ABT-702, an adenosine kinase inhibitor, attenuates inflammation in diabetic retinopathy. NM Elsherbiny, S Ahmad, M Naime, AM Elsherbini, S Fulzele, .

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Abt-702

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Protection of endogenous adenosine by ABT‐702 therefore produces a marked inhibition of the noxious evoked neuronal activity in inflamed and neuropathic rats. Fassett J, Hu X, Xu X, Lu Z, Zhang P, Chen Y, et al.Adenosine kinase regulation of cardiomyocyte hypertrophy. Am J Physiol Heart Circ Physiol. 2011;300:H1722-32 pubmed publisher 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 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.

19 Nov 2014 The adenosine kinase inhibitor ABT-702 reverses neuropathic pain When compared to Day 7 wild-type (WT; white bar) mice, ABT702 (5 

MDL number MFCD03452809. PubChem Substance ID 24890688 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 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

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Abt-702

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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]. In vivo: ABT 702 had dose-dependent antinociceptive and antiinflammatory actions in a variety of animal models of nociceptive, inflammatory, and neuropathic pain. ABT-702 dihydrochloride is a potent non-nucleoside adenosine kinase inhibitor, selective over other sites of adenosine interaction like A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase. ABT-702 potently inhibits the activity of rat brain cytosolic AK in a concentration-dependent manner with an IC50 value of 1.7 nM.
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17 Apr 2019 ment with the ADK inhibitor ABT-702 could markedly attenuate cisplatin-induced acute kidney injury, tubular cell apoptosis, oxidative stress 

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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.

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]. In vivo: ABT 702 had dose-dependent antinociceptive and antiinflammatory actions in a variety of animal models of nociceptive, inflammatory, and neuropathic pain. ABT-702 was also effective in the carrageenan-induced paw edema model of acute inflammation (ED(50) = 70 micromol/kg p.o.). The antinociceptive and anti-inflammatory effects of ABT-702 were blocked by selective ADO receptor antagonists, consistent with endogenous ADO accumulation and ADO receptor activation as a mechanism of action. 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. Fingerprint Dive into the research topics of 'ABT-702, an adenosine kinase inhibitor, attenuates inflammation in diabetic retinopathy'.

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, an adenosine kinase inhibitor, attenuates inflammation in diabetic retinopathy. [Nehal M Elsherbiny, Saif Ahmad, Mohammad Naime, Ahmed M Elsherbini, Sadanand Fulzele, Mohammed M Al-Gayyar, Laila A Eissa, Mamdouh M El-Shishtawy, Gregory I Liou] PMID 23770229 Fingerprint Dive into the research topics of 'ABT-702, an adenosine kinase inhibitor, attenuates inflammation in diabetic retinopathy'. Together they form a unique fingerprint. ABT 702 Medicine & Life Sciences ABT-702 was also effective in the carrageenan-induced paw edema model of acute inflammation (ED(50) = 70 micromol/kg p.o.). The antinociceptive and anti-inflammatory effects of ABT-702 were blocked by selective ADO receptor antagonists, consistent with endogenous ADO accumulation and ADO receptor activation as a mechanism of action.