Isolated arterioles incubated with ADK inhibitor, ABT-702 (0.1 μM) displayed an improved conducted vasodilation. In vivo treatment of obese ZSF1 rats with

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Selected citations for ABT 702 hydrochloride include: Hobson et al (2012) Stimulation of adenosine receptors in the nucleus accumbens reverses the expression of cocaine sensitization and cross-sensitization to DA D2 receptors in rats. ABT-702. January 2011; DOI: 10.1016/B978-008055232-3.63097-1. Authors: Michael Williams. Request full-text PDF. To read the full-text of this research, you can request a copy directly from the author. ABT 702 was also highly selective for AK inhibition as compared to other sites of ADO action including ADA, ADO receptors, and ADO transport sites [1].

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In addition, the effects of ABT-702 are possibly influenced by the activities of ADA and ENTs purine turnoverduring , which can cause ABT‐702 significantly reduced the postdischarge (10 mg kg −1, P=0.0001), and C‐fibre evoked responses (10 mg kg −1, P=0.0001) of spinal neurones in SNL rats (Figure 3A,B). In sham operated rats, however, the postdischarge was facilitated following the administration of ABT‐702. ABT 702 | ADK inhibitor | ABT702 | CAS [214697-26-4] | Axon 2289 | Axon Ligand™ with >99% purity available from supplier Axon Medchem, prime source of life science reagents for your research The involvement of adenosine signaling in the anti-inflammation effect of ABT-702 was supported by the TNF-α release blocking effect of A2AAR antagonist in AGA-treated microglial cells. SIGNIFICANCE: These results suggest a role for AK in regulating adenosine receptor signaling in the retina.

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ABT-702 is a potent non-nucleoside inhibitor of adenosine kinase (AK), a primary enzyme in the metabolic pathway of adenosine that phosphorylates adenosine at the 5′ position. ABT-702 is several orders of magnitude more selective for AK over other sites of adenosine action, such as A 1, A 2A and A 3 adenosine ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin- 3-yl)pyrido[2,3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties II. In vivo characterization in the rat.

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ABT-702 potently inhibits the activity of rat brain cytosolic AK in a concentration-dependent manner with an IC 50 value of 1.7 nM. ABT-702 also potently inhibits AK activity in intact cultured IMR-32 human neuroblastoma cells (IC 50 =51 nM), indicating that ABT-702 can penetrate the cell membrane and potently inhibit AK at its intracellular site.

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin- 3-yl)pyrido[2,3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties II. In vivo characterization in the rat. 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 (Jarvis et al., 2000). Animal preparation and experimental design Potent non-nucleoside adenosine kinase inhibitor (IC 50 = 1.7 nM), selective over other sites of adenosine interaction (A 1, A 2A and A 3 receptors, adenosine transporter and adenosine deaminase).