 1, 10 and 100 nmol/l of 3H-isoprenaline was 5.07, 47.0 and 500 pmol/g, respectively. The high accumulation observed during perfusion with 3H-isoprenaline (3 nmol/l) and tropolone (100 mumol/l) was significantly decreased by the addition of an uptake2 inhibitor, 3-O-methylisoprenaline (100 mumol/l), normetanephrine (100 mumol/l) or corticosterone (100 mumol/l), but not by hydrocortisone (30 mumol/l).