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Drug-Target Interaction

Drug

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PubChem ID:97297
Structure:
Synonyms:
(2R,3R,4S,5R)-2-(4-AMINO-5-IODO-7H-PYRROLO[2,3-D]PYRIMIDIN-7-YL)-5-(HYDROX
(2R,3R,4S,5R)-2-(4-AMINO-5-IODO-7H-PYRROLO[2,3-D]PYRIMIDIN-7-YL)-5-(HYDROXYMETHYL)TETRAHYDROFURAN-3,4-DIOL
(2R,3R,4S,5R)-2-(4-amino-5-iodopyrrolo[2,3-d]pyrimidin-7-yl)-5-(hydroxymethyl)oxolane-3,4-diol
2-(4-Amino-5-iodo-pyrrolo[2,3-d]pyrimidin-7-yl)-5-hydroxymethyl-tetrahydro-furan-3,4-diol
24386-93-4
5-iodo-7-(beta-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
5-Iodotubercidin
5ID
7-iodo-7-deazaadenosine
7-iodotubercidin
7H-Pyrrolo(2,3-d)pyrimidin-4-amine, 5-iodo-7-beta-D-ribofuranosyl-
AIDS-187690
AIDS187690
Ambap3549
CHEBI:40167
DB04604
LS-186784
LS-187457
NSC 113939

Target

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Uniprot ID:ADK_RAT
Synonyms:
Adenosine 5'-phosphotransferase
Adenosine kinase
AK
EC-Numbers:2.7.1.20
Organism:Rat
Rattus norvegicus
PDB IDs:1LNJ
Structure:
1LNJ

Binding Affinities:

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

References:

7838317
Inhibition of adenosine kinase increases endogenous adenosine and depresses neuronal activity in hippocampal slices.. M A Pak; H L Haas; U K Decking; J Schrader (1994) Neuropharmacology display abstract
Endogenous adenosine in the extracellular space inhibits neuronal activity. The roles of adenosine kinase, S-adenosylhomocysteine-hydrolase and adenosine deaminase activities in the regulation of the adenosine levels were investigated in rat hippocampal slices. Iodotubercidin, an inhibitor of adenosine kinase, added to the perfusion fluid at 5 microM increased the release of adenosine from the slices more than 2-fold. Iodotubercidin treatment caused inhibition of population spike discharges and hyperpolarization of pyramidal cells, mimicking the effects of exogenously applied adenosine. Adenosine dialdehyde, an inhibitor of S-adenosylhomocysteine hydrolase, and erythro-9-(2-hydroxy-3-nonyl) adenine (EHNA), an inhibitor of adenosine deaminase had little or no effect on the parameters tested. The action of iodotubercidin was greater during deaminase inhibition. The A1-receptor antagonist DPCPX had actions opposite to those of adenosine and blocked the electrophysiological effects of exogenous adenosine and of iodotubercidin. Thus adenosine kinase activity is a significant factor in the regulation of adenosine levels in the hippocampus.