ABT 702 - CAS 214697-26-4
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
ABT 702 is a non-nucleoside adenosine kinase (ADK) inhibitor (IC50 = 2 nM and 50 nM in cytosolic and intact cell assays, respectively). Study conformed that ABT702 could reduce pain and inflammation in animal models, yet be clastogenic in an in vitro Chinese Hamster micronucleus assay.
Brife Description:
ADK inhibitor
ABT 702; ABT702; ABT-702; 5-(3-bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-amine
Canonical SMILES:
1.ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Jarvis MF;Yu H;Kohlhaas K;Alexander K;Lee CH;Jiang M;Bhagwat SS;Williams M;Kowaluk EA J Pharmacol Exp Ther. 2000 Dec;295(3):1156-64.
Adenosine (ADO) is an inhibitory neuromodulator that can increase nociceptive thresholds in response to noxious stimulation. Inhibition of the ADO-metabolizing enzyme adenosine kinase (AK) increases extracellular ADO concentrations at sites of tissue trauma and AK inhibitors may have therapeutic potential as analgesic and anti-inflammatory agents. ABT-702 is a novel and potent (IC(50) = 1. 7 nM) non-nucleoside AK inhibitor that has several orders of magnitude selectivity over other sites of ADO interaction (A(1), A(2A), A(3) receptors, ADO transporter, and ADO deaminase). ABT-702 was 1300- to 7700-fold selective for AK compared with a number of other neurotransmitter and peptide receptors, ion channel proteins, neurotransmitter/nucleoside reuptake sites, and enzymes, including cycloxygenases-1 and -2. ABT-702 was equipotent (IC(50) = 1.5 +/- 0. 3 nM) in inhibiting native human AK (placenta), two human recombinant isoforms (AK(long) and AK(short)), and AK from monkey, dog, rat, and mouse brain. Kinetic studies revealed that AK inhibition by ABT-702 was competitive with respect to ADO and noncompetitive with respect to MgATP(2-). AK inhibition by ABT-702 was demonstrated to be reversible after 4 h of dialysis.
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CAS 214697-26-4 ABT 702

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